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Englerin A 

Cat. No. M27785
Englerin A  Structure
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Biological Activity

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload.

Chemical Information
Molecular Weight 442.54
Formula C26H34O6
CAS Number 1094250-15-3
Form Solid
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] Tiago Rodrigues, et al. Angew Chem Int Ed Engl. Unveiling (-)-Englerin A as a Modulator of L-Type Calcium Channels

[2] Suat Peng Neo, et al. J Proteome Res. Englerin A Rewires Phosphosignaling via Hsp27 Hyperphosphorylation to Induce Cytotoxicity in Renal Cancer Cells

[3] Florian J Sulzmaier, et al. PLoS One. Englerin a selectively induces necrosis in human renal cancer cells

[4] Sarath P D Seenadera, et al. ACS Med Chem Lett. Biological Effects of Modifications of the Englerin A Glycolate

[5] João de Sousa Valente, et al. Int J Mol Sci. (-)-Englerin-A Has Analgesic and Anti-Inflammatory Effects Independent of TRPC4 and 5

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