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MLR-1023

Cat. No. M8311
MLR-1023 Structure
Synonym:

Tolimidone

Size Price Availability
5mg USD 50  USD50 Out of stock
25mg USD 160  USD160 Out of stock
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Biological Activity

MLR-1023 (Tolimidone) is a potent, orally active, allosteric activator of the non-receptor Src-related Lyn kinase that produces lasting glucose lowering, reduces HbA1c levels, and preserves pancreatic β-cells in db/db mice. MLR-1023 increased insulin receptor sensitivity. MLR-1023 (Tolimidone) is antiulcer agent.

Chemical Information
Molecular Weight 202.21
Formula C11H10N2O2
CAS Number 41964-07-2
Form Solid
Solubility (25°C) DMSO 60 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] Candida J Rebello, et al. MLR-1023 Treatment in Mice and Humans Induces a Thermogenic Program, and Menthol Potentiates the Effect

[2] Christopher A Lipinski, et al. High throughput in vivo phenotypic screening for drug repurposing: Discovery of MLR-1023 a novel insulin sensitizer and novel Lyn kinase activator with clinical proof of concept

[3] Moon-Kyu Lee, et al. A novel non-PPARgamma insulin sensitizer: MLR-1023 clinicalproof-of-concept in type 2 diabetes mellitus

[4] Michael S Saporito, et al. MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo

[5] Alexander R Ochman, et al. The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes

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Keywords: MLR-1023, Tolimidone supplier, Src-bcr-Abl, inhibitors, activators

 
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