LY518674 | CAS# 425671-29-0 | PPAR-alpha agonist

MedKoo Cat#: 522712 | Name: LY518674

Description:

WARNING: This product is for research use only, not for human or veterinary use.

LY518674 is a Potent and selective PPAR-alpha agonist. 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. LY518674 is a potent and selective PPARalpha agonist that produced a much greater increase in serum HDL-c than the known fibrate drugs.

Chemical Structure

LY518674

CAS#425671-29-0

Theoretical Analysis

MedKoo Cat#: 522712

Name: LY518674

CAS#: 425671-29-0

Chemical Formula: C23H27N3O4

Exact Mass: 409.2002

Molecular Weight: 409.49

Elemental Analysis: C, 67.46; H, 6.65; N, 10.26; O, 15.63

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

LY518674; LY-518674; LY 518674.

IUPAC/Chemical Name

2-methyl-2-(4-(3-(1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)propyl)phenoxy)propanoic acid

InChi Key

PNHFDVSKDSLUFH-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H27N3O4/c1-16-7-9-18(10-8-16)15-26-22(29)24-20(25-26)6-4-5-17-11-13-19(14-12-17)30-23(2,3)21(27)28/h7-14H,4-6,15H2,1-3H3,(H,27,28)(H,24,25,29)

SMILES Code

CC(OC1=CC=C(CCCC(N2)=NN(CC3=CC=C(C)C=C3)C2=O)C=C1)(C)C(O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 409.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Khera AV, Millar JS, Ruotolo G, Wang MD, Rader DJ. Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome. Eur Heart J. 2015 Nov 14;36(43):3020-2. doi: 10.1093/eurheartj/ehv291. Epub 2015 Jun 25. PubMed PMID: 26112886; PubMed Central PMCID: PMC4644252. 2: Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N. Identification of the first potent, selective and bioavailable PPARα antagonist. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. doi: 10.1016/j.bmcl.2014.03.090. Epub 2014 Apr 4. PubMed PMID: 24745969. 3: Shah A, Rader DJ, Millar JS. The effect of PPAR-alpha agonism on apolipoprotein metabolism in humans. Atherosclerosis. 2010 May;210(1):35-40. doi: 10.1016/j.atherosclerosis.2009.11.010. Epub 2009 Dec 14. Review. PubMed PMID: 20005515. 4: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Mar;31(2):107-46. PubMed PMID: 19455266. 5: Mahdavi H, Kim JB, Safarpour S, Tien DA, Navab M. Dyslipidemia and cardiovascular diseases. Curr Opin Lipidol. 2009 Apr;20(2):157-8. doi: 10.1097/MOL.0b013e32832956ed. PubMed PMID: 19276898. 6: Ogata M, Tsujita M, Hossain MA, Akita N, Gonzalez FJ, Staels B, Suzuki S, Fukutomi T, Kimura G, Yokoyama S. On the mechanism for PPAR agonists to enhance ABCA1 gene expression. Atherosclerosis. 2009 Aug;205(2):413-9. doi: 10.1016/j.atherosclerosis.2009.01.008. Epub 2009 Jan 19. PubMed PMID: 19201410; PubMed Central PMCID: PMC2790138. 7: Millar JS, Duffy D, Gadi R, Bloedon LT, Dunbar RL, Wolfe ML, Movva R, Shah A, Fuki IV, McCoy M, Harris CJ, Wang MD, Howey DC, Rader DJ. Potent and selective PPAR-alpha agonist LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. Arterioscler Thromb Vasc Biol. 2009 Jan;29(1):140-6. doi: 10.1161/ATVBAHA.108.171223. Epub 2008 Nov 6. PubMed PMID: 18988892; PubMed Central PMCID: PMC2746746. 8: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Jun;30(5):383-408. PubMed PMID: 18806898. 9: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Apr;30(3):231-51. PubMed PMID: 18597009. 10: Hossain MA, Tsujita M, Gonzalez FJ, Yokoyama S. Effects of fibrate drugs on expression of ABCA1 and HDL biogenesis in hepatocytes. J Cardiovasc Pharmacol. 2008 Mar;51(3):258-66. doi: 10.1097/FJC.0b013e3181624b22. PubMed PMID: 18356690. 11: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Nov;29(9):625-55. PubMed PMID: 18193114. 12: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jul-Aug;29(6):427-37. PubMed PMID: 17922073. 13: Nissen SE, Nicholls SJ, Wolski K, Howey DC, McErlean E, Wang MD, Gomez EV, Russo JM. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials. JAMA. 2007 Mar 28;297(12):1362-73. Epub 2007 Mar 25. PubMed PMID: 17384435. 14: Singh JP, Kauffman R, Bensch W, Wang G, McClelland P, Bean J, Montrose C, Mantlo N, Wagle A. Identification of a novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-2-(4-{3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]prop yl}phenoxy)propanoic acid (LY518674), that produces marked changes in serum lipids and apolipoprotein A-1 expression. Mol Pharmacol. 2005 Sep;68(3):763-8. Epub 2005 Jun 2. PubMed PMID: 15933217. 15: Xu Y, Mayhugh D, Saeed A, Wang X, Thompson RC, Dominianni SJ, Kauffman RF, Singh J, Bean JS, Bensch WR, Barr RJ, Osborne J, Montrose-Rafizadeh C, Zink RW, Yumibe NP, Huang N, Luffer-Atlas D, Rungta D, Maise DE, Mantlo NB. Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist. J Med Chem. 2003 Nov 20;46(24):5121-4. PubMed PMID: 14613314.