GSK-25
- Product Name
- GSK-25
- CAS No.
- 874119-56-9
- Chemical Name
- GSK-25
- Synonyms
- GSK-25;GSK25;GSK 25;GSK-25, 10 mM in DMSO;4-(4-Chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4;4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide;4-(4-Chloro-2-fluorophenyl)-2-(2-chloro-4-pyridyl)-N-(6-fluoro-5-indazolyl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide;4-(4-Chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxamide;5-PyriMidinecarboxaMide, 4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-Methyl-;Rho-associated kinase,ROK,ROCK,Rho-associated protein kinase,S6K,bioavailable,Ribosomal S6 Kinase (RSK),Rho-kinase,Inhibitor,p70S6K,selective,pressure,P450,inhibit,GSK-25,GSK 25,blood,orally
- CBNumber
- CB82621139
- Molecular Formula
- C24H16Cl2F2N6O
- Formula Weight
- 513.33
- MOL File
- 874119-56-9.mol
GSK-25 Property
- Boiling point:
- 751.7±60.0 °C(Predicted)
- Density
- 1.57±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 100 mg/mL (194.81 mM)
- form
- Solid
- pka
- 11.61±0.40(Predicted)
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0003310
- Product name
- GSK-25
- Purity
- 99.68%
- Packaging
- 5mg
- Price
- $105
- Updated
- 2021/12/16
- Product number
- CS-0003310
- Product name
- GSK-25
- Purity
- 99.68%
- Packaging
- 10mg
- Price
- $178
- Updated
- 2021/12/16
- Product number
- CS-0003310
- Product name
- GSK-25
- Purity
- 99.68%
- Packaging
- 25mg
- Price
- $255
- Updated
- 2021/12/16
- Product number
- KIN0001346
- Product name
- GSK-25
- Purity
- 95.00%
- Packaging
- 1MG
- Price
- $340.2
- Updated
- 2021/12/16
- Product number
- CS-0003310
- Product name
- GSK-25
- Purity
- 99.68%
- Packaging
- 50mg
- Price
- $390
- Updated
- 2021/12/16
GSK-25 Chemical Properties,Usage,Production
Uses
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 μM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].
in vivo
GSK-25 (Rat aorta IC50=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[1].
?
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)[1].
IC 50
ROCK1: 7 nM (IC50); RSK1: 398 nM (IC50); p70S6K: 1000 nM (IC50)
References
[1] Sehon CA, et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4. DOI:10.1021/jm8005096
GSK-25 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK-25 Suppliers
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