PW0464 是具有纳摩尔活性的全 G 蛋白配体,是 D1R 的激动剂,其EC50 值为 5.8 nM (Gs-cAMP)。
货号:ajcx35128
CAS:1643462-93-4
分子式:C19H17F2N3O4
分子量:389.35
溶解度:N/A
纯度:98%
存储:Store at -20°C
库存:
现货
Background:
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1].
PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1].PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2].
[1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists. ACS Med Chem Lett
[2]. David R Sibley, et al. Novel Cryo-EM structures of the D1 dopamine receptor unlock its therapeutic potential. Signal Transduct Target Ther. 2021 May 22;6(1):205.