2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. BMS-823778 hydrochloride

BMS-823778 hydrochloride 是一种有效的、选择性的、具有口服活性的 11β-HSD1 抑制剂，对人 11β-HSD1 的 IC50 为 2.3 nM。

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BMS-823778 hydrochloride Chemical Structure

BMS-823778 hydrochloride Chemical Structure

CAS No. : 1140898-87-8

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BMS-823778 hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1[1].

IC50 & Target

IC50: 2.3 nM (human 11β-HSD1), 600 nM (mouse 11β-HSD1)[1]
Ki: 0.9 nM (human 11β-HSD1), 380 nM (mouse 11β-HSD1)[1]
体内研究
(In Vivo)

BMS-823778 (10-100 mg/kg; oral; once) hydrochloride 在饮食诱导肥胖 (DIO) 小鼠中表现出强烈的急性药效学作用 (ED50=34 mg/kg)[1]。

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

Animal Model: Diet-induced obese (DIO) mice[1]
Dosage: 10-100 mg/kg
Administration: Oral, once
Result: Inhibition of 11β-HSD-1 was observed as a measure of decrease in the plasma concentration of corticosterone. The ED50 was 34 mg/kg.
Animal Model: Male Balb/C mice[1]
Dosage: 5 or 10 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Single-Dose Pharmacokinetic Parameters of BMS-823778[1]
Species Route Dose (mg/kg) Cmax (µM) Tmax (h) AUC(0-24 h) (µM•h) T1/2 (h) CLTp (mL/min/kg) Vss (L/kg) F (%)
Mouse IV* 5 - - 106 5.2 2.3 1.2 -
PO** 10 10.6 ± 1.3 3 95 - - - 44

*PO Vehicle: 0.5% Methocel/0.1% Tween 80
** IV vehicle: 10% ethanol/30% propylene glycol/60% normal saline
Clinical Trial
分子量

364.27

Formula

C18H19Cl2N3O
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

BMS-823778 hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-8237781140898-87-8BMS823778BMS 82377811β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenasediet-induced obeseorally activeDIO miceInhibitorinhibitorinhibit

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