GPBAR-A |
| Catalog No.GC13880 |
agonist of bile acid receptor GPBAR1
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 877052-79-4
Sample solution is provided at 25 µL, 10mM.
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GPBAR-A is an agonist of bile acid receptor GPBAR1 [1].
The G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is a plasma membrane-bound receptor for bile acids. TGR5 is involved in gallstone formation and is expressed in the epithelium of human gallbladders [2].
GPBAR-A is an agonist of bile acid receptor GPBAR1. In GLUTag cells, GPBAR-A stimulated glucagon-like peptide (GLP-1) release. In primary colonic cultures, GPBAR-A increased GLP-1 release by 4.2-fold. In upper small intestinal cultures, GPBAR-A increased GLP-1 release by 2.6-fold. In GLUTag cells, GPBAR-A increased cAMP concentration by 57%. Also, GPBAR-A increased calcium in 56/149 cells and caused the mean response by 1.3-fold. In the presence of glucose, GPBAR-A increased calcium in 148/149 cells and caused the mean response by 2.6-fold. In the presence of diazoxide (the KATP channel opener, 340 μM) and 70 mM KCl, GPBAR-A also increased GLP-1 secretion. In colonic and small intestinal cultures, GPBAR-A increased the GLP-1 secretion by 2.4-fold and 1.5-fold. The GLP-1 secretion mediated by GPBAR-A was independent on KATP channel closure [1].
References:
[1]. Parker HE, Wallis K, le Roux CW, et al. Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br J Pharmacol, 2012, 165(2): 414-423.
[2]. Keitel V, Cupisti K, Ullmer C, et al. The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders. Hepatology, 2009, 50(3): 861-870.
| Cas No. | 877052-79-4 | SDF | |
| Formula | C23H15F7N2O2 | M.Wt | 484.37 |
| Solubility | <9.69mg/ml in ethanol; <48.44mg/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 | 2.0645 mL | 10.3227 mL | 20.6454 mL |
| 5 mM | 0.4129 mL | 2.0645 mL | 4.1291 mL |
| 10 mM | 0.2065 mL | 1.0323 mL | 2.0645 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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