Home>>Signaling Pathways>> GPCR/G protein>> Prostaglandin Receptor>>YM158 free base (YM-57158)

YM158 free base (YM-57158) Sale

(Synonyms: YM-57158) 目录号 : GC31980

YM158 free base (YM-57158) 是一种有效的选择性 LTD4 和 TXA2 受体拮抗剂,pA2 值分别约为 8.87 和 8.81。

YM158 free base (YM-57158) Chemical Structure

Cas No.:179102-65-9

规格 价格 库存 购买数量
1mg
¥14,637.00
现货
5mg
¥29,274.00
现货
10mg
¥51,676.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Animal experiment:

Guinea pigs[2]Male Hartley guinea pigs are used. Effects of YM158 (30 mg/kg, p.o.) , Pranlukast, and Daltroban are measured on the shortening of onset time for asthmatic response. Each compound is administered p.o. to animals without or with 5 mg/kg or 1 mg/kg of Indomethacin[2].

References:

[1]. Arakida Y, et al. In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
[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.

产品描述

YM158 free base is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.

YM158 antagonizes leukotriene (LT) D4 and thromboxane (TX) A2 receptors. Functional assays in vitro show that YM158 exhibits competitive dual antagonism of LTD4 and TXA2 receptor-mediated contraction of isolated guinea pig tracheae, with pA2 values of about 8.87 and 8.81, respectively. 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 with an IC50 value of 0.58 nM[1].

YM158, an orally active dual antagonist for LTD4 and TXA2 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 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; 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[2].

[1]. Arakida Y, et al. In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9. [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.

Chemical Properties

Cas No. 179102-65-9 SDF
别名 YM-57158
Canonical SMILES O=C(NC1=CC(CCCS(=O)(C2=CC=C(Cl)C=C2)=O)=CC=C1OCC3=NN=NN3)C4=CC=CC(OCC5=NC(C(C)(C)C)=CS5)=C4
分子式 C32H33ClN6O5S2 分子量 681.22
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.468 mL 7.3398 mL 14.6795 mL
5 mM 0.2936 mL 1.468 mL 2.9359 mL
10 mM 0.1468 mL 0.734 mL 1.468 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置