1033836-12-2|HPGDS inhibitor 1|CsnPharm

CAS No.: 1033836-12-2

HPGDS inhibitor 1 Catalog No. CSN12831

Synonyms: Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;H-PGDS Inhibitor I;MDK-36122

HPGDS inhibitor 1 is a selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.

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技术信息

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 ... more >>Disease Asthma Idiopathic Pulmonary Fibrosis Collapse <<	Phase 1	Active, not recruiting	August 2017	Australia ... more >> Linear Clinical Research Unit Perth, Australia Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6221 mL
- 13.1107 mL
- 26.2214 mL
- 5 mM
- 0.5244 mL
- 2.6221 mL
- 5.2443 mL
- 10 mM
- 0.2622 mL
- 1.3111 mL
- 2.6221 mL

技术信息

CAS号

1033836-12-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H19F4N3O

运输

蓝冰

分子量

381.37

别名

Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;H-PGDS Inhibitor I;MDK-36122

溶解度

DMSO	50.0 mg/mL (131.1 mM) warming
Water	Insoluble

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