CS17919
CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC50 of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases.
For research use only. We do not sell to patients.
- CAS No.: 2379346-41-3
- Formula: C22H20F4N6O2
- Molecular Weight:476.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MAP3K Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
ASK1 22.52 nM (IC50) |
In Vitro
CS17919 (0.32-10 μM; 72 h) provids potent protection in Palmitic acid-treated LO2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:L02 cells stimulated with 50 μM Palmitic acid (HY-N0830)
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Concentration:0.32 μM, 0.63 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Significantly prevented apoptosis at all doses.
In Vivo
CS17919 (50 mg/kg; po; twice daily; for 70 days) alleviates glomerular sclerosis in a DKD model[1].
CS17919 (20 mg/kg; po; twice daily; for 4 weeks) ameliorates liver inflammation and fibrosis in a NASH model[1].
Pharmacokinetic parameters of CS17919 in C57BL/6J following oral administration[1].
| Parameters | 20 mg/kg. p.o. | 50 mg/kg. p.o. |
| AUC0-∞ (h·ng/mL) | 23 113 ± 5898.47 | 58 795 ± 23 199.32 |
| AUC0-t (h·ng/mL) | 23 078 ± 5892.78 | 57 239 ± 20 606.29 |
| Cmax (ng/mL) | 4039 ± 646.90 | 5741 ± 1835 |
| MRT0-∞ (h) | 3.96 ± 0.91 | 6.43 ± 1.44 |
| T1/2 (h) | 2.20 ± 0.74 | 3.50 ± 1.86 |
| Tmax (h) | 1.50 ± 0.87 | 2.00 ± 0 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (6-8 weeks old) bearing unilateral ureteral obstruction model (UUO)[1]
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Dosage:10 mg/kg, 60 mg/kg (0.2% CMC-Na + 0.1% Tween-80)
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Administration:po; twice daily; for 11 days
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Result:Preserved kidney function and showed a non-significant tendency to alleviate kidney fibrosis.
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Animal Model:Male neonatal mice bearing chronic kidney disease (CKD)[1]
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Dosage:50 mg/kg
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Administration:po; twice daily; for 70 days
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Result:Significantly improved serum creatinine and glomerular sclerosis.
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Animal Model:Male C57BL/6J mice (6-8 weeks) bearing non-alcoholic steatohepatitis (NASH)[1]
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Dosage:20 mg/kg
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Administration:po; twice daily; for 4 weeks
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Result:Significantly improved liver inflammation and substantially reduced liver fibrosis.
Chemical Information
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CAS No. 2379346-41-3
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Molecular Weight 476.43
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Formula C22H20F4N6O2
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SMILES
CC1=C(C=C(C(F)=C1)C(NC2=NC(C3=NN=CN3[C@@H](C(F)(F)F)C)=CC=C2)=O)NC(C4CC4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)