4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide
GW788388
CAS: 452342-67-5
Molecular Formula: C25H23N5O2
4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide - Names and Identifiers
4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide - Physico-chemical Properties
| Molecular Formula | C25H23N5O2 |
| Molar Mass | 425.48 |
| Density | 1.34 |
| Solubility | DMSO 33 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Appearance | solid |
| Color | Off-white |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| In vitro study | GW788388 has anti-TGF-β activity in cell assays with an IC50 of 93 nM. GW788388 inhibits activin type II receptor but does not inhibit bone morphogenetic protein (BMP) type II receptor. GW788388 from 4 nM to 15 μm showed no cytotoxicity on mammary (NMuMG), MDA-MB-231, renal cell carcinoma (RCC)4, and U2OS cells in Namru mice. GW788388 inhibits TGF-β-induced Smad activation and suppresses target gene expression, reducing epithelial-mesenchymal changes and fibrogenesis. GW788388 inhibits growth regulated by ALK5, ALK4, ALK7 and TGF-β. |
| In vivo study | GW788388 shows an appropriate pharmacokinetic profile in mice (plasma clearance less than 40 mL/min/kg, half-life greater than 2 hours). GW788388 at a dose of 10 mg/kg acted on the renal fibrosis model induced by puromycin aminonuclear glycoside, and significantly induced collagen A1 mRNA expression by 80%. GW788388 at a dose of 2 mg/kg in rats with advanced diabetic nephropathy reduced TGF-β signaling and effectively reduced fibrogenesis. Treatment of myocardial infarction (MI) rats with GW788388 significantly reduced contractile function and decreased activated Smad2, α-SMA, and collagen I. GW788388 acts on myocardial infarction (MI) rats and also reduces cardiomyocyte hypertrophy. GW788388 at a dose of 2 mg/kg in animals injected with bleomycin decreased the fibrous response. |
4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide - Introduction
GW788388, a potent, selective ALK5 inhibitor with an IC50 of 18 nM, also inhibits other TGF-βI and II receptor kinase activities, but not BMP II receptors.
Last Update：2022-10-16 17:41:40
4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide - Reference Information
| biological activity | GW788388 is an effective and selective ALK5 inhibitor with IC50 of 18 nM, which also inhibits other TGF-βI and II receptor kinase activities, but does not inhibit BMP II receptors. |
| target | IC50: 18 nM (ALK5) |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: GW788388 Visit Supplier Webpage Request for quotationCAS: 452342-67-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide
2-ETHOXYNAPHTHALENE-1-CARBOXYLIC ACID
吲哚[1,2-A]吡嗪
2-ETHOXYNAPHTHALENE-1-CARBOXYLIC ACID
吲哚[1,2-A]吡嗪