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中文别名 替勃龙 英文别名 Tibolone CAS号 5630-53-5 SMILES [H][C@@]12CC[C@@](O)(C#C)[C@@]1(C)CC[C@]1([H])C3=C(CC(=O)CC3)C[C@@]([H])(C)[C@@]21[H] Inchi InchiKey 分子式 Formula C21H28O2 分子量 Molecular Weight 312.453 闪点 FP NA 熔点 Melting point NA 沸点 Boiling point NA Polarizability极化度 1 密度 Density NA 蒸汽压 Vapor Pressure 溶解度Solubility 性状 NA 储藏条件 Storage conditions Tibolone使用注意事项：1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害。3.取样品的移液枪头需及时更换，必要时为避免交叉污染尽可能选择滤芯吸头。4.称量药品时选用称量纸，并无风处取药和称量以免扬撒，试剂的容器使用前务必确保干净，并消毒。5.取药品时尽量采用多个药勺分别使用，使用后清洗干净。6.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染。大规格定制：定制产品请将信息发送至sales@bio-fount.com。Experimental considerations: 1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment. 2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution. 产品说明 This compound belongs to the class of organic compounds known as oxosteroids. These are steroid derivatives carrying a C=O group attached to steroid skeleton. IntroductionUpregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R. Application1This drug's effects are owed to the activity of its metabolites in various tissues4.Upon ingestion, tibolone is quickly converted into three major metabolites:3 alpha- and 3 beta-hydroxy-tibolone, which have oestrogenic effects, and theDelta(4)-isomer, which has progestogenic and androgenic effects. The specific tissue-selective effects of tibolone occur due to the metabolism, regulation of enzymes and receptor activation that varies in different tissues of the body.The bone-conserving effects occur due to estradiol receptor activation, while the progesterone and androgen receptors are not involved in this process. Breast tissue of monkeys is not found to be stimulated after tibolone administration, as occurs with estrogen plus progesterone used in combination. This is explained by the fact that tibolone and its metabolites inhibitsulphatase and 17 beta-hydroxysteroid dehydrogenase(HSD) type I andstimulate sulphotransferase and 17 beta-HSD type II. The combined effects of this process prevent the conversion to active estrogens.In the uterus, the progestogenic activity of theDelta(4)-metaboliteand the effect on estrogen-inactivating enzymes prevent estrogenic stimulation. The mammary gland is not stimulated in currently used animal models. Tibolone has been shown to regulate estrogenic activity in several tissue types by influencing the availability of estrogenic compounds for the estradiol receptor in a selective manner2.Additionally, tibolone modulates cellular homeostasis in the breast by preventing breast tissue proliferation and stimulating cell apoptosis. Tibolone does not stimulate the endometrium because of the action of its highly stable progestogenic metabolite (Delta(4)-isomer) in combination with an effect on the sulfatase (inhibition)-sulfotransferase (stimulation) system. The estrogenic metabolites of tibolone have direct, favorable effects on the cardiovascular system and, in animal models, this drug has shown no adverse consequences.The tissue-selective effects of tibolone are the result of metabolism, enzyme regulation and receptor activation that vary in different tissues. The bone-preserving effects of tibolone are the result of estradiol receptor activation, while other steroid receptors, mainly the progesterone and androgen receptors, are not involved in this process.In a study of monkeys, breast tissue was not stimulated, which occurs with estrogen and progesterone, because tibolone and its metabolites inhibitsulfatase and 17 beta-hydroxysteroid _dehydrogenase (HSD) type I and stimulate _sulfotransferase and 17 beta-HSD type II. The simultaneous effects of this process halt conversion to active estrogens. Additionally, tibolone affects cellular homeostasis in the breast by preventing proliferation and stimulating apoptosis. Tibolone does not stimulate the endometrium due to the action of the highly stable progestogenic metabolite (Delta(4)-isomer) in combination with an effect on the sulphatase (inhibition)-sulphotransferase (stimulation) pathway1.The levels of tibolone metabolites and the alteration of hormonal activities vary according to the tissue type. In endometrial tissue theΔ4-isomerfunctions as a progestagen, however, in the brain and liver, it shows androgenic effects. In breast tissue, the primary actions of tibolone are strong inhibition of sulfatase activity and weak inhibition of 17β-hydroxysteroid dehydrogenase activity, which leads to blocking the conversion estrone sulfate to E24.TargetActionsOrganismAEstrogen receptor alphaantagonistagonistHumans Application2Inhibitor Application3 警示图 危险性 危险性警示 warning 安全声明 安全防护 备注 实验过程中防止吸入、食如，做好安全防护 对不起，暂无产品评价！