| HPGDS inhibitor 1HPGDS inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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| Cas No. | 1033836-12-2 | SDF | Download SDF |
| Chemical Name | 6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide | ||
| Canonical SMILES | C1CN(CCC1NC(=O)C2=CN=C(C=C2)C3=CC(=CC=C3)F)CC(F)(F)F | ||
| Formula | C19H19F4N3O | M.Wt | 381.37 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
