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HPGDS inhibitor 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
HPGDS inhibitor 1图片
CAS NO:1033836-12-2
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
HPGDS inhibitor 1 是一种有效、选择性和口服活性的造血前列腺素 D 合成酶 (HPGDS) 抑制剂，在酶和细胞试验中的 IC50 分别为 0.6 nM 和 32 nM。
Cas No.1033836-12-2
别名6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺
化学名6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
Canonical SMILESC1CN(CCC1NC(=O)C2=CN=C(C=C2)C3=CC(=CC=C3)F)CC(F)(F)F
分子式C19H19F4N3O
分子量381.37
溶解度DMF: 5 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

HPGDS inhibitor 1 is an oral potent and selective inhibitor of hematopoietic prostaglandin D synthase (HPGDS) with IC50 value of 0.7nM [1].

Prostaglandin D2 (PGD2) is a mediator of allergy and inflammation. It is isomerized from PGH2 by PGDS. This production is important in airway allergic and inflammatory processes. HPGDS inhibitor 1 has a 3-fluorine substituent, making it stable in the in vitro human microsome assay. It has potent effects in enzyme assay and cellular assay with IC50 values of 0.7nM and 32nM, respectively. In addition, the potency is equal against purified HPGDS from various species with IC50 values ranging from 0.5-2.3nM. Besides that, HPGDS inhibitor 1 is selective against HPGDS over other relevant human enzymes including L-PGDS, mPGES, COX-1, COX-2 and 5 LOX [1].

In a model of antigen-induced airway response in allergic sheep, treatment of HPGDS inhibitor 1 completely prevents the late asthma reaction and blocks the Airway hyper-responsiveness [1].

References:
[1] Carron C P, Trujillo J I, Olson K L, et al. Discovery of an oral potent selective inhibitor of hematopoietic prostaglandin D synthase (HPGDS). ACS Medicinal Chemistry Letters, 2010, 1(2): 59-63.