MK-7246
产品说明书
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同义名 : | - |
| CAS号 : | 1218918-62-7 | |
| 货号 : | A358757 | |
| 分子式 : | C21H21FN2O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 416.47 | |
| MDL号 : | MFCD22741619 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 300 mg/mL(720.35 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that has been reported to modulate inflammatory responses in various rodent models of asthma, allergic rhinitis and atopic dermatitis[3]. MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5 ± 0.5 nM[3]. MK-7246 displays a relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (Ki, 373 ± 96 nM) and ≥1500-fold lower for the other prostanoid receptors (Ki, 7668 ± 2169 nM for EP2, 3804 ± 1290 nM for TP). MK-7246 is also tested in a panel of 157 enzyme and receptor assays at concentrations up to 100 μM and small but significant activity is detected only on phosphodiesterase 1 (PDE1, IC50 = 33.2 μM) and MAPK3 (ERK1, IC50 = 49.4 μM)[3]. MK-7246 yields ex vivo blockade of CRTH2 on eosinophils in monkeys and sheep, and it significantly blocks antigen-induced late-phase bronchoconstriction and airway hyper-responsiveness in sheep[3]. In a dose-dependent manner, MK-7246 decreased eosinophil influx and Th2 cytokine production following the alternaria alternata challenge[4]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
12.01mL 2.40mL 1.20mL |
24.01mL 4.80mL 2.40mL |
| 参考文献 |
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