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Mifobate (SR-202) is a potent PPARγ antagonist with antiobesity, antidiabetic and antiatherosclerotic effects. It selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM) and does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR).
| ln Vitro |
After six days, BRL 49653 and hormone-induced adipocyte clearance in 3T3-L1 cells are strongly inhibited by mifobate (100-400 μM; 24 hours rest) in a dose-dependent manner [1]. The agonist-coupled response of TZD-stimulated coactivator dormant coactivator-like 1 (SRC-1) is inhibited by mifobate (SR-202). Mifobate inhibits the release of fat when thiazolidinediones or a combination of insulin, dexamethasone, and 3-cell isotetra-1-methylxanthine (IBMX) are used [1].
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| ln Vivo |
In ob/ob mice, mifobate (400 mg/kg; given for 20 days) enhances insulin resistance[1].
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| Animal Protocol |
Animal/Disease Models: Eightweeks old male ob/ob mice[1]
Doses: 400 mg/kg Route of Administration: Feed (food mixture Maintenance for 20 days) Experimental Results: Prevented increase in glucose concentration over time. |
| References | |
| Additional Infomation |
Phosphoric acid [(4-chlorophenyl)-dimethoxyphosphorylmethyl] dimethyl ester is a trialkyl phosphate.
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| Molecular Formula |
C11H17CLO7P2
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|---|---|
| Molecular Weight |
358.6475
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| Exact Mass |
358.014
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| CAS # |
76541-72-5
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| PubChem CID |
60910
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| Appearance |
White to off-white solid powder
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| Density |
1.355g/cm3
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| Boiling Point |
436.6ºC at 760 mmHg
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| Flash Point |
350.8ºC
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| Index of Refraction |
1.494
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| LogP |
4.242
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
21
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| Complexity |
395
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VQHUQHAPWMNBLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H17ClO7P2/c1-15-20(13,16-2)11(19-21(14,17-3)18-4)9-5-7-10(12)8-6-9/h5-8,11H,1-4H3
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| Chemical Name |
Phosphoric acid, (4-chlorophenyl)(dimethoxyphosphinyl)methyl dimethyl ester
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| Synonyms |
SR 202 SR-202Mifobate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~278.82 mM)
H2O : ~35.87 mg/mL (~100.01 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 50 mg/mL (139.41 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7882 mL | 13.9412 mL | 27.8823 mL | |
| 5 mM | 0.5576 mL | 2.7882 mL | 5.5765 mL | |
| 10 mM | 0.2788 mL | 1.3941 mL | 2.7882 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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