tBPC |
Catalog No.GC50440
One-Click Copy Product Info
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tBPC is a selective positive allosteric modulator of the Y4 receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1942-71-8
Sample solution is provided at 25 µL, 10mM.
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tBPC is a selective positive allosteric modulator of the Y4 receptor. tBPC enhances the activation of the Y4 receptor in G protein signaling and arrestin3 recruitment, thereby potentiating the Y4R responses to pancreatic polypeptide, neuropeptide Y, and peptide YY, while maintaining specificity by selectively modulating the Y4 receptor without affecting the Y1, Y2, or Y5 receptors[1].
In vitro, treatment of COS7 cells and HEK293 cells with tBPC (5.1μM-30μM) for 30 minutes enhances the activation effect of Polypeptide and other peptides (NPY, PYY) on Y4R, as well as the rate of arrestin3 recruitment[1].
References:
[1] Schubert M, Stichel J, Du Y, et al. Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator. J Med Chem. 2017 Sep 14;60(17):7605-7612.
| Cell experiment [1]: | |
Cell lines | COS7 cells stably transfected with human Y4R-eYFP and chimeric △6Gαqi4-myr G-protein; HEK293 cells transiently expressing Y4R-Rluc8 and venus-arrestin3 fusion proteins; Mouse descending colon mucosa endogenously expressing Y4R. |
Preparation Method | For Ca²⁺ flux assays, transfected COS7 cells were seeded in plates and loaded with Fluo2-AM dye. For arrestin3 recruitment BRET assays, transfected HEK293 cells were seeded in plates and incubated with coelenterazine H. Cells tBPC (5.1μM-30μM) for 30 minutes. |
Reaction Conditions | 5.1-30µM; incubation for 30 min. |
Applications | tBPC potentiated Y4R activation by its native ligand Pancreatic Polypeptide (PP) and other peptide ligands (NPY, PYY) in both G-protein-mediated Ca²⁺ signaling and arrestin3 recruitment pathways. tBPC acted as a positive allosteric modulator (PAM) and displayed weak agonistic activity in overexpressing systems. |
References: | |
| Cas No. | 1942-71-8 | SDF | |
| Chemical Name | 2-[4-(1,1-Dimethylethyl)phenoxy]cyclohexanol | ||
| Canonical SMILES | CC(C)(C1=CC=C(C=C1)OC2CCCCC2O)C | ||
| Formula | C16H24O2 | M.Wt | 248.36 |
| Solubility | 24.84mg/ml in DMSO, 24.84mg/ml in Ethanol | Storage | Store at 4℃ |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0264 mL | 20.1321 mL | 40.2641 mL |
| 5 mM | 805.3 μL | 4.0264 mL | 8.0528 mL |
| 10 mM | 402.6 μL | 2.0132 mL | 4.0264 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)