Buloxibutid

Buloxibutid (AT2 receptor agonist C21) 是一种新型且具有选择性小分子 angiotensin II AT2 receptor (血管紧张素 II AT2 受体)激动剂,对 AT2 受体和 AT1 受体的 Ki 值分别为 0.4 nM 和 10 μM。

CAS号

477775-14-7

分子式

C15H12FIN2O3

主要靶点

RAAS

仅限科研使用

Cat No : CM02709

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Synonyms

AT2 receptor agonist C21



产品信息

Buloxibutid is a novel and selective small molecule angiotensin II AT2 receptor agonist with Ki values of 0.4 nM and 10 μM for AT2 and AT1 receptors, respectively.

CAS号 477775-14-7
分子式 C15H12FIN2O3
主要靶点 RAAS
主要通路 内分泌与激素
分子量 414.17
纯度 97.68%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 AT2 receptor agonist C21

靶点活性

AT2:0.4 nM(ki)|AT1:>10 μM(ki)

体内活性

Buloxibutid, with a bioavailability of 20-30% after oral administration and a half-life estimated to 4 h in rats. Which induces the outgrowth of neurite cells, stimulates p42/p44mapk, and enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats. And it lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats.[1]

溶解度

DMSO:22.5 mg/mL (47.31 mM)

参考文献

1.Wan Y, et al. Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. J Med Chem. 2004 Nov 18;47(24):5995-6008.
2.Schwengel K, et al. Angiotensin AT2-receptor stimulation improves survival and neurological outcome after experimental stroke in mice. J Mol Med (Berl). 2016;94(8):957-966.
3.Fatima N, et al. Angiotensin AT2 Receptor is Anti-inflammatory and Reno-Protective in Lipopolysaccharide Mice Model: Role of IL-10. Front Pharmacol. 2021;12:600163.

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