TGR5 Receptor Agonist (Synonyms: CCDC) |
| カタログ番号GC16363 |
TGR5 受容体アゴニスト (CCDC) は、強力なタケダ G タンパク質共役型受容体 5 (TGR5; GPCR19) アゴニストであり、U2-OS 細胞およびメラノフォア細胞においてそれぞれ 6.8 および 7.5 の pEC50 で効力の改善を示しています。
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Cas No.: 1197300-24-5
Sample solution is provided at 25 µL, 10mM.
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TGR5 Receptor Agonist is a potent and selective agonist of TGR5 G-protein receptor with a pEC50 value of 6.8 in the U2-OS cell assay [1].
TGR5 Receptor Agonist has been shown the activated potency of TGR5 receptor with pEC50 values of 6.8 and 7.5 in the U2-OS cells and melanophire cells assay, respectively. In addition, TGR5 Receptor Agonist has been found to be fully specific for the human TGR5 receptor in the U2-OS and melanophore cell lines and also selective against other 7TM receptors. Besides, TGR5 Receptor Agonist has been reported to have physicochemical properties and no measurable activity against the common cytochrome P450 (CYP450) isoforms or hERG dofetilide binding with a pIC50 value of <4.3.
References:
[1] Evans KA1, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem. 2009 Dec 24;52(24):7962-5.
| Cas No. | 1197300-24-5 | SDF | |
| 同義語 | CCDC | ||
| Chemical Name | 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethylisoxazole-4-carboxamide | ||
| Canonical SMILES | CC1=C(C(N(C2=CC=C(Cl)C=C2)C)=O)C(C3=CC=CC=C3Cl)=NO1 | ||
| Formula | C18H14Cl2N2O2 | M.Wt | 361.22 |
| 溶解度 | DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 30 mg/ml | 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. |
||
| 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 | 2.7684 mL | 13.842 mL | 27.684 mL |
| 5 mM | 0.5537 mL | 2.7684 mL | 5.5368 mL |
| 10 mM | 0.2768 mL | 1.3842 mL | 2.7684 mL |
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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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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