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ITI-214 free base
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ITI-214 free base图片
CAS NO:1160521-50-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
ITI-214 free base 是一种有效的中枢神经系统活性抑制剂,具有口服生物活性的PDE1抑制剂 (Kiof 58 pM),对其他PDE家族成员和一系列酶、受体、转运体和离子通道具有良好的选择性。ITI-214 free base 分别以 33 pM、380 pM和 35 pM 的 Ki抑制重组人 PDE1A、PDE1B 和 PDE1C。ITI-214 free base 在各种运动和认知功能的动物模型中显示出有效性。
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]

PDE1

58 pM (Ki)

PDE1A

33 pM (Ki)

PDE1B

380 pM (Ki)

PDE1C

35 pM (Ki)

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].

Animal Model:Male Sprague-Dawley rats[1]
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.
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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month