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CIAC001

Cat. No. M42594
CIAC001 Structure
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Biological Activity

CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity.

Chemical Information
Molecular Weight 339.43
Formula C20H25N3O2
CAS Number 2649154-82-3
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] Sha Jin et al. J Med Chem. Cannabidiol Analogue CIAC001 for the Treatment of Morphine-Induced Addiction by Targeting PKM2

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PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1.

PKM2-IN-4

Pkm2-in-4 is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces mitochondrial H202 production rate and electron transport system coupling.

TP-1454

TP-1454 is an activator of PKM2 and can be used in studies related to solid tumors.

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Keywords: CIAC001 supplier, Pyruvate Kinase, inhibitors, activators


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