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Product details

名称

GSK-25

分子类型

小分子

英文名称

GSK-25

货号

G649634-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor ( IC 50 =7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC 50 =398 nM, p70S6K: IC 50 =1 μM). GSK-25 inhibits P450 profile (IC 50 s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) In Vivo GSK-25 (Rat aorta IC 50 =256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure . GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:ROCK1 7 nM (IC 50 ) RSK1 398 nM (IC 50 ) p70S6K 1000 nM (IC 50 )

生化机理

GSK-25 是一种强效、选择性和口服生物利用度高的 ROCK1 抑制剂（IC 50 =7 nM）。GSK-25 对 31 种激酶（>100 倍）以及 RSK1 和 p70S6K 都具有良好的选择性（RSK1：IC 50 =398 nM，p70S6K：IC 50 =1 μM）。GSK-25 可抑制 P450

CAS号

874119-56-9

分子式

C24H16Cl2F2N6O

分子量

513.33 g/mol

PubChem编号

11548023

Isomeric SMILES

CC1=C(C(N=C(N1)C2=CC(=NC=C2)Cl)C3=C(C=C(C=C3)Cl)F)C(=O)NC4=C(C=C5C(=C4)C=NN5)F

IIUPAC Name

4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide

INCHI

1S/C24H16Cl2F2N6O/c1-11-21(24(35)32-19-6-13-10-30-34-18(13)9-17(19)28)22(15-3-2-14(25)8-16(15)27)33-23(31-11)12-4-5-29-20(26)7-12/h2-10,22H,1H3,(H,30,34)(H,31,33)(H,32,35)

InChi Key

KZYAHEIPPAPADQ-UHFFFAOYSA-N

Smiles

CC1=C(C(N=C(N1)C2=CC(=NC=C2)Cl)C3=C(C=C(C=C3)Cl)F)C(=O)NC4=C(C=C5C(=C4)C=NN5)F

PubChem CID

11548023

溶解性

DMSO : 50 mg/mL (97.40 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

512.073 Da

单同位素质量Monoisotopic Mass

512.073 Da

拓扑极表面积Topological Polar Surface Area

95.100 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

875

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

4.3

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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