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BETP

Catalog No. TQ0124   CAS 1371569-69-5

BETP is an agonist of GLP-1 receptor (EC50s: 0.66 and 0.755 μM for human and rat GLP-1 receptor).

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BETP Chemical Structure
BETP, CAS 1371569-69-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
2 mg In stock $ 57.00
5 mg In stock $ 85.00
10 mg In stock $ 142.00
25 mg In stock $ 279.00
50 mg In stock $ 498.00
100 mg In stock $ 725.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 97.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BETP is an agonist of GLP-1 receptor (EC50s: 0.66 and 0.755 μM for human and rat GLP-1 receptor).
Targets&IC50 GLP1:0.66 μM(Human), GLP1:0.755 μM(Rat)
In vitro BETP (Compound B) is inactive in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. BETP (1-10 μM) enhances insulin secretion in normal and diabetic human islets. In addition, BETP in combination with GLP-1 shows additive effects on increasing GLP-1 receptor signaling [1]. BETP increases the potency of oxyntomodulin by 10-fold (EC50: 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 [2].
In vivo 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 demonstrate higher plasma insulin levels in the SD rat hyperglycemic clamp model [1]. BETP (5 mg/kg) enhances oxyntomodulin-stimulated insulin secretion [2].
Animal Research IVGTT studies are performed. Male SD rats are group-housed three per cage in polycarbonate cages with filter tops. Rats are maintained on a 12:12 h light-dark cycle (lights on at 6:00 a.m.) at 21°C and receive diet and deionized water ad libitum. Rats were fasted overnight and anesthetized with 60 mg/kg pentobarbital for the duration of the experiment. For glucose and compounds (BETP, etc.) administration, a catheter with a diameter of 0.84 mm is inserted into the jugular vein. For rapid blood collection, a larger catheter with 1.02-mm diameter is inserted into the carotid artery. Blood is collected for glucose and insulin levels at times 0, 2, 4, 6, 10, and 20 min after intravenous administration of the BETP which is immediately followed by an intravenous glucose bolus of 0.5 g/kg. Plasma levels of glucose and insulin are determined [1].
Molecular Weight 406.42
Formula C20H17F3N2O2S
CAS No. 1371569-69-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 25 mg/mL (61.51 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Sloop KW, et al. Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. Diabetes. 2010 Dec;59(12):3099-107. 2. Willard FS, et al. Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin. Mol Pharmacol. 2012 Dec;82(6):1066-73.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Diabetic Compound Library Bioactive Compound Library Anti-Obesity Compound Library NO PAINS Compound Library Bioactive Compounds Library Max

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Keywords

BETP 1371569-69-5 GPCR/G Protein Glucagon Receptor inhibit GCGR Inhibitor inhibitor

 

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