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Selonsertib

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

Product Specifications

CAS Number

[1448428-04-3]

Product Name Alternative

GS-4997

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; MAP3K

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Selonsertib.html

Purity

99.05

Solubility

DMSO : 66.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F

Molecular Formula

C24H24FN7O

Molecular Weight

445.49

Precautions

H302, H315, H319, H335

References & Citations

[1]Lanier M, et al. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure. ACS Med Chem Lett. 2017 Feb 8;8 (3) :316-320.|[2]Lin JH, et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129 (1) :29-33.|[3]Loomba R, et al. The ASK1 inhibitor selonsertib in patients with nonalcoholic steatohepatitis: A randomized, phase 2trial. Hepatology. 2018 Feb;67 (2) :549-559.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

MAP3K5/ASK1

Available Sizes

Curated Selection

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