MA-0204
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MedKoo CAT#: 555298

CAS#: 2095128-17-7 (free acid)

Description: 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. In normal rats undergoing IR-AKI, MA-0204 attenuates the increases of plasma and urinary biomarkers of AKI, improves renal function, mitigates proximal tubular damage and boosts mitochondrial gene expression. MA-0204 is a potential Treatment for Duchenne Muscular Dystrophy (DMD)

Chemical Structure

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MA-0204
CAS# 2095128-17-7 (free acid)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555298
Name: MA-0204
CAS#: 2095128-17-7 (free acid)
Chemical Formula: C25H27F3N2O4
Exact Mass: 476.19
Molecular Weight: 476.496
Elemental Analysis: C, 63.02; H, 5.71; F, 11.96; N, 5.88; O, 13.43

Price and Availability

Size Price Availability Quantity
100mg USD 1450 2 weeks
200mg USD 1950 2 weeks
500mg USD 2950 2 weeks
1g USD 4250 2 weeks
2g USD 6950 2 weeks
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Related CAS #: 2095128-30-4   2095128-17-7 (free acid)    

Synonym: MA-0204; MA 0204; MA0204.

IUPAC/Chemical Name: (R)-3-methyl-6-(2-((5-methyl-2-(4-(trifluoromethoxy)phenyl)-1H-imidazol-1-yl)methyl)phenoxy)hexanoic acid

InChi Key: GYNMVDMBFKGCCR-QGZVFWFLSA-N

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

SMILES Code: O=C(O)C[C@H](C)CCCOC1=CC=CC=C1CN2C(C)=CN=C2C3=CC=C(OC(F)(F)F)C=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: MA-0204 was tested in vivo in mice and in vitro in patientderived muscle myoblasts (from Duchenne Muscular Dystrophy (DMD) patients); MA-0204 altered the expression of PPARδ target genes and improved fatty acid oxidation, which supports the therapeutic hypothesis for the study of MA-0204 in DMD patients.

Product Data:
Product Data
Instruction:
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Biological target: MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively.
In vitro activity: Compound 17 (MA-0204) was profiled in multiple in vitro and in vivo assays (Table 3). Compound 17 is >10 000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. The PPARδ potency was 10-fold less for mouse and rat PPARδ receptors than for the human PPARδ receptor; this effect is well documented for PPAR modulators. Compound 17 is selective (EC50 >10 μM) over other nuclear receptors, for example: androgen, progesterone, and glucocorticoid receptors. Reference: ACS Med Chem Lett. 2018 Jul 31;9(9):935-940. https://pubmed.ncbi.nlm.nih.gov/30258544/
In vivo activity: To determine if 17 (MA-0204) was capable of eliciting a biological effect in skeletal muscle, mice were dosed orally with MA-0204 and GW501516, and target gene expression was assessed by qPCR (quantitative polymerase chain reaction). As shown in FigureFigure33, 17 increased PPARδ target gene transcription in the muscle, represented here by Pdk4 (pyruvate dehydrogenase kinase 4). Reference: ACS Med Chem Lett. 2018 Jul 31;9(9):935-940. https://pubmed.ncbi.nlm.nih.gov/30258544/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.3 90.93

Preparing Stock Solutions

The following data is based on the product molecular weight 476.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lagu B, Kluge AF, Tozzo E, Fredenburg R, Bell EL, Goddeeris MM, Dwyer P, Basinski A, Senaiar RS, Jaleel M, Tiwari NK, Panigrahi SK, Krishnamurthy NR, Takahashi T, Patane MA. Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD). ACS Med Chem Lett. 2018 Jul 31;9(9):935-940. doi: 10.1021/acsmedchemlett.8b00287. Erratum in: ACS Med Chem Lett. 2019 Apr 24;10(6):1013. PMID: 30258544; PMCID: PMC6142063.
In vitro protocol: 1. Lagu B, Kluge AF, Tozzo E, Fredenburg R, Bell EL, Goddeeris MM, Dwyer P, Basinski A, Senaiar RS, Jaleel M, Tiwari NK, Panigrahi SK, Krishnamurthy NR, Takahashi T, Patane MA. Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD). ACS Med Chem Lett. 2018 Jul 31;9(9):935-940. doi: 10.1021/acsmedchemlett.8b00287. Erratum in: ACS Med Chem Lett. 2019 Apr 24;10(6):1013. PMID: 30258544; PMCID: PMC6142063.
In vivo protocol: 1. Lagu B, Kluge AF, Tozzo E, Fredenburg R, Bell EL, Goddeeris MM, Dwyer P, Basinski A, Senaiar RS, Jaleel M, Tiwari NK, Panigrahi SK, Krishnamurthy NR, Takahashi T, Patane MA. Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD). ACS Med Chem Lett. 2018 Jul 31;9(9):935-940. doi: 10.1021/acsmedchemlett.8b00287. Erratum in: ACS Med Chem Lett. 2019 Apr 24;10(6):1013. PMID: 30258544; PMCID: PMC6142063.

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Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD)
Bharat Lagu, Arthur F. Kluge, Effie Tozzo, Ross Fredenburg, Eric L. Bell, Matthew M. Goddeeris, Peter Dwyer, Andrew Basinski, Ramesh S. Senaiar, Mahaboobi Jaleel, Nirbhay Kumar Tiwari, Sunil K. Panigrahi, Narasimha Rao Krishnamurthy, Taisuke Takahashi, and Michael A. Patane
Publication Date (Web): July 31, 2018 (Letter)
DOI: 10.1021/acsmedchemlett.8b00287