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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-BnOCPA
BnOCPA

Chemical Structure : BnOCPA

CAS No.: 872693-38-4

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BnOCPA (Benzyloxy-cyclopentyladenosine)

货号: PC-49105Not For Human Use, Lab Use Only.

BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.

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纯度 & COA & 质检文件 纯度: 99.9% (HPLC) Select Batch:

生物&药学活性

BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.
BnOCPA displays 8000- and >150-fold greater efficacy at rat A1Rs (rA1Rs) than at rat A2ARs (rA2ARs) and A3Rs (rA3Rs), respectively.
BnOCPA exquisitely discriminates between native pre- and postsynaptic A1Rs in the intact mammalian CNS.
BnOCPA potently inhibited excitatory synaptic transmission in rat hippocampal slices with IC50 of 65 nM.
BnOCPA demonstrates unique Gα signalling in the selective activation of Gob, selectively induces canonical activation states at A1R:Gob, but non-productive metastable states at other Gαi/o subunits.
BnOCPA (IP; 10 µg/kg) or intravenously (IV; 10 or 25 µg/kg)) is a potent analgesic without causing sedation or motor impairment.

物理化学性质&存储条件

分子量 441.488
分子式 C22H27N5O5
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

(2R,3R,4S,5R)-2-(6-(((1R,2R)-2-(benzyloxy)cyclopentyl)amino)-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol

参考文献

1. Mark J Wall, et al. Nat Commun. 2022 Jul 18;13(1):4150.

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