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EMD638683

Cat. No. M11404
EMD638683  Structure
Size Price Availability Quantity
5mg USD 300  USD300 In stock
25mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

EMD638683 is a highly selective SGK1 inhibitor with an IC50 value of 3 μM.

Chemical Information
Molecular Weight 364.34
Formula C18H18F2N2O4
CAS Number 1181770-72-8
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] Abhishek Kumar Verma, et al. J Biomol Struct Dyn. Unlocking SGK1 inhibitor potential of bis-[1-N,7-N, pyrazolo tetraethoxyphthalimido{-4-(3,5-Dimethyl-4-(spiro-3-methylpyazolo)-1,7-dihydro-1H-dipyrazolo[3,4-b;4',3'-e]pyridin-8-yl)}]p-disubstituted phenyl compounds: a computational study

[2] Jakob Voelkl, et al. J Clin Invest. SGK1 induces vascular smooth muscle cell calcification through NF-κB signaling

[3] Wenqiang Gan, et al. Biochim Biophys Acta Mol Basis Dis. The SGK1 inhibitor EMD638683, prevents Angiotensin II-induced cardiac inflammation and fibrosis by blocking NLRP3 inflammasome activation

[4] Syeda T Towhid, et al. Cell Physiol Biochem. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683

[5] Teresa F Ackermann, et al. Cell Physiol Biochem. EMD638683, a novel SGK inhibitor with antihypertensive potency

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  Catalog
Abmole Inhibitor Catalog




Keywords: EMD638683 supplier, SGK, inhibitors, activators


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