1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- manufacturers
- ASK1-IN-2
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- $68.00
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2026-07-27
- CAS:2541792-70-3
- Purity: 99.36%
- Supply Ability: 10g
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| | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Basic information |
| Product Name: | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- | | Synonyms: | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-;6-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-1H-indole-2-carboxamide;ASK1-IN-2;colitis,ulcerative,signal-regulating,ASK1 IN 2,ASK1IN2,inhibit,MAP kinase kinase kinase, MEKK, MAPKKK,Apoptosis,ASK1,Inhibitor,ASK-1-IN-2,MAP3K;ASK1-IN-2, 10 mM in DMSO | | CAS: | 2541792-70-3 | | MF: | C19H17FN6O | | MW: | 364.38 | | EINECS: | | | Product Categories: | | | Mol File: | 2541792-70-3.mol | ![1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Structure](CAS/20210111/GIF/2541792-70-3.gif) |
| | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Chemical Properties |
| density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (686.10 mM; Need ultrasonic) | | pka | 12.33±0.70(Predicted) | | form | Solid | | color | White to off-white |
| | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Usage And Synthesis |
| Uses | 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[1]. | | 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[1].
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[1].
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[1].
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 hng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1]. | Animal Model: | Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water[1] | | Dosage: | 25 mg/kg | | Administration: | P.o. daily for 7 days | | Result: | Induced a significant recovery of body weight loss, with an increase of +11.2%.
Decreased the disease activity index (DAI) score about a 2 unit.
Significantly prevented colon shortening.
Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.
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| Animal Model: | Male SD rats [1] | | Dosage: | 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) | | Administration: | I.v. and p.o. administration | | Result: | I.v.: CL=1.38 L/h/kg; T1/2=1.45 h.
P.o.: AUClast=4517 hng/mL; F=62.2%; T1/2=2.31 h.
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| | IC 50 | ASK1: 32.8 nM (IC50) | | References | [1] Hou S, et, al. Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis. Eur J Med Chem. 2020 Dec 24;211:113114. DOI:10.1016/j.ejmech.2020.113114 |
| | 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Preparation Products And Raw materials |
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