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「同位素标记抑制剂」Cyclosporin A acetate-d4

发布时间:2025-06-10     作者:德尔塔生物   分享到:

【产品介绍】:

生物活性:Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579)[1]. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM[2]. Cyclosporin A also inhibits CD11a/CD18 adhesion[3].
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.
Cyclosporin A acetate-d4 相关抗体:
Albumin Antibody
CD46 Antibody
C3 Antibody
C5b-9 Antibody
Annexin A2 Antibody
GC1q R Antibody (YA2311)
Complement factor B Antibody (YA2984)
分子量:1248.67
Formula:C64H109D4N11O13
非标记 CAS:59865-13-3
性状:固体
颜色:White to off-white
中文名称:环孢霉素A-d4;环孢素A-d4;环孢多肽A-d4;环孢灵-d4;赛斯平-d4;环孢素-d4
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:Powder:-20°C:3 years
In solvent:-80°C:6 months,-20°C:1 month
纯度 & 产品资料
纯度: 99.90%
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-246.
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[2]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5.
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[3]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25.
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[4]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428.
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[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92.
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[6]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90.
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[7]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7.
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[8]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7.
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[9]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15.
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