| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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MA-0204 is a highly potent and selective PPARd modulator (PPARδ EC50 = 0.4 nM; PPARalpha, EC50 == 6,660 nM) that upregulates the expression of FAO genes in human renal proximal tubule cells, resulting in increased mitochondrial fatty acid oxidation. MA-0204 improves renal function, reduces proximal tubular damage, increases mitochondrial gene expression, and attenuates the increases of plasma and urine biomarkers of AKI in normal rats undergoing IR-AKI. DMD patients may benefit from MA-0204 as a treatment.
| Targets |
PPARδ (EC50 = 0.4 nM); PPARδ (EC50 = 7.9 nM); PPARδ (EC50 = 10 nM)
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|---|---|
| ln Vitro |
MA-0204 exhibits a selectivity of >10,000 times for PPARδ activation relative to PPARα and PPARγ receptors. MA-0204 has good permeability, minimal efflux potential, and high protein binding to mouse plasma.[1].
In mice with DMD, MA-0204 (1.2–12 nM) enhances fatty acid oxidation in the muscle myoblasts[1]. In muscle myoblasts from DMD patients, MA-0204 (0.04–40 nM) activates target gene expression[1]. |
| ln Vivo |
In the muscle, PPARδ (30, 100 mg/kg) increases target gene transcription[1].
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| References |
| Molecular Formula |
C25H27F3N2O4
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|---|---|
| Molecular Weight |
476.488097429276
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| Exact Mass |
476.192
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| Elemental Analysis |
C, 63.02; H, 5.71; F, 11.96; N, 5.88; O, 13.43
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| CAS # |
2095128-17-7
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| Related CAS # |
2095128-30-4;2095128-17-7 (free acid);
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| PubChem CID |
126752361
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| Appearance |
White to off-white solid powder
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| LogP |
5.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
34
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| Complexity |
628
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CN=C(N1CC2=CC=CC=C2OCCC[C@@H](C)CC(=O)O)C3=CC=C(C=C3)OC(F)(F)F
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| InChi Key |
GYNMVDMBFKGCCR-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C25H27F3N2O4/c1-17(14-23(31)32)6-5-13-33-22-8-4-3-7-20(22)16-30-18(2)15-29-24(30)19-9-11-21(12-10-19)34-25(26,27)28/h3-4,7-12,15,17H,5-6,13-14,16H2,1-2H3,(H,31,32)/t17-/m1/s1
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| Chemical Name |
(3R)-3-methyl-6-[2-[[5-methyl-2-[4-(trifluoromethoxy)phenyl]imidazol-1-yl]methyl]phenoxy]hexanoic acid
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| Synonyms |
MA 0204MA-0204 MA0204.
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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: ~43.3 mg/mL (~90.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.17 mg/mL (4.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (4.55 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 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0987 mL | 10.4934 mL | 20.9868 mL | |
| 5 mM | 0.4197 mL | 2.0987 mL | 4.1974 mL | |
| 10 mM | 0.2099 mL | 1.0493 mL | 2.0987 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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