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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-BETP
BETP

Chemical Structure : BETP

CAS No.: 1371569-69-5

BETP

货号: PC-23495Not For Human Use, Lab Use Only.

BETP is a potent, allosteric activator/agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively, also inhibits importin α1 import and importin β1 dependent cargo import with EC50 of μM uM in phenotypic importin α1 translocation assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BETP is a potent, allosteric activator/agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively, also inhibits importin α1 import and importin β1 dependent cargo import with EC50 of μM uM in phenotypic importin α1 translocation assays.
BETP increases oxyntomodulin binding affinity for the GLP-1 receptor and enhances oxyntomodulin-mediated GLP-1 receptor signaling as measured by activation of the α subunit of heterotrimeric G protein and cAMP accumulation.
BETP exhibits glucose-dependent insulin secretion in rats following i.v. (but not oral) administration.
BETP is a positive allosteric modulator at the glucagon-like peptide-1 receptor (GLP-1R), covalently modifies cysteines 347 and 438 in GLP-1R.

物理化学性质&存储条件

分子量 406.42
分子式 C20H17F3N2O2S
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

4-(3-(Benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine

参考文献

1. Sloop KW, et al. Diabetes. 2010 Dec;59(12):3099-107.

2. Willard FS, et al. Mol Pharmacol. 2012 Dec;82(6):1066-73.

3. Vercruysse T, et al. Commun Biol. 2024 Nov 23;7(1):1560.

4. Nolte WM, et al. Nat Chem Biol. 2014 Aug;10(8):629-31.

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