PW0464 (Synonyms: PW0464) |
| カタログ番号GC63157 |
ナノモルの強力な完全 G タンパク質バイアス型リガンドである PW0464 は、非カテコール D1R アゴニストであり、EC50 は 5.8 nM (Gs-cAMP) です。
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Cas No.: 1643462-93-4
Sample solution is provided at 25 µL, 10mM.
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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.
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