[CAS NO. 1448428-04-3] Selonsertib

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PRODUCTS SPECIFICATIONS [1448428-04-3]

Catalog

HY-18938

Brand

MCE

CAS

1448428-04-3

DESCRIPTION [1448428-04-3]

Overview

MDL	MFCD29920355
Molecular Weight	445.49
Molecular Formula	C24H24FN7O
SMILES	O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F

For research use only. We do not sell to patients.

11 Publications Citing Use of MCE

Summary

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 ( ASK1 ) inhibitor with a pIC ₅₀ of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

IC50 & Target

ASK1

8.3 (pIC ₅₀ )

In Vitro

Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis ^[1] . Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02234141	Gilead Sciences	Pulmonary Arterial Hypertension	November 2014	Phase 2
NCT02854631	Gilead Sciences	Alcoholic Hepatitis (AH)	September 1, 2016	Phase 2
NCT02509624	Gilead Sciences	Diabetic Kidney Disease	August 18, 2015	Phase 1
NCT02177786	Gilead Sciences	Diabetic Kidney Disease	June 2014	Phase 2
NCT03087968	HepQuant, LLC	Severe Alcoholic Hepatitis	July 31, 2016	Early Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL ( 69.59 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2447 mL	11.2236 mL	22.4472 mL
5 mM	0.4489 mL	2.2447 mL	4.4894 mL
10 mM	0.2245 mL	1.1224 mL	2.2447 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.62 mg/mL (5.88 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

* All of the co-solvents are available by MCE.