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[CAS NO. 1448428-04-3] Selonsertib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18938 |
| Brand: | MCE |
| CAS: | 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 |
11 Publications Citing Use of MCE
- [1]Biomaterials. 2022 Sep 28;290:121817.
- [2]J Hazard Mater. 2021, 125179.
- [3]Cancers (Basel). 2022 Dec 15;14(24):6206.
- [4]Cell Biosci. 2021 Jan 7;11(1):9.
- [5]Biochim Biophys Acta Mol Basis Dis. 2022 Sep 16;166553.
- [6]Phytomedicine. 2023: 154646.
- [7]Phytother Res. 2022 Nov 24.
- [8]Int Immunopharmacol. 2023, 114: 109563.
- [9]Neurochem Res. 2022 Oct 30.
- [10]Research Square Print. 2022 Aug.
- [11]Research Square Preprint. 2021 Jul.
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
DMSO : ≥ 31 mg/mL ( 69.59 mM )
* "≥" means soluble, but saturation unknown.
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 |
-
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.
-
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
References
- [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.
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