LAS101057

A potent adenosine A2B receptor antagonist

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库存: 现货

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1mg

￥875.00

700.00

- +
5mg

￥1737.00

1390.00

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10mg

￥2937.00

2350.00

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20mg

￥5175.00

4140.00

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已选 0 种 0 瓶

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货号: ajce51984
CAS: 925676-48-8
别名:
分子式: C18H14FN5O
分子量: 335.34
纯度: >98%
溶解度: DMSO : ≥ 125 mg/mL (372.76 mM);Water : < 0.1 mg/mL (insoluble)
储存: 4°C, protect from light
库存: 现货

Background

LAS101057 is a potent adenosine A_2B receptor antagonist (K_i = 24 nM).¹ It is selective for A_2B over A_2A, A₁, and A₃ receptors, as well as a panel of 340 enzymes, receptors, channels, and transporters at 10 μM. LAS101057 inhibits cAMP signaling induced by 5’-N-ethylcarboxamidoadenosine in HEK293 cells expressing recombinant human A_2B receptors (IC₅₀ = 120 nM). It reduces NECA-induced release of IL-6 in human primary dermal fibroblasts. LAS101057 (10 mg/kg) prevents methacholine-induced airway hyperresponsiveness (AHR) and reduces bronchoalveolar lavage fluid (BALF) levels of IL-4 and IL-13 in an ovalbumin-sensitized mouse model of asthma.

1.Eastwood, P., Esteve, C., Gonzalez, J., et al.Discovery of LAS101057: A potent, selective, and orally efficacious A2B adenosine receptor antagonistMed. Chem. Lett.2(3)213-218(2011)