YM-264 fumarate

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

MedKoo CAT#: 526945

CAS#: 131888-54-5 (fumarate)

Description: YM-264 is a selective, potent and orally active platelet-activating factor antagonist potentially for the treatment of asthma. YM264 inhibited [3H] platelet-activating factor binding to rabbit platelet membranes with a pKi value of 8.85. YM264 inhibited the platelet-activating factor-induced human, rabbit and guinea-pig platelet aggregation with pA2 values of 8.68, 8.33 and 8.14, respectively. ight in a parallel manner.


Price and Availability

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YM-264 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526945
Name: YM-264 fumarate
CAS#: 131888-54-5 (fumarate)
Chemical Formula: C28H36N4O5S
Exact Mass:
Molecular Weight: 540.679
Elemental Analysis: C, 62.20; H, 6.71; N, 10.36; O, 14.80; S, 5.93


Related CAS #: 126911-71-5 (free base)   131888-54-5 (fumarate)    

Synonym: YM-264; YM 264; YM-64.

IUPAC/Chemical Name: (4-(3-methyl-3-phenylbutyl)piperazin-1-yl)(2-(pyridin-3-yl)thiazolidin-4-yl)methanone fumarate

InChi Key: LBPPBLYOJCIZRW-WLHGVMLRSA-N

InChi Code: InChI=1S/C24H32N4OS.C4H4O4/c1-24(2,20-8-4-3-5-9-20)10-12-27-13-15-28(16-14-27)23(29)21-18-30-22(26-21)19-7-6-11-25-17-19;5-3(6)1-2-4(7)8/h3-9,11,17,21-22,26H,10,12-16,18H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+

SMILES Code: O=C(N1CCN(CCC(C2=CC=CC=C2)(C)C)CC1)C3NC(C4=CC=CN=C4)SC3.O=C(O)/C=C/C(O)=O


Technical Data

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).

Harmonized System Code:
293490


Additional Information


References

1: Tsukumo Y, Harada D, Manabe H. Pharmacological characterization of itch-associated response induced by repeated application of oxazolone in mice. J Pharmacol Sci. 2010;113(3):255-62. PubMed PMID: 20595784.

2: Suzuki T, Nagaoka H, Hara H, Takeuchi M, Saito M, Yamada T, Tomioka K, Matsumoto H, Takanuki K, Mase T. 2-(3-Pyridyl)thiazolidine-4-carboxamide derivatives. III.) Synthesis of metabolites and metabolism of 2-(3-pyridyl)thiazolidine-4-carboxamides YM461 and YM264 as platelet-activating factor (PAF) receptor antagonists. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):165-70. PubMed PMID: 10071851.

3: Yamano M, Umeda M, Miyata K, Yamada T. Protective effects of a PAF receptor antagonist and a neutrophil elastase inhibitor on multiple organ failure induced by cerulein plus lipopolysaccharide in rats. Naunyn Schmiedebergs Arch Pharmacol. 1998 Aug;358(2):253-63. PubMed PMID: 9750012.

4: Nagaoka H, Hara H, Suzuki T, Takahashi T, Takeuchi M, Matsuhisa A, Saito M, Yamada T, Tomioka K, Mase T. 2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel orally active antagonists of platelet-activating factor (PAF). Chem Pharm Bull (Tokyo). 1997 Oct;45(10):1659-64. PubMed PMID: 9353894.

5: Arima M, Yukawa T, Makino S. Effect of YM264 on the airway hyperresponsiveness and the late asthmatic response in a guinea pig model of asthma. Chest. 1995 Aug;108(2):529-34. PubMed PMID: 7634894.

6: Yamada T, Tomioka K, Horie M, Sakurai Y, Nagaoka H, Mase T. Effects of YM264, a novel PAF antagonist, on puromycin aminonucleoside-induced nephropathy in the rat. Biochem Biophys Res Commun. 1991 Apr 30;176(2):781-5. PubMed PMID: 2025290.

7: Yamada T, Tomioka K, Saito M, Horie M, Mase T, Hara H, Nagaoka H. Pharmacological properties of YM264, a potent and orally active antagonist of platelet-activating factor. Arch Int Pharmacodyn Ther. 1990 Nov-Dec;308:123-36. PubMed PMID: 2099131.