SB756050 |
Catalog No.GC31370
One-Click Copy Product Info
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A TGR5 agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 447410-57-3
Sample solution is provided at 25 µL, 10mM.
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SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D)[1].
SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 ? sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different[1].
[1]. Hodge RJ, et al. Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes. Clin Pharmacol Drug Dev. 2013 Jul;2(3):213-22.
| Cas No. | 447410-57-3 | SDF | |
| Canonical SMILES | O=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O | ||
| Formula | C21H28N2O8S2 | M.Wt | 500.59 |
| Solubility | DMSO : ≥ 150 mg/mL (299.65 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9976 mL | 9.9882 mL | 19.9764 mL |
| 5 mM | 399.5 μL | 1.9976 mL | 3.9953 mL |
| 10 mM | 199.8 μL | 998.8 μL | 1.9976 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 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)