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首页-小分子抑制剂&激动剂-Immunology/Inflammation-PGE synthase-HQL-79
HQL-79

Chemical Structure : HQL-79

CAS No.: 162641-16-9

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HQL-79 (HQL79)

货号: PC-49639Not For Human Use, Lab Use Only.

HQL-79 (HQL79) is an orally selective inhibitor of human hematopoietic prostaglandin D synthase (H-PGDS), inhibits human H-PGDS competitively against the substrate PGH2 and non-competitively against GSH with Ki of 5 and 3 uM, respectively.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HQL-79 (HQL79) is an orally selective inhibitor of human hematopoietic prostaglandin D synthase (H-PGDS), inhibits human H-PGDS competitively against the substrate PGH2 and non-competitively against GSH with Ki of 5 and 3 uM, respectively.
HQL-79 binds to H-PGDS with an affinity that is 12-fold higher in the presence of GSH and Mg2+ (Kd, 0.8 uM) than in their absence.
HQL-79 selectively inhibited PGD2 production by H-PGDS-expressing human megakaryocytes and rat mastocytoma cells with an IC50 value of about 100 uM but only marginally affected the production of other prostanoids.
Orally administered HQL-79 (30 mg/kg body weight) inhibited antigen-induced production of PGD2, without affecting the production of PGE2 and PGF2alpha, and ameliorated airway inflammation in wild-type and human H-PGDS-overexpressing mice.

物理化学性质&存储条件

分子量 377.48
分子式 C22H27N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(Diphenylmethoxy)-1-[3-(2H-tetrazol-5-yl)propyl]piperidine

参考文献

1. Aritake K, et al. J Biol Chem. 2006 Jun 2;281(22):15277-86.

2. Tajima T, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):493-501.

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