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首页-小分子抑制剂&激动剂-GPCR-Angiotensin Receptor-Buloxibutid
Buloxibutid

Chemical Structure : Buloxibutid

CAS No.: 477775-14-7

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Buloxibutid (C21)

货号: PC-25932Not For Human Use, Lab Use Only.

Buloxibutid (C21) is an orally available, selective, high-affinity angiotensin II type 2 receptor (AT2R) agonist with Ki of 0.4 nM, >10,000-fold selective over AT1R.

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10 mg ￥1180 In stock
25 mg ￥1980 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

Buloxibutid (C21) is an orally available, selective, high-affinity angiotensin II type 2 receptor (AT2R) agonist with Ki of 0.4 nM, >10,000-fold selective over AT1R.
Buloxibutid induces outgrowth of neurite cells, stimulates p42/p44(mapk), enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats.
Buloxibutid exerts a similar biological response as the endogenous peptide angiotensin II after selective activation of the AT(2) receptor.
Buloxibutid reduced vascular remodeling (reduced endothelial proliferation and thickening of the vascular wall) in vesselsof rat Sugen-hypoxia PH model.
Buloxibutid (C21) significantly inhibited AML progression and enhanced the efficacy of chemotherapy, particularly in relapsed AML models.

物理化学性质&存储条件

分子量 475.62
分子式 C23H29N3O4S2
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

Butyl (3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophen-2-yl)sulfonylcarbamate

参考文献

1. Tornling G, et al. Int J Mol Sci. 2023 Apr 19;24(8):7478.

2. Steckelings UM, et al. Pharmacol Rev. 2022 Oct;74(4):1051-1135.

3. Yiqian Wan, et al. J Med Chem. 2004 Nov 18;47(24):5995-6008.

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