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首页-小分子抑制剂&激动剂-GPCR-Adrenergic Receptor-CCF219B
CCF219B

Chemical Structure : CCF219B

CAS No.: 2521695-94-1

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CCF219B (Compound 3, Cmpd-3)

货号: PC-24568Not For Human Use, Lab Use Only.

CCF219B (Compound 3, Cmpd-3) is a potent, selective positive allosteric modulator of the α1A-adrenergic receptor (α1A-AR) with an affinity of 30 ​nM, 10-50-fold selectivity against the α1B- and α1D-AR subtypes.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CCF219B (Compound 3, Cmpd-3) is a potent, selective positive allosteric modulator of the α1A-adrenergic receptor (α1A-AR) with an affinity of 30 ​nM, 10-50-fold selectivity against the α1B- and α1D-AR subtypes.
Cmpd-3 PAM activity is receptor, ligand, and signal-biased; potentiation of NE-mediated but not Epi-mediated cAMP.
Cmpd-3 is not an agonist and is a pure PAM.
Cmpd-3 potentiates the phosphorylation of p-CREB, Cmpd-3 increases NE-mediated phosphorylation of CREB in the presence of α2-and β-AR blockers.
Cmpd-3 can potentiate the NE-mediated cAMP response in transfected Rat-1 fibroblasts.

物理化学性质&存储条件

分子量 339.45
分子式 C16H25N3O3S
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

N-(3-((4,5-dihydro-1H-imidazol-2-yl)methoxy)-2-isobutylphenyl)-N-methylmethanesulfonamide

参考文献

1. Robert S Papay, et al. Curr Res Pharmacol Drug Discov. 2022 Dec 2:4:100142.

2. Robert S Papay, et al. Pharmaceuticals (Basel). 2025 Mar 27;18(4):476.

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