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DS16570511

Cat. No. M14197
DS16570511 Structure
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Biological Activity

DS16570511 is cell-permeable inhibitor of the mitochondrial calcium uniporter, which blocks the MCU- or MICU1-dependent increase of Ca2+ influx.

Chemical Information
Molecular Weight 562.44
CAS Number 2446154-84-1
Solubility (25°C) DMSO 90 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] Konstantin N Belosludtsev, et al. The effect of DS16570511, a new inhibitor of mitochondrial calcium uniporter, on calcium homeostasis, metabolism, and functional state of cultured cortical neurons and isolated brain mitochondria

[2] Katalin Mrta, et al. Pharmacological inhibition of the mitochondrial Ca 2+ uniporter: Relevance for pathophysiology and human therapy

[3] David S Dang, et al. Inhibition of mitochondrial calcium uniporter enhances postmortem proteolysis and tenderness in beef cattle

[4] Manuel Vicente, et al. Visualization of Mitochondrial Ca 2+ Signals in Skeletal Muscle of Zebrafish Embryos with Bioluminescent Indicators

[5] Naohiro Kon, et al. DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter

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Keywords: DS16570511 supplier, Calcium Channel, inhibitors, activators


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