1. GPCR/G Protein
  2. Glucagon Receptor

BETP 

目录号: HY-103546 纯度: 99.28%
产品使用指南

BETP 是一种胰高血糖素样肽(GLP-1)受体激动剂,对人和大鼠 GLP-1 受体的 EC50 值分别为 0.66 μM 和 0.755 μM。

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BETP Chemical Structure

BETP Chemical Structure

CAS No. : 1371569-69-5

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥1210 In-stock
5 mg ¥1100 In-stock
10 mg ¥1700 In-stock
25 mg ¥3400 In-stock
50 mg ¥6100 In-stock
100 mg ¥9900 In-stock
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Description

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.

IC50 & Target

EC50: 0.66 μM (Human GLP-1 receptor), 0.755 μM (Rat GLP-1 receptor)[1]

In Vitro

BETP is a GLP-1 receptor agonist, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. 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 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[2].

In Vivo

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[1]. BETP (5 mg/kg) enhances oxyntomodulin-stimulated insulin secretion[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4605 mL 12.3025 mL 24.6051 mL
5 mM 0.4921 mL 2.4605 mL 4.9210 mL
10 mM 0.2461 mL 1.2303 mL 2.4605 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
The 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 are 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 time 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

406.42

Formula

C₂₀H₁₇F₃N₂O₂S

CAS No.

1371569-69-5

SMILES

FC(C1=CC(C2=CC=CC(OCC3=CC=CC=C3)=C2)=NC(S(CC)=O)=N1)(F)F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
BETP
目录号:
HY-103546
需求量:

BETP

Cat. No.: HY-103546