| 名称 | GSK143 |
| 描述 | GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addition, GSK143 exhibits promising anti-inflammatory properties by reducing inflammation and impeding the recruitment of immune cells in the intestinal muscularis of mice. |
| 体外活性 | GSK143 (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 (10-10000 nM; every 24 h for 3 days) has an IC 50 of 323 nM in CLL cells. GSK 143 (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux[2]. GSK143 (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 h 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 | Shipping with blue ice/Shipping at ambient temperature. |
| 关键字 | GSK-143 | GSK143 | GSK 143 |
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