2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. SKI2852

SKI2852 是一种有效的、选择性的、具有口服活性的 11β-羟基类固醇脱氢酶 1 型(11β-HSD1) 抑制剂，其对 mHSD1 和 hHSD1 的 IC50 分别为 1.6 nM 和 2.9 nM。

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SKI2852 Chemical Structure

SKI2852 Chemical Structure

CAS No. : 1346554-47-9

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SKI2852 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC50s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively[1].

IC50 & Target

IC50: 1.6 nM (mHSD1), 2.9 nM (hHSD1)[1]
体外研究
(In Vitro)

SKI2852 在稳定转染人 11β-HSD1 cDNA 的 HEK293 细胞中抑制 11β-HSD1 的 IC50 为 4.4 ± 0.5 nM[1]。
SKI2852 的酰胺羰基与 Ser170 的羟基侧链建立了中心氢键相互作用，Ser170 是确定11β-HSD1 活性的催化三联体之一 (Ser170, Tyr183 和 Lys 187)[1]。

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

SKI2852 相关抗体:
体内研究
(In Vivo)

SKI2852 (20 mg/kg; oral; once daily for 25 days) 可显著降低 ob/ob 小鼠的血糖和 HbA1c 水平，并改善脂质谱[1]。
In Vivo PK Data for SKI2852[1]

species iva pob
CL (L/kg/h) Vss (L/kg) t1/2 (h) AUC (μg × h/mL) Cmax (μg/mL) tmax (h) AUC (μg × h/mL) F (%)
mousec 0.42 1.1 1.7 2.35 2.21 1.0 11.26 96
ratc 0.93 2.1 1.8 1.12 1.02 1.3 3.39 60
dogd 0.36 2.4 4.7 1.47 1.12 2.1 11.52 98

a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. b0.5% methylcellulose and 1% Tween80 was used as vehicle. cDosed iv at 1 mg/kg, po at 5mg/kg. dDosed iv at 0.5 mg/kg, po at 4 mg/kg.

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

Animal Model: ob/ob mice, diet-induced obesity (DIO) model[1]
Dosage: 20 mg/kg
Administration: Oral, once daily for 25 days
Result: Efficiently reduced postprandial glucose and/or blood HbA1c levels and suppressed hepatic mRNA levels of gluconeogenic enzymes. Clearly enhanced hepatic and whole-body insulin sensitivities in a hyperinsulinemic-euglycemic clamp experiment in DIO mice.
Animal Model: C57BL/6 mice, rats and dogs[1]
Dosage: 0.5 or 4 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic profiles.
分子量

543.65

Formula

C27H34FN5O4S
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

SKI2852 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

SKI28521346554-47-9SKI 2852SKI-285211β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenaseHEK293HbA1cdiet-induced obesityDIOdiabetesInhibitorinhibitorinhibit

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目录号：
HY-19325
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