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MK-7246

MK-7246

产品编号 TQ0051   CAS 1218918-62-7

MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).

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MK-7246 Chemical Structure
MK-7246, CAS 1218918-62-7
规格 价格/CNY 货期 数量
5 mg ¥ 2,730 8-10周
25 mg ¥ 10,900 8-10周
50 mg ¥ 14,900 8-10周
100 mg ¥ 19,900 8-10周
1 mL * 10 mM (in DMSO) ¥ 2,610 8-10周
其他形式的 MK-7246:
产品目录号及名称: MK-7246 (TQ0051)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).
靶点活性 CRTH2:2.5 nM (Ki)
体外活性 MK-7246 competes for [3H]PGD2 specific binding to cell membranes expressing recombinant human CRTH2 with high-affinity (Ki, 2.5 nM). MK-7246 displays 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) [1].
体内活性 Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose-dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05) [2].
激酶实验 The binding kinetics of [3H]MK-7246 (specific activity, 41 Ci/mmol) at human CRTH2 is characterized using recombinant HEK293E cell membranes. The radioligand binding experimental condition for CRTH2 as follows: the incubation mixture contains 10 mM MgCl2 instead of MnCl2, 10 nM [3H]MK-7246, and 1.25 μg of membrane protein. Total binding represents 10% of the radioligand adds to the incubation media, and specific binding at equilibrium corresponded to 85 to 95% of the total binding. The membranes are first incubated with [3H]MK-7246 for 120 min in the absence (total binding) or presence (nonspecific binding) of 10 μM MK-7246. To one series of total binding incubation tubes, 10 μM MK-7246 or 100 μM PGD2 is added to initiate dissociation of the radioligand from the receptor, and the reaction is left to proceed for up to 300 min. The samples are then harvested and processed as detailed above. The association and dissociation kinetic data analysis is done by nonlinear regression curve-fitting using Prism software to determine the observed on rate (Kobs) and dissociation rate (koff) constants, and t1/2 of on and off rates [1].
动物实验 Intratracheal Budesonide is dosed 1 h prior to and 23 h post the A. alternate intratracheal dose while oral Budesonide (3 mg/kg) is administered 2 h before and 22 h post the A. alternata extract instillation. An intratracheally dosed Budesonide is prepared. MK-7246 (3, 10, 30 and 100 mg/kg) is administered orally 1 h before and 23 h post an A. alternata extract instillation in order to examine the effect of the CRTH2 antagonist on A. alternata elicited pulmonary inflammatory responses. Budesonide dosed orally is used as a positive control in both experiments. The animals are lightly anesthetized with 3% Isoflurane (supplemented with 100% oxygen), either 2 h following oral dosing or 1 h following intratracheal dosing. The animals are also secured on a rodent work stand to facilitate the localization of the larynx and tracheal openings. The micro sprayer needle is inserted into the trachea and 0.1 mL of 10,000 μg/mL (total of 1000 μg) A. alternata extract is administered using a micro sprayer. The animals are observed until they recover from anesthesia and then return to their cages and allow food and water ad libitum [2].
分子量 416.47
分子式 C21H21FN2O4S
CAS No. 1218918-62-7

存储

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

溶解度

DMSO: 245 mg/mL (588.27 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4011 mL 12.0057 mL 24.0113 mL 60.0283 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL 12.0057 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 mL 6.0028 mL
20 mM 0.1201 mL 0.6003 mL 1.2006 mL 3.0014 mL
50 mM 0.048 mL 0.2401 mL 0.4802 mL 1.2006 mL
100 mM 0.024 mL 0.1201 mL 0.2401 mL 0.6003 mL

计算器

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参考文献

1. Gervais FG, et al. Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist. Mol Pharmacol. 2011 Jan;79(1):69-76. 2. Gil MA, et al. Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation. Eur J Pharmacol. 2014 Nov 15;743:106-16.
AM-1638 CRTh2 antagonist 1 4-CMTB LY2922470 Grp94 Inhibitor-1 ONC212 Tetrahydromagnolol GW9508

剂量换算

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

MK-7246 1218918-62-7 Endocrinology/Hormones GPCR/G Protein GPR MK7246 MK 7246 Inhibitor inhibitor inhibit

 

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