产品
编 号：F117459
分子式：C14H13N5S
分子量：283.35
分子式：C14H13N5S
分子量：283.35
产品类型
规格
价格
是否有货
结构图
CAS No: 1314140-00-5
产品详情
生物活性：
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 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.
体内研究：
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.
体外研究：
TC-N 22A is selected for mGlu4 and has an EC50 of 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.
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 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.
体内研究：
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.
体外研究：
TC-N 22A is selected for mGlu4 and has an EC50 of 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备