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HPGDS inhibitor 2 (GSK-2894631A) is a potent, selective hematopoietic prostaglandin D synthase (h-pgds) inhibitor, IC50 = 9.9 nm.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $88 | In Stock | |
5 mg | $213 | In Stock | |
10 mg | $347 | In Stock | |
25 mg | $619 | In Stock | |
50 mg | $793 | In Stock | |
100 mg | $1,060 | In Stock | |
500 mg | $2,120 | In Stock | |
1 mL x 10 mM (in DMSO) | $235 | In Stock |
Description | HPGDS inhibitor 2 (GSK-2894631A) is a potent, selective hematopoietic prostaglandin D synthase (h-pgds) inhibitor, IC50 = 9.9 nm. |
Targets&IC50 | HPGDS:9.9 nM (IC50) |
In vitro | GSK2894631A(IC50 = 9.9 nM, LE = 0.42) is a potent, competitive, and reversible inhibitor of H-PGDS. GSK2894631A exhibited good H-PGDS cellular activity (RBL IC50 = 160 nM) in a rat basophilic leukemia (RBL) cell PGD2 production assay. |
In vivo | GSK2894631A had a low i.v. clearance (Cl = 5.6 mL/min/kg), moderate i.v. steady state volume of distribution (VSS = 1.7 l/kg), long i.v. terminal half-life (t1/2 = 3.8 hr), and good oral exposure (p.o. DNAUC = 1800 ng/hr/mL, F = 61%) in mice. It attenuated PGD2 production in an acute in vivo murine mast cell degranulation model (ED50 = 0.032 mg/kg, EC50 = 21 nM) of inflammation. Unfortunately, at higher doses (≥10 mg/kg) in a chronic eccentric muscle damage model (vide infra Fig. 6) in mice, 1a-treated animals exhibited seizure-like activity at day four of dosing. |
Alias | GSK-2894631A |
Molecular Weight | 378.41 |
Formula | C20H24F2N2O3 |
Cas No. | 2101626-26-8 |
Smiles | CC(C)(O)[C@H]1CC[C@@H](CC1)NC(=O)c1cnc2cc(OC(F)F)ccc2c1 |
Relative Density. | 1.27 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 130 mg/mL (343.54 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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