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S-2E

Cat. No. M8184
S-2E Structure
Synonym:

S2E

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Biological Activity

S-2E is an orally active and noncompetitive HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. S-2E has an anti-hyperlipidemic action. In the liver, S-2E is converted into its active metabolite, S-2E-CoA. S-2E-CoA noncompetitively inhibited the enzymatic activities of both 3-hydroxy-3-methylglutaryl coenzyme-A (HMG-CoA) reductase and acetyl-CoA carboxylase at K(i)=18.11 microM and K(i)=69.2 microM, respectively.

Chemical Information
Molecular Weight 367.44
Formula C22H25NO4
CAS Number 155730-92-0
Solubility (25°C) DMSO 10 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] Agnieszka Gunia-Krzyżak, et al. S(+)-(2 E)- N-(2-Hydroxypropyl)-3-Phenylprop-2-Enamide (KM-568): A Novel Cinnamamide Derivative with Anticonvulsant Activity in Animal Models of Seizures and Epilepsy

[2] Agnieszka Gunia-Krzyżak, et al. Physicochemical and biological evaluation of a cinnamamide derivative R,S-(2E)-1-(3-hydroxypiperidin-1-yl)-3-phenylprop-2-en-1-one (KM-608) for nervous system disorders

[3] Koichi Ohmori, et al. Effects of a novel anti-hyperlipidemic agent, S-2E, on blood lipid levels in rats with fructose-induced hypertriglyceridemia

[4] K Ohmori, et al. Effects of a novel antihyperlipidemic agent, S-2E, on the blood lipid abnormalities in homozygous WHHL rabbits

[5] Koichi Ohmori, et al. Anti-hyperlipidemic action of a newly synthesized benzoic acid derivative, S-2E

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Keywords: S-2E, S2E supplier, Acetyl-CoA Carboxylase, inhibitors, activators


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