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Selonsertib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Selonsertib图片
CAS NO:1448428-04-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 445.49
Formula C24H24FN7O
CAS No. 1448428-04-3 (free base)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 31 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F
Synonyms

Selonsertib free base; GS-4997; GS4997; GS 4997; Selonsertib;

Chemical Name: 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide

实验参考方法
In Vitro

In vitro activity: Selonsertib (Also known as GS-4997) is a highly selective and potent once-daily orally available inhibitor of ASK1 (apoptosis signal-regulating kinase 1) with a pIC50 of 8.3±0.07. Selonsertib has potential anti-inflammatory, antineoplastic and anti-fibrotic activities and has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis. Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, Selonsertib was identified. Selonsertib displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.


Kinase Assay: Selonsertib (Also known as GS-4997) is a highly selective and potent once-daily orally available inhibitor of ASK1 (apoptosis signal-regulating kinase 1) with a pIC50 of 8.3±0.07. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain.


Cell Assay: An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral administration, ASK1 inhibitor GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation

In Vivo
Animal model
Formulation & Dosage
References Nephron. 2015;129(1):29-33.ACS Med Chem Lett. 2017 Feb 8;8(3):316-320. /cancer-drug/def/ask1-inhibitor-gs-4997