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TC-N 22A
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。
TC-N 22A图片
CAS NO:1314140-00-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TC-N 22A 是一种强效的、选择性的、口服活性的、可以通透血脑的mGlu4正向别构调节剂 (PAM),在表达人 mGlu4的 BHK 细胞中EC50为 9 nM。TC-N 22A 在激动和正向别构模型中,对 mGlu 1、2、3、5 和 7 受体的活性很小 (EC50>10 μM)。TC-N 22A 可以用于中枢神经系统疾病研究的潜力。
生物活性

TC-N 22A is a potent, selective, orally active and brain-permeablemGlu4PAM with anEC50of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo[1].

IC50& Target

EC50: 9 nM (mGlu4receptor)
EC50: >10 μM (mGlu 1, 2, 3, 5, and 7 receptors)[1]

体外研究
(In Vitro)

TC-N 22A is selected for mGlu4and has an EC50of 9 nM in human mGlu4-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC50>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC50>10 μM) and shows low potential for hERG channel inhibition[1].

体内研究
(In Vivo)

TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats[1].

分子量

283.35

Formula

C14H13N5S

CAS 号

1314140-00-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vivo:
  • 1.

    TC-N 22A is suspended in 20% aqueous hydroxypropyl β-cyclodextrin[1].