产品
编 号：F051654
分子式：C29H26FN7O
分子量：507.56
分子式：C29H26FN7O
分子量：507.56
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CAS No: 1160521-50-5
产品详情
生物活性：
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
体内研究：
ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg.Animal Model:Male Sprague-Dawley rats
Dosage:0.1-10 mg/kg
Administration:P.o.
Result:Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.
体外研究：
ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (Ki=?34 pM), r-hPDE1B (Ki=?380 pM), and r-hPDE1C (Ki=?37 pM) enzymes transiently expressed in HEK cells. The compound expressed >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki=?33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families.
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
体内研究：
ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg.Animal Model:Male Sprague-Dawley rats
Dosage:0.1-10 mg/kg
Administration:P.o.
Result:Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.
体外研究：
ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (Ki=?34 pM), r-hPDE1B (Ki=?380 pM), and r-hPDE1C (Ki=?37 pM) enzymes transiently expressed in HEK cells. The compound expressed >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki=?33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families.
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