SR 202 |
カタログ番号GC11586
One-Click Copy Product Info
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SR 202 (SR-202) は強力で特異的な PPARγ です。拮抗薬。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 76541-72-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 140 μM for attenuation of troglitazone-induced peroxisome proliferator-activated receptor gamma (PPAR) transcriptional activity [1]
The phosphonophosphate SR-202 [(S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate] is a PPAR antagonist, which inhibits both TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1 and TZD-induced transcriptional activity of the receptor. PPAR is a nuclear receptor which regulates glucose metabolism and fatty acid storage.
In vitro: SR-202 is a specific antagonist of PPAR, which shows selectivity both among the PPAR family members and other nuclear receptors. SR-202 also Inhibits PPAR-dependent differentiation of adipocytes. In cell culture, SR-202 efficiently antagonizes hormone- and TZD induced adipocyte differentiation [1].
In vivo:. Decreasing PPAR activity by treatment with SR-202 leads to a reduction of both high fat diet-induced adipocyte hypertrophy and insulin resistance. Treatment with SR-202 also dramatically improves insulin sensitivity in the diabetic ob/ob mice [1]. When wild-type mice are fed a high-fat diet, the plasma levels of TNF-α are raised, and SR-202 treatment protects against this rise [2]..
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Rieusset J, Touri F, Michalik L, Escher P, Desvergne B, Niesor E, Wahli W. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity. Mol Endocrinol. 2002 Nov;16(11):2628-44.
[2] Doggrell S. Do peroxisome proliferation receptor-gamma antagonists have clinical potential as combined antiobesity and antidiabetic drugs Expert Opin Investig Drugs. 2003 Apr;12(4):713-6.
| Cas No. | 76541-72-5 | SDF | |
| Chemical Name | (S)-(4-chlorophenyl)(dimethoxyphosphoryl)methyl dimethyl phosphate | ||
| Canonical SMILES | ClC1=CC=C(C=C1)[C@@H](OP(OC)(OC)=O)P(OC)(OC)=O | ||
| Formula | C11H17ClO7P2 | M.Wt | 358.65 |
| 溶解度 | Water: 100 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7882 mL | 13.9412 mL | 27.8823 mL |
| 5 mM | 557.6 μL | 2.7882 mL | 5.5765 mL |
| 10 mM | 278.8 μL | 1.3941 mL | 2.7882 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)