1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-
- CAS No.
- 2541792-70-3
- Chemical Name:
- 1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-
- Synonyms
- ASK1-IN-2;ASK1-IN-2, 10 mM in DMSO;6-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-1H-indole-2-carboxamide;1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]-;colitis,ulcerative,signal-regulating,ASK1 IN 2,ASK1IN2,inhibit,MAP kinase kinase kinase, MEKK, MAPKKK,Apoptosis,ASK1,Inhibitor,ASK-1-IN-2,MAP3K
- CBNumber:
- CB28239271
- Molecular Formula:
- C19H17FN6O
- Molecular Weight:
- 364.38
- MDL Number:
- MFCD33548891
- 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]- price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0145639 | ASK1-IN-2 98.49% | 2541792-70-3 | 5mg | $350 | 2021-12-16 | Buy |
ChemScene | CS-0145639 | ASK1-IN-2 98.49% | 2541792-70-3 | 10mg | $580 | 2021-12-16 | Buy |
ChemScene | CS-0145639 | ASK1-IN-2 98.49% | 2541792-70-3 | 25mg | $1100 | 2021-12-16 | Buy |
ChemScene | CS-0145639 | ASK1-IN-2 98.49% | 2541792-70-3 | 50mg | $1700 | 2021-12-16 | Buy |
ChemScene | CS-0145639 | ASK1-IN-2 98.49% | 2541792-70-3 | 100mg | $2500 | 2021-12-16 | Buy |
1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Chemical Properties,Uses,Production
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 h?ng/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. |
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 h?ng/mL; F=62.2%; T1/2=2.31 h. |
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
Raw materials
Preparation Products
1H-Indole-2-carboxamide, 6-fluoro-N-[6-[4-(1-methylethyl)-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 12952 | 65 |
Zhengzhou HSH Science & Technology Co., Ltd. | 0371-55932928 18937192232 | 1282296214@qq.com | China | 495 | 55 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4611 | 55 | |
Shanghai Beckham Medical Technology Co., Ltd | 021-13816613772 13816613772 | huahero21@sina.com | China | 996 | 55 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
Shanghai Chaolan Chemical Technology Center | 021-QQ:65489617 15618227136 | Sales@ATKchemical.com | China | 9342 | 58 |
Shandong Jirun Biomedical Technology Co., Ltd. | 0539-0539-8613587 17661611089 | 2639273505@qq.com | China | 185 | 58 |