产品
编 号：F030505
分子式：C18H25N5O
分子量：327.42
分子式：C18H25N5O
分子量：327.42
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CAS No: 1082954-71-9
产品详情
生物活性：
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model.
体内研究：
A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) isfound to reduce scratching induced by the histamine H4 agonist clobenpropit (HY-101198).A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (Fpo/iv=26%) with a half-life of 3.7 h and a Cmax of 0.30 μM at a Tmax of 1.5 h after dosing.Animal Model:Mice
Dosage:98.23 μg/kg , 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis)
Administration:Intraperitoneal injection
Result:Fpo/iv=26%, T1/2=3.7 hours, Cmax=0.30 μM, Tmax=1.5 hours
体外研究：
A-987306 has potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays.A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H4R over the humanH1, H2 , and H3 receptors in cell-based Ca2+-flux functional assay (FLIPR).A-987306 shows lower selectivity for H4R in the rat (only 4-fold selective for the rat H4R over the rat H3R) in FLIPR.
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model.
体内研究：
A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) isfound to reduce scratching induced by the histamine H4 agonist clobenpropit (HY-101198).A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (Fpo/iv=26%) with a half-life of 3.7 h and a Cmax of 0.30 μM at a Tmax of 1.5 h after dosing.Animal Model:Mice
Dosage:98.23 μg/kg , 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis)
Administration:Intraperitoneal injection
Result:Fpo/iv=26%, T1/2=3.7 hours, Cmax=0.30 μM, Tmax=1.5 hours
体外研究：
A-987306 has potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays.A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H4R over the humanH1, H2 , and H3 receptors in cell-based Ca2+-flux functional assay (FLIPR).A-987306 shows lower selectivity for H4R in the rat (only 4-fold selective for the rat H4R over the rat H3R) in FLIPR.
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