Selonsertib (GS-4997) (Synonyms: GS-4977, GS-4997) |
| Catalog No.GC12124 |
Selonsertib (GS-4997) (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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448428-04-3
Sample solution is provided at 25 µL, 10mM.
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Selonsertib (GS-4997) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor.
ASK1, a redox-sensitive mitogen-activated protein kinase kinase kinase, functions as a key signaling node by promoting deleterious effects. ASK1 activation can cause downstream activation of the terminal MAPK kinases p38 and c-Jun N-terminal kinase, which stimulate production of inflammatory cytokines, induce fibrosis, promote apoptotic and necrotic cell death, increase aberrant cell proliferation, as well as contribute to metabolic perturbations.
In vitro: GS-4997 has been identified as a highly selective and potent ASK1 inhibitor that competed with ATP in the ASK1 catalytic kinase domain. Moreover, the ASK1 inhibition caused by GS-4997 was found to be significantly different in mechanism from bardoxolone methyl. GS- 4997 could also shut down cell signaling involved in pathogenesis, while bardoxolone methyl activated mRNA transcription in every cell exposed to drug. In addition, GS-4997 could selectively target affected cells in which the oxidative burden was high [1].
In vivo: So far, there is no animal in vivo data released.
Clinical trial: The phase II study regarding delineating study population, efficacy outcomes, treatment period as well as statistical methods to resolve specific challenges for DKD study has been designed based on the biology of oxidative stress signaling through ASK1, the biology of DKD pathogenesis, and solid statistical methods [1].
Reference:
[1] 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.
| Cas No. | 1448428-04-3 | SDF | |
| Synonyms | GS-4977, GS-4997 | ||
| 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 | ||
| Canonical SMILES | O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F | ||
| Formula | C24H24FN7O | M.Wt | 445.49 |
| Solubility | ≥ 44.5 mg/mL in DMSO, ≥ 88.8 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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