Description
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.
Product information
CAS Number: 2541792-70-3
Molecular Weight: 364.38
Formula: C19H17FN6O
Chemical Name: 6-fluoro-N-{6-[4-(propan-2-yl)-4H-1,2,4-triazol-3-yl]pyridin-2-yl}-1H-indole-2-carboxamide
Smiles: CC(C)N1C=NN=C1C1=CC=CC(NC(=O)C2=CC3=CC=C(F)C=C3N2)=N1
InChiKey: LYUQNMNUBOUCBX-UHFFFAOYSA-N
InChi: InChI=1S/C19H17FN6O/c1-11(2)26-10-21-25-18(26)14-4-3-5-17(23-14)24-19(27)16-8-12-6-7-13(20)9-15(12)22-16/h3-11,22H,1-2H3,(H,23,24,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (686.10 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%.
In Vivo:
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice. ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues. ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats. ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats.
Products are for research use only. Not for human use.
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