CAS NO: | 1160521-50-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | ITI-214 free base is a potent, CNS-active, orally bioavailablePDE1inhibitor (Kiof 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[1][2]. | ||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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[2]. | ||||||||||||
体内研究 (In Vivo) | ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg[1].
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Clinical Trial | |||||||||||||
分子量 | 507.56 | ||||||||||||
性状 | Solid | ||||||||||||
Formula | C29H26FN7O | ||||||||||||
CAS 号 | 1160521-50-5 | ||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||
储存方式 |
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