ITI-214

小分子

ITI-214

I654939-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor ( K i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K i s of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions In Vitro ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (K i =?33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:PDE1 58 pM (Ki) PDE1A 33 pM (Ki) PDE1B 380 pM (Ki) PDE1C 35 pM (Ki)

ITI-214 是一种强效、具有中枢神经系统活性、口服生物可用性的 PDE1 抑制剂（K i 为 58 pM），对其他 PDE 家族成员以及一系列酶、受体、转运体和离子通道具有极佳的选择性。ITI-214 可抑制重组全-len

1642303-38-5(DMSO)

C29H29FN7O5P

605.6 g/mol

CN1C(=O)C2=C(N(N=C2N3C1=NC4C3CCC4)CC5=CC=C(C=C5)C6=NC(=CC=C6)F)NC7=CC=CC=C7.OP(=O)(O)O