BETP |
| Catalog No.GC16232 |
BETP는 인간 및 쥐 GLP-1 수용체에 대해 각각 0.66 및 0.755μM의 EC50을 갖는 글루카곤 유사 펩티드-1(GLP-1) 수용체의 작용제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1371569-69-5
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
References:
[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.
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 1371569-69-5 | SDF | |
| Chemical Name | 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine | ||
| Canonical SMILES | FC(F)(C1=CC(C2=CC=CC(OCC3=CC=CC=C3)=C2)=NC(S(CC)=O)=N1)F | ||
| Formula | C20H17F3N2O2S | M.Wt | 406.42 |
| Solubility | <20.32mg/ml in ethanol; <40.64mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 | 4.921 mL |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4605 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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