1371569-69-5|BETP|CsnPharm

CAS No.: 1371569-69-5

BETP Catalog No. CSN22077

Synonyms: BETP

BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The glucagon-like peptide-1 receptor (GLP-1R) is one of the preeminent class B G-protein coupled receptor(GPCRs) as both its physiologic control of insulin secretion, and its ligand binding-receptor interactions using structural biology^[1]. BETP represents a novel small-molecule activator of GLP-1R, and exhibits glucose-dependent insulin secretion in rats following i.v. (but not oral) administration^[2]. Sustained degradation of BETP with small-molecule BET proteolysis-targeting chimera (PROTAC), ARV-825, resulted in marked downregulation of surface CXCR4 and CD44, key proteins in leukemia-microenvironment interaction, in AML cells. BETP degradation markedly decreased CD34+CD38-CD90-CD45RA+ leukemic stem cell population and alone or in combination with Cytarabine, prolonged survival in mouse model of human leukemia including AML-PDX^[3]. BETP increases the potency of oxyntomodulin by 10-fold (EC50 of 80 pM). GLP-1 does not change the potencies and efficacies of both oxyntomodulin and glucagon at the glucagon receptor. BETP (0-30 μM) increases the binding affinity of oxyntomodulin for the GLP-1 receptor. BETP (5 mg/kg) enhances oxyntomodulin-stimulated insulin secretion^[4]. BETP has insulinotropic effect in SD rats. BETP (10 mg/kg, jugular vein cannula) exhibits insulin secretagogue activity in the intravenous glucose tolerance test (IVGTT) model. BETP (10 mg/kg, i.v.)-treated rats need 20% higher glucose infusion rates and demonstrates higher plasma insulin levels in SD rat hyperglycemic clamp model^[5].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT01412424 Acromegaly Phase 3 Completed - -
NCT01412424 - - Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01412424	Acromegaly	Phase 3	Completed	-	-
NCT01412424	-	-	Completed	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4605 mL
- 12.3025 mL
- 24.6050 mL
- 5 mM
- 0.4921 mL
- 2.4605 mL
- 4.9210 mL
- 10 mM
- 0.2461 mL
- 1.2303 mL
- 2.4605 mL

技术信息

CAS号

1371569-69-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17F3N2O2S

运输

蓝冰

分子量

406.42

别名

BETP

溶解度

DMSO	95.0 mg/mL (233.7 mM) warming
Water	Insoluble

动物实验配方

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BETP Catalog No. CSN22077

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