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PW0464 Sale

(Synonyms: PW0464) 目录号 : GC63157

PW0464 是一种纳摩尔有效的完全 G 蛋白偏向配体,是一种非儿茶酚 D1R 激动剂,EC50 为 5.8 nM (Gs-cAMP)。

PW0464 Chemical Structure

Cas No.:1643462-93-4

规格 价格 库存 购买数量
5 mg
¥4,320.00
现货
10 mg
¥7,200.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 1643462-93-4 SDF
别名 PW0464
分子式 C19H17F2N3O4 分子量 389.35
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1 mg 5 mg 10 mg
1 mM 2.5684 mL 12.8419 mL 25.6838 mL
5 mM 0.5137 mL 2.5684 mL 5.1368 mL
10 mM 0.2568 mL 1.2842 mL 2.5684 mL
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Research Update

Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists

ACS Med Chem Lett 2019 Apr 5;10(5):792-799.PMID:31098001DOI:PMC6511950

Noncatechol heterocycles have recently been discovered as potent and selective G protein biased dopamine 1 receptor (D1R) agonists with superior pharmacokinetic properties. To determine the structure-activity relationships centered on G protein or β-arrestin signaling bias, systematic medicinal chemistry was employed around three aromatic pharmacophores of the lead compound 5 (PF2334), generating a series of new molecules that were evaluated at both D1R Gs-dependent cAMP signaling and β-arrestin recruitment in HEK293 cells. Here, we report the chemical synthesis, pharmacological evaluation, and molecular docking studies leading to the identification of two novel noncatechol D1R agonists that are a subnanomolar potent unbiased ligand 19 (PW0441) and a nanomolar potent complete G protein biased ligand 24 (PW0464), respectively. These novel D1R agonists provide important tools to study D1R activation and signaling bias in both health and disease.