179102-65-9
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- CAS号:
- 179102-65-9
- 英文名:
- Benzamide, N-[5-[3-[(4-chlorophenyl)sulfonyl]propyl]-2-(2H-tetrazol-5-ylmethoxy)phenyl]-3-[[4-(1,1-dimethylethyl)-2-thiazolyl]methoxy]-
- 英文别名:
- YM158 free base;YM-158 free base,YM158 free base;Benzamide, N-[5-[3-[(4-chlorophenyl)sulfonyl]propyl]-2-(2H-tetrazol-5-ylmethoxy)phenyl]-3-[[4-(1,1-dimethylethyl)-2-thiazolyl]methoxy]-
- 中文名:
- 179102-65-9
- 中文别名:
- 化合物 T10501
- CBNumber:
- CB33339616
- 分子式:
- C32H33ClN6O5S2
- 分子量:
- 681.22
- MOL File:
- 179102-65-9.mol
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179102-65-9化学性质
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密度:
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1.383±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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4.12±0.10(Predicted)
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179102-65-9性质、用途与生产工艺
YM158 free base 是一种有效的选择性 LTD4 和 TXA2 受体拮抗剂, pA2 值分别为 8.87 和 8.81。
LTD
4
8.87 (pA2)
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TXA
2
Receptor
8.81 (pA2)
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YM158 antagonizes leukotriene (LT) D
4
and thromboxane (TX) A
2
receptors. Functional assays in vitro show that YM158 exhibits competitive dual antagonism of LTD
4
and TXA
2
receptor-mediated contraction of isolated guinea pig tracheae, with pA
2
values of about 8.87 and 8.81, respectively. Its antagonistic activity for the LTD
4
receptor is approximately 6.5 times less potent than that of Montelukast, and that for the TXA
2
receptor is 2.5 times more potent than that of Seratrodast. YM158 also inhibits PGD
2
- and PGF
2α
-induced tracheal contractions. YM158 antagonizes the stable TXA
2
analog U46619-induced aggregation of both guinea pig and human platelets and inhibits the LTD
4
-induced contraction of guinea pig ileum. YM158 produces a concentration-dependent inhibition of guinea pig ileum contraction induced by 1 nM LTD
4
with an IC
50
value of 0.58 nM.
YM158, an orally active dual antagonist for LTD
4
and TXA
2
receptors, is expected to have a stronger antiasthmatic efficacy in a broader class of asthmatic patients than single antagonistic drugs.The effect of YM158 is examined on these asthmatic responses in mediator-controlled and passively sensitized guinea pigs. Because the inhibitory effects of YM158 on increase in the airway resistance induced by LTD
4
or U46619 are shown to be dose-dependent when p.o. administered 1 h before LTD
4
or U46619 injection, with ED
50
values of 8.6 and 14 mg/kg, respectively, the antagonistic activities of p.o. YM158 for LTD
4
and TXA
2
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 LTD
4
is predominant, TXA
2
is predominant; or where both mediators participated equally. 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.
179102-65-9
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179102-65-9, 179102-65-9 相关搜索:
- C32H33ClN6O5S2
- 化合物 T10501
- 179102-65-9
- YM-158 free base,YM158 free base
- YM158 free base
- Benzamide, N-[5-[3-[(4-chlorophenyl)sulfonyl]propyl]-2-(2H-tetrazol-5-ylmethoxy)phenyl]-3-[[4-(1,1-dimethylethyl)-2-thiazolyl]methoxy]-