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HPGDS inhibitor 1

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Chemical Structure| 1033836-12-2 同义名 : Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;H-PGDS Inhibitor I;MDK36122
CAS号 : 1033836-12-2
货号 : A414719
分子式 : C19H19F4N3O
纯度 : 99%+
分子量 : 381.367
MDL号 : MFCD18206776
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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].
临床研究
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 <<
实验方案
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
参考文献

[1]Chris PC, John IT, et al. Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS). ACS Med. Chem. Lett., 2010, 1 (2), pp 59–63.

[2]Carron CP, et al. Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS). ACS Med Chem Lett. 2010 Feb 2;1(2):59-63.