1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor Endogenous Metabolite Drug Metabolite
  3. 5α-Tetrahydrocorticosterone

5α-Tetrahydrocorticosterone  (Synonyms: 5α-THB)

目录号: HY-113364
产品使用指南 技术支持

5α-Tetrahydrocorticosterone (5α-HB) 是一种内源性类固醇,可作为糖皮质激素受体 (glucocorticoid receptor) (GR) 的激动剂,同时也是 Corticosterone (HY-B1618) 的代谢产物。5α-Tetrahydrocorticosterone 是一种在体内中有效的局部抗炎剂。5α-Tetrahydrocorticosterone 降低大鼠肝细胞中代谢物与糖皮质激素受体-皮质酮及其 5α-还原代谢物的结合,Kd 值为 268 nM。5α-Tetrahydrocorticosterone 可用于炎症性皮肤疾病的研究。

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5α-Tetrahydrocorticosterone

5α-Tetrahydrocorticosterone Chemical Structure

CAS No. : 600-63-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5α-Tetrahydrocorticosterone (5α-HB), an endogenous steroid, is a glucocorticoid receptor (GR) agonist and a metabolite of Corticosterone (HY-B1618). 5α-Tetrahydrocorticosterone is an effective topical anti-inflammatory agent in vivo. 5α-Tetrahydrocorticosterone reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd of 268 nM. 5α-Tetrahydrocorticosterone can be used for research on inflammatory skin diseases[1].

体外研究
(In Vitro)

5α-Tetrahydrocorticosterone (0.001-100 μM) 降低大鼠肝细胞中代谢物与糖皮质激素受体-皮质酮及其 5α-还原代谢物的结合,Kd 值为268 nM[1]
5α-Tetrahydrocorticosterone (1 μM, 16 h) 增加 H4IIE 细胞中 TATPEPCK mRNA 的表达[1]
5α-Tetrahydrocorticosterone (1-10000 nM, 7 days) 以浓度依赖的方式抑制小鼠主动脉环的血管生长,EC50 值为 2512 nM[2]
5α-Tetrahydrocorticosterone (3 μM) 增加主动脉环中 Mcp1Per1 的水平,并抑制 Pecam1 的表达[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

5α-Tetrahydrocorticosterone (5 mg/kg,腹腔注射,单次给药) 对双侧肾上腺切除的小鼠表现出糖皮质激素样作用[1]
5α-Tetrahydrocorticosterone (25-200 μg,局部给药,28 天) 抑制小鼠中由巴豆油诱导的耳部肿胀[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult lean male Zucker rats (6-8 weeks) were bilaterally adrenalectomized[1]
Dosage: 5 mg/kg
Administration: i.p. for a single dose
Result: Remained low plasma corticosterone levels.
Induced a classical negative feedback effect upon the hypothalamic-pituitary-adrenal axis.
Animal Model: Male C57BL/6 mice with a single topical application of croton oil in ear skin[3]
Dosage: 25, 100, 200 μg
Administration: Local administration for 28 days
Result: Suppressed ear swelling in mice, with an ED50 of 23 μg.
Did not cause skin thinning, adrenal atrophy, weight loss, thymic involution, or raised insulin levels.
分子量

350.49

Formula

C21H34O4

CAS 号
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
参考文献
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