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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-LAS101057
LAS101057

Chemical Structure : LAS101057

CAS No.: 925676-48-8

LAS101057 (LAS 101057)

货号: PC-20638Not For Human Use, Lab Use Only.

LAS101057 (LAS 101057) is a potent, selective, and orally efficacious A2B adenosine receptor antagonist with Ki of 24 nM (human A2B).

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5 mg ¥1380 In stock
10 mg ¥2180 In stock
25 mg ¥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LAS101057 (LAS 101057) is a potent, selective, and orally efficacious A2B adenosine receptor antagonist with Ki of 24 nM (human A2B).
LAS101057 is >400-fold selective in a diverse panel of more than 340 enzymes, receptors, channels, and transporters.
LAS101057 effects a concentration-dependent down-regulation of IL-6 production with a potency (67%) at 100 nM on NECA-induced IL-6 release in human primary dermal fibroblasts.
LAS101057 (10 mg/kg) is active in an ovalbumin (OVA)-sensitized mouse model after oral administration, reducing airway hyperresponsiveness to methacholine, Th2 cytokine production, and OVA-specific IgE levels.

物理化学性质&存储条件

分子量 335.34
分子式 C18H14FN5O
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-(5-(3-fluoropyridin-4-yl)-6-(pyridin-3-yl)pyrazin-2-yl)cyclopropanecarboxamide

参考文献

1. Paul Eastwood, et al. ACS Med Chem Lett. 2011 Mar 10; 2(3): 213–218.

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