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YM158 free base

Catalog No. T10501   CAS 179102-65-9
Synonyms: YM-57158

YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).

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YM158 free base Chemical Structure
YM158 free base, CAS 179102-65-9
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Biological Description
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Description YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).
Targets&IC50 LTD4:8.87(pA2), TXA2 Receptor:8.81 (pA2)
In vitro YM158 exhibits competitive dual antagonism of LTD4 and TXA2 receptor-mediated contraction of isolated guinea pig tracheae (pA2s: about 8.87 and 8.81). Its antagonistic activity for the LTD4 receptor is approximately 6.5 times less potent than that of Montelukast, and that for the TXA2 receptor is 2.5 times more potent than that of Seratrodast. YM158 also inhibits PGD2- and PGF2α -induced tracheal contractions. YM158 antagonizes the stable TXA2 analog U46619-induced aggregation of both guinea pig and human platelets and inhibits the LTD4-induced contraction of guinea pig ileum. YM158 produces a concentration-dependent inhibition of guinea pig ileum contraction induced by 1 nM LTD4 (IC50: 0.58 nM) [1].
In vivo Because the inhibitory effects of YM158 on an increase in the airway resistance induced by LTD4 or U46619 are shown to be dose-dependent when p.o. administered 1 h before LTD4 or U46619 injection, with ED50 values of 8.6 and 14 mg/kg, respectively, the antagonistic activities of p.o. YM158 for LTD4 and TXA2 receptors are exhibited at the same dose range. Oral YM158 shows significant effects, approximately the same as the combination of Pranlukast and Daltroban on antigen-induced response under various conditions; namely, where LTD4 is predominant, TXA2 is predominant. In groups not treated with Indomethacin, administration of Daltroban (10 mg/kg), a combination of Pranlukast (30 mg/kg) and Daltroban (10 mg/kg), or YM158 (30 mg/kg) significantly prolongs the onset time for asthmatic response and significantly suppresses symptoms [2].
Synonyms YM-57158
Molecular Weight 681.22
Formula C32H33ClN6O5S2
CAS No. 179102-65-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Arakida Y, et al. In vitro pharmacologic profile of YM158, a new dual antagonist for LTD 2. Arakida Y, et al. Effects of lipid mediator antagonists on predominant mediator-controlled asthmatic reactions in passively sensitized guinea pigs. J Pharmacol Exp Ther. 1999 Sep;290(3):1285-91.

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Keywords

YM158 free base 179102-65-9 Others YM-57158 YM158 YM 57158 YM57158 YM-158 free base YM-158 YM 158 inhibitor inhibit

 

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