1. MAPK/ERK Pathway
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  3. 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.

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CS17919 Chemical Structure

CS17919 Chemical Structure

CAS No. : 2379346-41-3

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Description

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[1].

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.

Apoptosis Analysis[1]

Cell Line: L02 cells stimulated with 50 μM Palmitic acid (HY-N0830)
Concentration: 0.32 μM, 0.63 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Significantly prevented apoptosis at all doses.
In Vivo

CS17919 (10-60 mg/kg; po; twice daily; for 11 days) improves kidney injury and fibrosis in the UUO model[1].
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].
1.19

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.

Animal Model: Male C57BL/6J mice (6-8 weeks old) bearing unilateral ureteral obstruction model (UUO)[1]
Dosage: 10 mg/kg, 60 mg/kg (0.2% CMC-Na + 0.1% Tween-80)
Administration: po; twice daily; for 11 days
Result: Preserved kidney function and showed a non-significant tendency to alleviate kidney fibrosis.
Animal Model: Male neonatal mice bearing chronic kidney disease (CKD)[1]
Dosage: 50 mg/kg
Administration: po; twice daily; for 70 days
Result: Significantly improved serum creatinine and glomerular sclerosis.
Animal Model: Male C57BL/6J mice (6-8 weeks) bearing non-alcoholic steatohepatitis (NASH)[1]
Dosage: 20 mg/kg
Administration: po; twice daily; for 4 weeks
Result: Significantly improved liver inflammation and substantially reduced liver fibrosis.
Molecular Weight

476.43

Formula

C22H20F4N6O2

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CS17919 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CS17919
Cat. No.:
HY-163752
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