货号:A414719 同义名:
Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;H-PGDS Inhibitor I
HPGDS inhibitor 1是一种选择性的造血前列腺素 D 合成酶(HPGDS)抑制剂,IC50 值为 0.7 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50μL*10mM(DMSO) | ¥119随货¥89 | 咨询 | |
100μL*10mM(DMSO) | ¥169随货¥119 | 咨询 | |
250μL*10mM(DMSO) | ¥299随货¥209 | 咨询 | |
500μL*10mM(DMSO) | ¥429随货¥309 | 咨询 | |
10mM*1mL(DMSO) | ¥674 | 咨询 | |
1mg | ¥251 | 咨询 | |
5mg | ¥804 | 咨询 | |
10mg | ¥1243 | 咨询 | |
50mg | ¥3028 | 咨询 |
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描述 | Hematopoietic Prostaglandin D Synthase (HPGDS) is responsible for the synthesis of PGD2 (Prostaglandin D2), a mediator of allergy and inflammation, by mast cells and Th-2 cells. HPGDS inhibitor 1 is a potent and selective HPGDS inhibitor with IC50s of 0.6 nM and 32 nM in enzyme and cell-based assays, respectively. In vitro, HPGDS inhibitor 1 had equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM). Oral administration of HPGDS inhibitor 1 (1 mg/kg and 10 mg/kg) blocked PGD2 production in the rat spleen in a time- and dose-dependent manner. Moreover, HPGDS inhibitor 1 (1 mg/mL) illustrated efficacy in a sheep model of asthma[2]. |
作用机制 | There is a favorable π-π stacking interaction between the central pyridyl ring of the compound and the Trp104 of the protein[2]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02397005 | Chronic Obstructive Pulmonary ... 展开 >>Disease Asthma Idiopathic Pulmonary Fibrosis 收起 << | Phase 1 | Active, not recruiting | August 2017 | Australia ... 展开 >> Linear Clinical Research Unit Perth, Australia 收起 << |
计算器 | ||||
存储液制备 | ![]() | 1mg | 5mg | 10mg |
1 mM 5 mM 10 mM | 2.62mL 0.52mL 0.26mL | 13.11mL 2.62mL 1.31mL | 26.22mL 5.24mL 2.62mL |
CAS号 | 1033836-12-2 |
分子式 | C19H19F4N3O |
分子量 | 381.367 |
别名 | Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;H-PGDS Inhibitor I;MDK36122 |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 | DMSO: 50 mg/mL(131.11 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |