2. Anti-infection Metabolic Enzyme/Protease
  3. HIV HIV Integrase
  4. GSK3739936

GSK3739936  (Synonyms: BMS-986180)

目录号: HY-150080
产品使用指南

摩尔计算器

GSK3739936 (BMS-986180) 是一种有效的 HIV-1 变构整合酶 (HIV-1 allosteric integrase) 抑制剂，IC50 为 11.1 nM，EC50 为 1.7 nM。GSK3739936 也是一种弱 CYP 抑制剂 (IC50>24.3 μM)。GSK3739936 在实验动物中表现出良好的药代动力学特性，吸收快、清除率低至中等，以及口服生物利用度良好。

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GSK3739936 Chemical Structure

GSK3739936 Chemical Structure

CAS No. : 1803444-21-4

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GSK3739936 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

GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability[1].

IC50 & Target

IC50: 11.1 nM (HIV-1 integrase)[1]
EC50: 1.7 nM (HIV-1 integrase)[1]
IC50: >24.3 μM (CYP)[1]
体外研究
(In Vitro)

GSK3739936 is not cytotoxic to MT-2 cells, exhibiting CC50 values of >20 μM[1].

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

GSK3739936 相关抗体:
体内研究
(In Vivo)

GSK3739936 exhibits favorable pharmacokinetic property with rapid absorption, low to moderate clearance and excellent oral bioavailability[1].
Pharmacokinetic Parameters of GSK3739936 in Preclinical Species[1].

Male CD-1 mice Male Sprague-Dawley rats Cynomolgus monkey Male beagle dogs
IV dose (mg/kg) 1 1 1 1
CL (mL/min/kg) 5.4 5.5 14.5 2.9
t1/2 (h) 6.3 4.3 2.4 5.1
Vss (L/kg) 2.4 1.8 1.5 0.7
PO dose (mg/kg) 5 5 2 2
Cmax (nM) 2361 2762 525 2963
tmax (h) 5 2.7 2 2
AUC (nM·h) 24516 14022 2231 18471
F (%) 89 52 54 75

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

Animal Model: Male CD-1 mice, male Sprague-Dawley rats, cynomolgus monkey and male beagle dogs[1]
Dosage: 1 mg/kg for IV; 5 or 2 mg/kg for PO
Administration: PO or IV; single dosage
Result: Exhibited a low clearance in the mouse, rat, and dog with moderate to long elimination half-lives, while displays moderate clearance and a short elimination half-life in the cynomolgus monkey.
The absolute oral bioavailability ranged between 52 and 89%.
The tmax value of 2-5 h suggesting rapid absorption in all four species.
分子量

562.71

Formula

C34H43FN2O4
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

GSK3739936 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

GSK37399361803444-21-4BMS-986180GSK 3739936GSK-3739936BMS986180BMS 986180HIVHIV IntegraseHuman immunodeficiency virusHIV-1CD-1 miceSD ratscynomolgus monkeybeagle dogsInhibitorinhibitorinhibit

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