HPGDS inhibitor 1 (Synonyms: H-PGDS Inhibitor I) |
| カタログ番号GC14633 |
HPGDS インヒビター 1 は、酵素アッセイと細胞アッセイでそれぞれ 0.6 nM と 32 nM の IC50 を持つ強力で選択的な経口活性造血プロスタグランジン D シンターゼ (HPGDS) 阻害剤です。
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Cas No.: 1033836-12-2
Sample solution is provided at 25 µL, 10mM.
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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.
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