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MK-7246

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Chemical Structure| 1218918-62-7 同义名 : -
CAS号 : 1218918-62-7
货号 : A358757
分子式 : C21H21FN2O4S
纯度 : 99%+
分子量 : 416.466
MDL号 : MFCD22741619
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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
动物实验配方：
生物活性
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
1mg 5mg 10mg

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

[1]Gallant M, Beaulieu C, et al. Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93.

[2]Eriksson J, Roy T, et al. Synthesis and preclinical evaluation of the CRTH2 antagonist [11C]MK-7246 as a novel PET tracer and potential surrogate marker for pancreatic beta-cell mass. Nucl Med Biol. 2019 Apr;71:1-10.

[3]Gervais FG, Sawyer N, Stocco R, Hamel M, Krawczyk C, Sillaots S, Denis D, Wong E, Wang Z, Gallant M, Abraham WM, Slipetz D, Crackower MA, O'Neill GP. 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. doi: 10.1124/mol.110.068585. Epub 2010 Oct 13. PMID: 20943773.

[4]Gil MA, Caniga M, Woodhouse JD, Eckman J, Lee HH, Salmon M, Naber J, Hamilton VT, Sevilla RS, Bettano K, Klappenbach J, Moy L, Correll CC, Gervais FG, Siliphaivanh P, Zhang W, Zhang-Hoover J, McLeod RL, Cicmil M. 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. doi: 10.1016/j.ejphar.2014.09.021. Epub 2014 Sep 23. PMID: 25261040.