GSK143 dihydrochloride T39874

Product Introduction
Bioactivity


英文名: GSK143 dihydrochloride

描述: GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The compound demonstrates anti-inflammatory properties and hinders the recruitment of immune cells in the intestinal muscularis of mice.

体外活性: GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC 50 =4.7), LCK (pIC 50 =5.3), LYN (pIC 50 =5.4), JAK1/2/3 (pIC 50 =5.8/5.8/5.7), Aurora B (pIC 50 =4.8), hWB (pIC 50 =6.6), hERG (pIC 50 =4.7)[1]. GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC 50 of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux[2]. GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner[3]. Cell Viability Assay[2]Cell Line: Chronic lymphocytic leukaemia (CLL) cells Concentration: 10, 100, 1000, 10000 nM Incubation Time: Every 24 hours for 3 days Result: Had an IC 50 of 323 nM.

体内活性: GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg[3]. GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2]. GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T 1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V ss of 4.1 L/kg in rats[1]. Animal Model: Wild type C57NL/BL6 mice, 10-12 weeks old[3]Dosage: 0.1, 1, 3, 10 mg/kg Administration: Orally; 1.5 hours before intestinal manipulation (IM) Result: Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis. Animal Model: Male CD rats (175-200 g)[1]Dosage: 1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V ss of 4.1 L/kg.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: GSK143 dihydrochloride | GSK-143 dihydrochloride | GSK143 | GSK-143 | GSK143 Dihydrochloride | GSK 143 Dihydrochloride | GSK-143 Dihydrochloride | GSK 143

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途