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HPGDS inhibitor 1

Catalog No.
B1046
HPGDS inhibitor
Grouped product items
SizePriceStock Qty
5mg
$293.00
Ship with 10-15 days
10mg
$512.00
Ship with 10-15 days
50mg
$1,319.00
Ship with 10-15 days
100mg
$2,051.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt381.37
Cas No.1033836-12-2
FormulaC19H19F4N3O
SolubilitySoluble in DMSO
Chemical Name6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
SDFDownload SDF
Canonical SMILESC1CN(CCC1NC(=O)C2=CN=C(C=C2)C3=CC(=CC=C3)F)CC(F)(F)F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

HPGDS inhibitor 1