BR102375 |
| Catalog No.GC35547 |
BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2366255-59-4
Sample solution is provided at 25 µL, 10mM.
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BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%[1].
BR102375 (Compound 18) (10 μM) increases gene expression levels relevant to PPARγ activation and enhances glucose uptake under insulin stimulation[1].BR102375 (Compound 18) (10 nM, 100 nM, 1 μM; 6 days, 14 days) shows a concentration-dependent, insulin-sensitive effects on adipogenesis[1]. RT-PCR[1] Cell Line: 3T3-L1 mouse preadipocyte cells
BR102375 (Compound 18) has decent efficacy on mouse diabetes model[1].BR102375 reveals significant suppressive effect on random blood glucose increase(75 mpk, p.o., bid), shows decent effect on insulin resistance on Oral glucose tolerance test (OGTT) and discloses similar findings in body weight gain almost identical to Pioglitazone[1].
[1]. Choung W, et al. Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2019 Jun 19. pii: S0960-894X(19)30407-X.
| Cas No. | 2366255-59-4 | SDF | |
| Canonical SMILES | CCCCC(N1CC2=CC=C(C3=C(C4=NOC(N4)=O)C=CC=C3)C=C2)=NC(C)=C(CC5=NC(C(C)(C)C)=NO5)C1=O | ||
| Formula | C31H34N6O4 | M.Wt | 554.64 |
| Solubility | Soluble 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 | 1.803 mL | 9.0149 mL | 18.0297 mL |
| 5 mM | 0.3606 mL | 1.803 mL | 3.6059 mL |
| 10 mM | 0.1803 mL | 0.9015 mL | 1.803 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 12 reference(s) in Google Scholar.)
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