MK-7246
Based on 1 publication(s) in Google Scholar
MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
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- Purity: 99.63%
- CAS No.: 1218918-62-7
- 화학식: C21H21FN2O4S
- 분자량:416.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) MK-7246
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Biological Activity
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DP 2.5 nM (Ki) |
TP 3804 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.7 nM
Compound: 6, MK-7246
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Displacement of [3H]PGD2 from human CRTH2 expressed in HEK293 cells after 60 mins by liquid scintillation counting
Displacement of [3H]PGD2 from human CRTH2 expressed in HEK293 cells after 60 mins by liquid scintillation counting
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[PMID: 22224640] |
| HEK293 | IC50 |
3 nM
Compound: MK-7246
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Antagonist activity at human CRTH2 expressed in HEK293 cells assessed as inhibition of forskolin-induced increase intracellular [125I]cAMP level by scintillation proximity assay
Antagonist activity at human CRTH2 expressed in HEK293 cells assessed as inhibition of forskolin-induced increase intracellular [125I]cAMP level by scintillation proximity assay
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[PMID: 21185722] |
| HEK293 | IC50 |
3 nM
Compound: 4, MK-7246
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Antagonist activity at human recombinant CRTH2 receptor expressed in HEK293 cells assessed as inhibition of DK-PGD2-induced intracellular cAMP formation
Antagonist activity at human recombinant CRTH2 receptor expressed in HEK293 cells assessed as inhibition of DK-PGD2-induced intracellular cAMP formation
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[PMID: 21106375] |
| HEK293-EBNA | IC50 |
3 nM
Compound: MK-7246
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Antagonist activity at human CRTH2 receptor expressed in HEK293-EBNA cells assessed as inhibition of forskolin-stimulated intracellular cAMP production by [125I]-cAMP scintillation proximity assay
Antagonist activity at human CRTH2 receptor expressed in HEK293-EBNA cells assessed as inhibition of forskolin-stimulated intracellular cAMP production by [125I]-cAMP scintillation proximity assay
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[PMID: 21515053] |
The affinity and selectivity of MK-7246 for human CRTH2 and recombinant human prostanoid receptors is determined by equilibrium competition analysis using the relevant radioligands and cell membranes expressing the various receptors. 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 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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1218918-62-7
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Appearance Solid
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분자량 416.47
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화학식 C21H21FN2O4S
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Color White to off-white
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SMILES
O=C(O)CC1=C(CC[C@@H](N(S(=O)(C2=CC=C(F)C=C2)=O)C)C3)N3C4=C1C=CC=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
용액&용해도
DMSO : 300 mg/mL (720.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 3.75 mg/mL (9.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3.75 mg/mL (9.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
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 an oral dosing or 1 h following an intratracheal dosing. The animals are also secured on a rodent work stand to facilitate the localization of the larynx and tracheal openings. The microsprayer 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 microsprayer. The animals are observed until they recover from anesthesia and then return to their cages and allow food and water ad libitum.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 | |
| 15 mM | 0.1601 mL | 0.8004 mL | 1.6008 mL | 4.0019 mL | |
| 20 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0014 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9605 mL | 2.4011 mL | |
| 30 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0009 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6003 mL | 1.5007 mL | |
| 50 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2006 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL | |
| 80 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7504 mL | |
| 100 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6003 mL |
MK-7246 Related Classifications
HY-15853 Related Classifications
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