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MBX-102 acid

Cat. No. M7931
MBX-102 acid Structure
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Biological Activity

MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ.

Chemical Information
Molecular Weight 330.69
Formula C15H10ClF3O3
CAS Number 23953-39-1
Solubility (25°C) DMSO: ≥20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Arrigo F G Cicero, et al. Therapeutic Strategies for the Treatment of Chronic Hyperuricemia: An Evidence-Based Update

[2] Theodore R Fields. The Challenges of Approaching and Managing Gout

[3] Thomas Bardin, et al. Novel uricosurics

[4] Apurva Chandalia, et al. MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activation

[5] Holly J Clarke, et al. Cross-Species Differential Plasma Protein Binding of MBX-102/JNJ39659100: A Novel PPAR-gamma Agonist

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