HPGDS inhibitor 1 (Synonyms: H-PGDS Inhibitor I) |
| Catalog No.GC14633 |
El inhibidor 1 de HPGDS es un inhibidor potente, selectivo y oralmente activo de la sintasa hematopoyética D de la prostaglandina (HPGDS) con una IC50 de 0,6 nM y 32 nM en ensayos enzimÁticos y celulares, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
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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