3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Basic information
- Product Name:
- 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- Synonyms:
-
- HPGDS inhibitor 1
- 6-(3-Fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]-3-pyridinecarboxamide
- 3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- 6-(3-fluorophenyl)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)nicotinaMide
- HPGDS inhibitor 1, >=98%
- Prostaglandin D Synthase (hematopoietic-type) Inhibitor I
- CS-1438
- MDK36122
- CAS:
- 1033836-12-2
- MF:
- C19H19F4N3O
- MW:
- 381.37
- Product Categories:
-
- Inhibitors
- Mol File:
- 1033836-12-2.mol
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Chemical Properties
- Boiling point:
- 487.2±45.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO
- form
- crystalline solid
- pka
- 9.55±0.20(Predicted)
- color
- White to off-white
3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]- Usage And Synthesis
Uses
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX[1].
Biological Activity
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].
in vitro
HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC 50 , 0.5-2.3 nM).
in vivo
HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T 1/2 is 4.1 hours in rats.
Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of it blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of it in a time- and dose-dependent manner.
It (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma.
target
IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays)
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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