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LY518674

Cat. No. M10453
LY518674 Structure
Synonym:

LY-674

Size Price Availability
5mg USD 500  USD500 4-7 Days
10mg USD 870  USD870 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY518674 is a potent and selective PPAR-alpha antagonist with EC50 of 42 nM for human PPARα. LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. LY518674 produced a dose-dependent increase in serum HDL-c, resulting in 208 +/- 15% elevation at optimum dose. In cultured hepatocytes, LY518674 produced 50% higher apoA-1 secretion, which was associated with increase in radiolabeled methionine incorporation in apoA-1.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 409.48
Formula C23H27N3O4
CAS Number 425671-29-0
Purity >99%
Solubility DMSO ≥ 100 mg/mL
Storage at -20°C
References

[1] Amit V Khera, et al. Eur Heart J. Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome

[2] Yalda Bravo, et al. Bioorg Med Chem Lett. Identification of the first potent, selective and bioavailable PPARα antagonist

[3] Steven E Nissen, et al. JAMA. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials

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  Catalog
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Keywords: LY518674, LY-674 supplier, PPAR, inhibitors

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