PF-00610355 ( PF-610355 )

产品货号. M16243 CAS No. 862541-45-5

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

PF-00610355
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

PF-00610355 (PF 610355) 是一种有效、选择性、长效的 β2-肾上腺素受体激动剂，EC50 为 0.26 nM。
产品描述

PF-00610355 (PF 610355) is a potent, selective, and long-acting β2-adrenoreceptor agonist with EC50 of 0.26 nM; displays 220-fold selectivity over β1; exhibits potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstructive pulmonary disease.Asthma Phase 2 Discontinued.
体外实验

——
体内实验

PF-610355 is a long-acting (once daily) inhaled β2-adrenoreceptor agonist. PF-610355 has low oral bioavailability due to poor absorption through the gut lumen and high first pass metabolism and warranted further progression. PF-610355 has a short half-life (Clint = 33 (μL/min)/mg) that suggested an unbound intrinsic clearance of >10000 (mL/min)/kg. PF-610355 exhibits an ideal pharmacokinetic profile for an inhaled agent.
同义词

PF-610355
通路

GPCR/G Protein
靶点

Adrenergic Receptor
受体

Adrenergic Receptor
研究领域

Inflammation/Immunology
适应症

Asthma

CAS Number

862541-45-5
分子量

617.76
分子式

C34H39N3O6S
纯度

>98% (HPLC)
溶解度

——
SMILES

O=C(NCC1=CC(C2=CC=C(O)C=C2)=CC=C1)CC3=CC=CC(CC(C)(NC[C@H](O)C4=CC=C(O)C(NS(=O)(C)=O)=C4)C)=C3
化学全称

N-((4'-hydroxy(1,1'-biphenyl)-3-yl)methyl)-3-(2-(((2R)-2-hydroxy-2-(4-hydroxy-3-((methylsulfonyl)amino)phenyl)ethyl)amino)-2-methylpropyl)-benzeneacetamide

1. Glossop PA, et al. J Med Chem. 2010 Sep 23;53(18):6640-52. 2. Diderichsen PM, et al. Br J Clin Pharmacol. 2013 Nov;76(5):752-62.

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