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Ramelteon-d3,雷美替胺-d3; TAK-375-d3「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Ramelteon-d3 is a deuterium-labelled Ramelteon (HY-A0014).分子量:262.36Formula:C16H18D3NO2CAS 号:1432057-38-9非标记 CAS:196597-26-9性状:固体颜色:White to off-white中文名称:雷美替胺-d3;瑞美替昂-d3;拉米替隆-d3;雷美尔通-d3;瑞美替胺-d3运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Powder:-20°C:3 years,4°C:2 yearsIn solvent:-80°C:6 months,-20°C:1 month
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Alosetron-d3,阿洛司琼-d3; GR 68755-d3; GR 68755X-d3「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Alosetron-d3 is a deuterium labeled Alosetron. Alosetron is a serotonin 5HT3-receptor antagonist[1].分子量:297.37Formula:C17H15D3N4OCAS 号:1190043-13-0非标记 CAS:122852-42-0中文名称:阿洛司琼-d3;洛曲尼斯-d3;罗肠兴-d3运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (524 KB)产品使用指南 (1538 KB)参考文献[1]. Harris LA, et al. Alosetron: an effective treatment for diarrhea-predominant irritable bowel syndrome. Womens Health (Lond). 2007 Jan;3(1):15-27. [Content Brief]
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Moxifloxacin-d3 hydrochloride,莫西沙星盐酸盐-d3; BAY 12-8039-d3「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Moxifloxacin-d3 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin hydrochloride is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2][3].IC50 & Target:Quinolone体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Moxifloxacin-d3 hydrochloride 相关抗体:MRP2 AntibodyElongation factor 2 Antibody (YA962)Elongation factor 2 Antibody (YA964)PU.1/SPI1 Antibody (YA1116)Sulfadimidine Antibody (YA906)Elongation factor 2 Antibody (YA963)Anthrax Protective gen Antibody (YA1060)Elongation factor 1 gamma Antibody (YA2004)Pulmonary Surfactant Associated Protein D Antibody (YA2107)Cathelicidin Antibody (YA2380)Elongation Factor Ts Antibody (YA2524)Elongation Factor 1A2 Antibody (YA2879)BPI Antibody (YA3068)MetRS Antibody (YA3196)分子量:440.91Formula:C21H22D3ClFN3O4CAS 号:2734919-98-1非标记 CAS:151096-09-2中文名称:盐酸莫西沙星-d3;莫西沙星盐酸盐-d3运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (5
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Linuron-d6,利谷隆-d6「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Linuron-d6 is the deuterium labeled 3-Bromo-L-tyrosine[1].体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[75].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Linuron-d6 相关抗体:Androgen receptor AntibodyPOMC Antibody (YA1619)分子量:255.13Formula:C9H4D6Cl2N2O2CAS 号:1219804-76-8非标记 CAS:330-55-2中文名称:利谷隆-d6运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (518 KB)产品使用指南 (1538 KB)参考文献[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. [Content Brief]
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Cyclobenzaprine-d6 hydrochloride,盐酸环苯扎林-d6; MK130-d6 hydrochloride「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Cyclobenzaprine-d6 (hydrochloride) is deuterium labeled Cyclobenzaprine (hydrochloride).体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Cyclobenzaprine-d6 hydrochloride 相关抗体:MTNR1A Antibody分子量:317.89Formula:C20H16D6ClNCAS 号:2748492-38-6非标记 CAS:6202-23-9中文名称:阿米替林EP杂质B-d6运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (525 KB)产品使用指南 (1538 KB)参考文献[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief][2]. Kobayashi, H., Y. Hasegawa, and H. Ono, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol, 1996. 311(1): p. 29-35. [Content Brief][3]. Honda, M., T. Nishida, and H. Ono, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol, 2003. 458(1-2): p. 91-9. [Content Brief]
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Itopride-d6 hydrochloride,盐酸伊托必利-d6; HSR803-d6 hydrochloride「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].IC50 & Target:D2 Receptor体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Itopride-d6 hydrochloride 相关抗体:CHRNA9 AntibodyDRD2 AntibodyChAT AntibodyDopamine Receptor D3 Antibody (YA1742)DOPA Decarboxylase Antibody (YA2428)Dopamine Receptor D1 Antibody (YA3270)Torsin 1A Antibody (YA2935)PITX3 Antibody (YA2974)HMBS Antibody (YA3061)分子量:400.93Formula:C20H21D6ClN2O4CAS 号:1346601-02-2非标记 CAS:122892-31-3中文名称:盐酸伊托必利-d6;依托必利盐酸盐-d6运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (525 KB)产品使用指南 (1538 KB)参考文献[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief][2]. Hyun Chul Lim, et al. Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro. Effect of Itopride
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Phenylephrine-d6 hydrochloride,盐酸去氧肾上腺素-d6; (R-(--Phenylephrine-d6 hydrochloride; L-Phenylephrine-d6 hydrochloride「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Phenylephrine-d6 hydrochloride 相关抗体:BNSP AntibodyFACL4 AntibodyBrdU Antibody (YA578)GAPDH AntibodyGlucose 6 Phosphate Dehydrogenase AntibodyMETTL3 AntibodyTSG101 AntibodyAlkaline Phosphatase AntibodyCalnexin Antibody (YA573)Lamin A/C AntibodyLamin B1 AntibodyLAMP1 AntibodyLAMP2 Antibody (YA713)LAMP2a AntibodyNQO1 Antibody (YA697)NQO1 Antibody (YA261)OPA1 AntibodyRBM3 AntibodySynaptophysin Antibody (YA043)Laminin beta 1 AntibodyHeme Oxygenase 1 AntibodyKi67 Antibody (YA717)Ki67 Antibody (YA322)Asparagine Synthetase AntibodyCalnexin AntibodyKi67 Antibody (YA001)Osteopontin AntibodySynaptophysin Antibody (YA664)TREM2 AntibodyGAPDH Antibody (YA848)分子量:209.70Formula:C9H8D6ClNO2CAS 号:1089675-56-8非标记 CAS:61-76-7中文名称:盐酸去氧肾上腺素-d6运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 &
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Crystal Violet-d6,结晶紫-d6; Basic Violet 3-d6; Gentian Violet-d6; Methyl Violet 10B-d6「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Crystal Violet-d6 is the deuterium labeled Boc-Glycine[1].体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[75].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.分子量:414.02Formula:C25H24D6ClN3CAS 号:1266676-01-0非标记 CAS:548-62-9中文名称:结晶紫-d6;龙胆紫-d6;甲紫-d6;甲基紫-d6运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (521 KB)产品使用指南 (1538 KB)参考文献[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. [Content Brief]
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Venlafaxine-d6-1,文拉法辛-d6-1; Wy 45030-d6-1「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Venlafaxine-d6-1 相关抗体:Serotonin Transporter Antibody (YA1638)HTR7 Antibody (YA2796)HTR2C Antibody (YA3364)分子量:283.44Formula:C17H21D6NO2CAS 号:940297-06-3非标记 CAS:93413-69-5中文名称:文拉法辛-d6-1运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.纯度 & 产品资料Data Sheet (532 KB)产品使用指南 (1538 KB)参考文献[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief][2]. Bymaster FP, et al. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80. [Content Brief][3]. Goeringer KE, et al. Postmortem tissue concentrations of venlafaxine. Forensic Sci Int. 2001 Sep 15;
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Lidocaine-d6 hydrochloride,盐酸利多卡因-d6; Lignocaine-d6 hydrochloride「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Lidocaine-d6 hydrochloride 相关抗体:MEK1/2 AntibodyERK1/2 AntibodyPhospho-ERK1/2 (Thr202/Tyr204)/(Thr185/Tyr187) AntibodyNF-KB p65 AntibodyPhospho-ERK1/2 (Thr202/Tyr204)/(Thr185/Tyr187) Antibody (YA455)Phospho-NF-KB p65 (Ser536) AntibodyE-Cadherin Antibody (YA470)Fatty Acid Synthase Antibody (YA766)DYKDDDDK Tag (FLAG) AntibodyGAPDH AntibodyGFP Antibodyp53 Antibody (YA250)RUNX2 AntibodyPhospho-NF-κB p65 (Ser529) AntibodyFerritin Heavy Chain AntibodyCOX2 AntibodyCtip2 AntibodyCyclin D1 Antibody (YA485)Cytochrome C AntibodyNF-KB p65 Antibody (YA267)ERK2 Antibodyc-Myc AntibodyCyclin E1 AntibodyPhospho-MEK1 (Ser298) AntibodyxCT Antibody
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Olaparib-d4-1,AZD2281-d4-1; KU0059436-d4-1「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘代因其可能影响药物的药代动力学和代谢特征而受到关注。德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Olaparib-d4-1 相关抗体:PARP1 AntibodyPARP2 AntibodyCleaved PARP AntibodyCleaved-PARP1 AntibodyPARP1 Antibody (YA245)StAR AntibodySSB Antibody (YA668)GTF2H1 Antibody (YA1067)BRAT1 Antibody (YA2294)BRCC36 Antibody (YA2298)Killin Antibody (YA3144)分子量:438.49Formula:C24H19D4FN4O3CAS 号:2143107-55-3非标记 CAS:763113-22-0性状:固体颜色:White to off-white中文名称:奥拉帕尼 d4运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Powder:-20°C:3 years,4°C:2 yearsIn solvent:-80°C:6 months,-20°C:1 month
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Tamoxifen-d5,ICI 47699-d5; (Z-Tamoxifen-d5; trans-Tamoxifen-d5「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].IC50 & Target[1][2]Estrogen receptorHSP90体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘代因其可能影响药物的药代动力学和代谢特征而受到关注[1]。德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.Tamoxifen-d5 相关抗体:ERK1/2 AntibodyE-Cadherin Antibody (YA470)Fatty Acid Synthase Antibody (YA766)DYKDDDDK Tag (FLAG) AntibodyGAPDH AntibodyGFP Antibodyp53 Antibody (YA250)RUNX2 AntibodyFerritin Heavy Chain AntibodyHsp70 1B AntibodyCOX2 AntibodyCtip2 AntibodyCyclin D1 Antibody (YA485)Cytochrome C AntibodyHsp70 Antibody (YA359)Hsp90 alpha Antibodyc-Myc AntibodyCyclin E1 AntibodyHsc70 AntibodyAIF Antibody (YA636)ALIX AntibodyCNPase AntibodyCortactin AntibodyCOX IV AntibodyCOX2/Cyclooxygenase 2 AntibodyCyclin A2 AntibodyCyclin B1 Antibody (YA486)DR5 AntibodyDrosha AntibodyE-Cadherin Antibody (YA778)分子量:376.55Formula:C26H24D5NOCAS 号:157698-32-3非标记 CAS:10540-29-1性状:固体颜色:White to off-white中文名称:他莫昔芬 d5运输条件:Room temperature in continental US; may vary elsewhere.储存方式:Powder:-20°C:3 years,4°C:2 yearsIn solvent:-80°C:6 months,-20°C:1 month
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(E-Ferulic acid-d3,(E-Coniferic acid-d3「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299[1].体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘代因其可能影响药物的药代动力学和代谢特征而受到关注[1]。德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.(E)-Ferulic acid-d3 相关抗体:BNSP AntibodyFACL4 AntibodyBrdU Antibody (YA578)Bcl-2 AntibodyGAPDH AntibodyBeta-Catenin AntibodyBcl2 AntibodyFerritin Heavy Chain AntibodyGlucose 6 Phosphate Dehydrogenase AntibodyBax Antibody (YA591)METTL3 AntibodyTSG101 AntibodyAlkaline Phosphatase AntibodyBad AntibodyBak Antibody (YA592)BAX Antibody (YA825)Bcl-XL AntibodyBim AntibodyBNIP3 AntibodyCalnexin Antibody (YA573)Lamin A/C AntibodyLamin B1 AntibodyLAMP1 AntibodyLAMP2 Antibody (YA713)LAMP2a AntibodyNQO1 Antibody (YA697)NQO1 Antibody (YA261)OPA1 AntibodyPUMA AntibodyRBM3 Antibody分子量:197.20Formula:C10H7D3O4CAS 号:860605-59-0非标记 CAS:1135-24-6性状:固体颜色:White to off-white中文名称:反式-阿
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L-5-Hydroxytryptophan-d4,5-羟基色氨酸-d4; L-5-HTP-d4; Oxitriptan-d4「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:L-5-Hydroxytryptophan-d4 (L-5-HTP-d4; Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[1]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[2][3][4][5][6].体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.L-5-Hydroxytryptophan-d4 相关抗体:BNSP AntibodyFACL4 AntibodyBrdU Antibody (YA578)GAPDH AntibodyGlucose 6 Phosphate Dehydrogenase AntibodyMETTL3 AntibodyTSG101 AntibodyAlkaline Phosphatase AntibodyCalnexin Antibody (YA573)Lamin A/C AntibodyLamin B1 AntibodyLAMP1 AntibodyLAMP2 Antibody (YA713)LAMP2a AntibodyNQO1 Antibody (YA697)NQO1 Antibody (YA261)OPA1 AntibodyRBM3 AntibodySynaptophysin Antibody (YA043)Laminin beta 1 AntibodyHeme Oxygenase 1 AntibodyKi67 Antibody (YA717)Ki67 Antibody (YA322)Asparagine Synthetase AntibodyCalnexin AntibodyKi67 Antibody (YA001)Osteopontin AntibodySynaptophysin Antibody (YA664)TREM2 AntibodyGAPDH Antibody (YA848)分子量:224.25Formula:C11H8D4N2O3CAS 号:1246818-91-6非标记 CAS:4350-09-8性状:固体颜色:Light yellow to light brown中文名称:L-5-羟色氨酸-d4运输条件:Room temperature in continental U
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Retinoic acid-d5,维生素A酸-d5; Vitamin A acid-d5; all-trans-Retinoic acid-d5; ATRA-d5「同位素标记抑制剂」
作者:德尔塔生物 日期:2025-08-13
生物活性:Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[1][2][3][4][5].体外研究(In Vitro):氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。Retinoic acid 是维生素 A 的一种高效衍生物,几乎所有必需的生理过程和功能都需要 Retinoic acid,因为它参与超过 530 种不同基因的转录调节。Retinoic acid 通过作为 Retinoic acid 受体 (RARα-γ) 的激活配体发挥其作用,Retinoic acid 受体与 Retinoic acid X 受体 (RXRα-γ) 形成异二聚体[2]。 Retinoic acid 具有高亲和力和同种型选择性,它以低亲和力与 PPARα 和 PPARγ 结合,Kd 值为 100-200 nM。 相比之下,Retinoic acid 与 PPARβ/δ 结合的 Kd 为 17 nM[3]。未分化的 P19 细胞表达 Retinoic acid (RA) 受体 RARα、RARβ、RARγ 和 PPARβ/δ,以及 Retinoic acid 结合蛋白 CRABP-II 和 FABP5。Retinoic acid 处理细胞诱导分化导致 CRABP-II 的瞬时上调和 FABP5 的下调,这在各自的蛋白质和 mRNA 水平上观察到。 在最初的下降之后,与未分化的 P19 细胞相比,成熟神经元中 FABP5 蛋白和 mRNA 的水平增加了 2-2.5 倍。 诱导分化不会显着影响 RARα 或 PPARβ/δ 的水平。 到第 4 天,RARγ mRNA 的水平降低了约 5 倍,并且在成熟神经元中保持较低水平[4]。Retinoic acid 是一种来源于视黄醇(维生素 A)的形态发生素,在细胞生