HPGDS inhibitor 3,2255311-93-2

价格询价

品牌MedChemExpress(MCE)
产地美国
货号HY-146662
更新日期2025年12月05日

MedChemExpress LLC

品牌商

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HPGDS inhibitor 3

CAS No. : 2255311-93-2

MCE 国际站：HPGDS inhibitor 3

产品活性：HPGDS inhibitor 3 是一种具有口服活性且高效的外周限制性造血前列腺素 D 合成酶 (H-PGDS) 抑制剂，IC₅₀ 为 9.4 nM，EC₅₀ 为 42 nM。HPGDS inhibitor 3 具有良好的选择性，在小鼠、大鼠和犬体内的药动学参数良好，且无中枢神经系统毒性。HPGDS inhibitor 3 具有抗炎活性。

研究领域：Immunology/Inflammation

作用靶点：PGE synthase

In Vivo: HPGDS inhibitor 3 (compound 1y) (1-3 mg/kg; PO and IV; single) has a lower IV clearance, similar steady state volume of distribution, longer terminal half-life, and high oral bioavailability, as well as very low brain exposures in mouse, rat and dog.
HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) attenuates PGD₂ release to baseline levels in a dose-dependent manner; also inhibits LPS-induced PGD₂ increase in plasma and skeletal muscle in a dose-dependent manner.
HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) .
HPGDS inhibitor 3 (1, 3, and 10 mg/kg; PO; q.d., for 16 days) significantly enhances functional recovery of injured limbs, and hastens the time to full functional recovery of injured limb muscles.
HPGDS inhibitor 3 (10, 30 and 100 mg/kg; PO; once daily, for 7 days or 4 days) exhibits well tolerated at 30 mg/kg/day in rat but not tolerated at 100 mg/kg/day; shows well tolerated at 30 mg/kg/day in dogs but not tolerated at 75 mg/kg/day.
Pharmacokinetic Parameters of HPGDS inhibitor 3 in mice, rats and dogs.

	Mouse IV, 1 mg/kg PO, 3 mg/kg	Rat IV, 0.4 mg/kg PO, 2.4 mg/kg	Dog IV, 0.5 mg/kg PO, 1 mg/kg
T_1/2 (h)	2.9	5.1	6.2
CL (mL/min/kg)	9.0	4.5	1.9
V_ss (L/kg)	1.6	1.6	1.0
F (%)	71	100	92
Brain:blood ratio	0.06