ASK1-IN-2 - ≥98% , CAS No.2541792-70-3

CAS: 2541792-70-3 Cat. No.: A648376 分子式: C₁₉H₁₇FN₆O 分子量: 364.38 PubChem CID: 155671000

グレード＆純度 ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) , with an IC 50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis

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%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (T 1/2 =1.45 h) in rats . ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUC last =4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T 1/2 =2.31 h) in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water 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 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; T 1/2 =1.45 h. P.o.: AUC last =4517 h•ng/mL; F=62.2%; T 1/2 =2.31 h.

Form:Solid

IC50& Target:ASK1 32.8 nM (IC 50 )

仕様

仕様と純度

≥98%

生化学的・生理学的メカニズム

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) , with an IC 50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥98%

名前と識別子

カノニカル・スマイル

CC(C)N1C=NN=C1C2=NC(=CC=C2)NC(=O)C3=CC4=C(N3)C=C(C=C4)F

IUPAC Name

6-fluoro-N-[6-(4-propan-2-yl-1,2,4-triazol-3-yl)pyridin-2-yl]-1H-indole-2-carboxamide

InChIKey

LYUQNMNUBOUCBX-UHFFFAOYSA-N

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)

PubChem CID

155671000

分子量

364.38

化学的性質と物理的性質

• 溶解度: DMSO : 250 mg/mL (686.10 mM; Need ultrasonic)