| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87961-1mg |
≥98% | ￥800.00 |
10 | - | - | - | - |
|
S87961-5mg |
≥98% | ￥2000.00 |
10 | - | - | - | - |
|
S87961-10mg |
≥98% | ￥3200.00 |
8 | - | - | - | - |
|
S87961-25mg |
≥98% | ￥6251.00 |
5 | - | - | - | - |
|
S87961-50mg |
≥98% | ￥10000.00 |
3 | - | - | - | - |
|
S87961-100mg |
≥98% | ￥16000.00 |
2 | - | - | - | - |
|
| 产品描述： | HPGDS inhibitor 2 is a potent, selective hematopoietic prostaglandin D synthase (h-pgds) inhibitor, IC50 = 9.9 nm | ||||||||||||||||||||
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| 靶点： | PGE Synthase;PGESynthase | ||||||||||||||||||||
| 体外研究： | GSK2894631A(IC50 = 9.9 nM, LE = 0.42) is a potent, competitive, and reversible inhibitor of H-PGDS. GSK2894631A exhibited good H-PGDS cellular activity (RBL IC50 = 160 nM) in a rat basophilic leukemia (RBL) cell PGD2 production assay | ||||||||||||||||||||
| 体内研究： | GSK2894631A had a low i.v. clearance (Cl = 5.6 mL/min/kg), moderate i.v. steady state volume of distribution (VSS = 1.7 l/kg), long i.v. terminal half-life (t1/2 = 3.8 hr), and good oral exposure (p.o. DNAUC = 1800 ng/hr/mL, F = 61%) in mice. It attenuated PGD2 production in an acute in vivo murine mast cell degranulation model (ED50 = 0.032 mg/kg, EC50 = 21 nM) of inflammation. Unfortunately, at higher doses (≥10 mg/kg) in a chronic eccentric muscle damage model (vide infra Fig. 6) in mice, 1a-treated animals exhibited seizure-like activity at day four of dosing. | ||||||||||||||||||||
| 参考文献： | 1. Rc A , Dnd A , Yd A , et al. The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure[J]. Bioorganic & Medicinal Chemistry, 2020, 28( 23). | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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北京