WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526945
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.
Hodoodo Cat#: H526945
Name: YM-264 fumarate
CAS#: 131888-54-5 (fumarate)
Chemical Formula: C28H36N4O5S
Exact Mass: 0.00
Molecular Weight: 540.679
Elemental Analysis: C, 62.20; H, 6.71; N, 10.36; O, 14.80; S, 5.93
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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
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 540.68 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
