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MedKoo Cat#: 561812 | Name: Pemafibrate sodium

Description:

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

Pemafibrate sodium is discontinued

Chemical Structure

Pemafibrate sodium
Pemafibrate sodium
CAS#950644-31-2 (sodium)

Theoretical Analysis

MedKoo Cat#: 561812

Name: Pemafibrate sodium

CAS#: 950644-31-2 (sodium)

Chemical Formula: C28H29N2NaO6

Exact Mass: 512.1923

Molecular Weight: 512.53

Elemental Analysis: C, 65.62; H, 5.70; N, 5.47; Na, 4.49; O, 18.73

Price and Availability

This product was removed for the commercial reasons.
Related CAS #
950644-31-2 (sodium) 848259-27-8 (free acid)
Synonym
Pemafibrate sodium;
IUPAC/Chemical Name
Sodium (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoate
InChi Key
JSNXVHCVJMDNKW-VQIWEWKSSA-M
InChi Code
InChI=1S/C28H30N2O6.Na/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22;/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32);/q;+1/p-1/t25-;/m1./s1
SMILES Code
CC[C@@H](OC1=CC=CC(CN(C2=NC3=CC=CC=C3O2)CCCOC4=CC=C(OC)C=C4)=C1)C([O-])=O.[Na+]
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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 512.53 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.

Recalculate based on batch purity %
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: Araki E, Yamashita S, Arai H, Yokote K, Satoh J, Inoguchi T, Nakamura J, Maegawa H, Yoshioka N, Tanizawa Y, Watada H, Suganami H, Ishibashi S. Effects of Pemafibrate, a Novel Selective PPARα Modulator, on Lipid and Glucose Metabolism in Patients With Type 2 Diabetes and Hypertriglyceridemia: A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial. Diabetes Care. 2018 Jan 3. pii: dc171589. doi: 10.2337/dc17-1589. [Epub ahead of print] PubMed PMID: 29298800. 2: Sumida Y, Yoneda M. Current and future pharmacological therapies for NAFLD/NASH. J Gastroenterol. 2017 Dec 16. doi: 10.1007/s00535-017-1415-1. [Epub ahead of print] Review. PubMed PMID: 29247356. 3: Ishibashi S, Arai H, Yokote K, Araki E, Suganami H, Yamashita S; K-877 Study Group. Efficacy and safety of pemafibrate (K-877), a selective peroxisome proliferator-activated receptor α modulator, in patients with dyslipidemia: Results from a 24-week, randomized, double blind, active-controlled, phase 3 trial. J Clin Lipidol. 2017 Oct 28. pii: S1933-2874(17)30466-X. doi: 10.1016/j.jacl.2017.10.006. [Epub ahead of print] PubMed PMID: 29203092. 4: Fujioka Y. Effects of a Novel Selective Peroxisome Proliferator-Activated Receptor α Modulator K-877 (Pemafibrate) on Postprandial hyperlipidemia. J Atheroscler Thromb. 2017 Oct 18. doi: 10.5551/jat.ED088. [Epub ahead of print] PubMed PMID: 29046503. 5: Fruchart JC. Pemafibrate (K-877), a novel selective peroxisome proliferator-activated receptor alpha modulator for management of atherogenic dyslipidaemia. Cardiovasc Diabetol. 2017 Oct 4;16(1):124. doi: 10.1186/s12933-017-0602-y. Review. PubMed PMID: 28978316; PubMed Central PMCID: PMC5628452. 6: Blair HA. Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810. doi: 10.1007/s40265-017-0818-x. PubMed PMID: 28929345. 7: Sairyo M, Kobayashi T, Masuda D, Kanno K, Zhu Y, Okada T, Koseki M, Ohama T, Nishida M, Sakata Y, Yamashita S. A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb. 2017 Aug 5. doi: 10.5551/jat.39693. [Epub ahead of print] PubMed PMID: 28781340. 8: Camejo G. Phase 2 clinical trials with K-877 (pemafibrate): A promising selective PPAR-α modulator for treatment of combined dyslipidemia. Atherosclerosis. 2017 Jun;261:163-164. doi: 10.1016/j.atherosclerosis.2017.04.013. Epub 2017 Apr 15. PubMed PMID: 28434555. 9: Arai H, Yamashita S, Yokote K, Araki E, Suganami H, Ishibashi S; K-877 Study Group. Efficacy and safety of K-877, a novel selective peroxisome proliferator-activated receptor α modulator (SPPARMα), in combination with statin treatment: Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia. Atherosclerosis. 2017 Jun;261:144-152. doi: 10.1016/j.atherosclerosis.2017.03.032. Epub 2017 Mar 24. PubMed PMID: 28410749. 10: Ferri N, Corsini A, Sirtori C, Ruscica M. PPAR-α agonists are still on the rise: an update on clinical and experimental findings. Expert Opin Investig Drugs. 2017 May;26(5):593-602. doi: 10.1080/13543784.2017.1312339. Epub 2017 Apr 11. Review. PubMed PMID: 28343425. 11: Reiner Ž. Hypertriglyceridaemia and risk of coronary artery disease. Nat Rev Cardiol. 2017 Jul;14(7):401-411. doi: 10.1038/nrcardio.2017.31. Epub 2017 Mar 16. Review. PubMed PMID: 28300080. 12: Honda Y, Kessoku T, Ogawa Y, Tomeno W, Imajo K, Fujita K, Yoneda M, Takizawa T, Saito S, Nagashima Y, Nakajima A. Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. Sci Rep. 2017 Feb 14;7:42477. doi: 10.1038/srep42477. PubMed PMID: 28195199; PubMed Central PMCID: PMC5307366. 13: Hennuyer N, Duplan I, Paquet C, Vanhoutte J, Woitrain E, Touche V, Colin S, Vallez E, Lestavel S, Lefebvre P, Staels B. The novel selective PPARα modulator (SPPARMα) pemafibrate improves dyslipidemia, enhances reverse cholesterol transport and decreases inflammation and atherosclerosis. Atherosclerosis. 2016 Jun;249:200-8. doi: 10.1016/j.atherosclerosis.2016.03.003. Epub 2016 Mar 4. PubMed PMID: 27108950. 14: Ishibashi S, Yamashita S, Arai H, Araki E, Yokote K, Suganami H, Fruchart JC, Kodama T; K-877-04 Study Group. Effects of K-877, a novel selective PPARα modulator (SPPARMα), in dyslipidaemic patients: A randomized, double blind, active- and placebo-controlled, phase 2 trial. Atherosclerosis. 2016 Jun;249:36-43. doi: 10.1016/j.atherosclerosis.2016.02.029. Epub 2016 Feb 26. PubMed PMID: 27062408. 15: Yamazaki Y, Ogawa S, Shibuya K. Synthesis of highly deuterium-labeled (R)-K-13675, PPAR alpha agonist, for use as an internal standard for low-level quantification of drugs in plasma. Bioorg Med Chem. 2009 Mar 1;17(5):1911-7. doi: 10.1016/j.bmc.2009.01.049. Epub 2009 Feb 13. PubMed PMID: 19217302. 16: Kitajima K, Miura S, Mastuo Y, Uehara Y, Saku K. Newly developed PPAR-alpha agonist (R)-K-13675 inhibits the secretion of inflammatory markers without affecting cell proliferation or tube formation. Atherosclerosis. 2009 Mar;203(1):75-81. doi: 10.1016/j.atherosclerosis.2008.05.055. Epub 2008 Jun 6. PubMed PMID: 18606415.