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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-AVN-101
AVN-101

Chemical Structure : AVN-101

CAS No.: 1025725-91-0

AVN-101 (AVN101)

货号: PC-61504Not For Human Use, Lab Use Only.

AVN-101 is a higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AVN-101 is a higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM).
AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki = 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki = 0.41-3.6 nM) receptors.
AVN-101 demonstrates reasonable anxiolytic and anti-depressive activities in animal models of CNS diseases with low safety concerns.

物理化学性质&存储条件

分子量 304.437
分子式 C21H24N2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,8-dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole

参考文献

1. Ivachtchenko AV, et al. J Alzheimers Dis. 2016 May 25;53(2):583-620.

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