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编 号：F612177
分子式：C21H18ClFNNaO4S
分子量：457.88
分子式：C21H18ClFNNaO4S
分子量：457.88
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CAS No: 572874-50-1
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生物活性：
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.
体内研究：
Laropiprant sodium (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles.Pharmacokinetic Analysis in Male Sprague-Dawley ratsRouteDose (mg/kg)AUC0-∞ (μM·hr)Clp (mL/min/kg)Vdss (L/kg)T1/2 (hr)
PO122.71.90.77.4
PO596.02.10.97.6
RouteDose (mg/kg)AUC0-∞ (μM·hr)Cmax (μM)Tmax (hr)F(%)
IV552.615.61.2/
体外研究：
Laropiprant sodium (0.01-1000 μM; 10 mins; HEK293 cells) is an Inverse Agonist of DP1 cAMP Signaling and reduces DP1 cAMP signaling below basal levels.Laropiprant sodium (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression.
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.
体内研究：
Laropiprant sodium (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles.Pharmacokinetic Analysis in Male Sprague-Dawley ratsRouteDose (mg/kg)AUC0-∞ (μM·hr)Clp (mL/min/kg)Vdss (L/kg)T1/2 (hr)
PO122.71.90.77.4
PO596.02.10.97.6
RouteDose (mg/kg)AUC0-∞ (μM·hr)Cmax (μM)Tmax (hr)F(%)
IV552.615.61.2/
体外研究：
Laropiprant sodium (0.01-1000 μM; 10 mins; HEK293 cells) is an Inverse Agonist of DP1 cAMP Signaling and reduces DP1 cAMP signaling below basal levels.Laropiprant sodium (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression.
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