MK-7246

Cat. No.: HY-15853 Purity: 99.63%: FAQs
Data Sheet SDS COA Handling Instructions

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MK-7246 is a potent and selective CRTH2 antagonist with a K_i of 2.5±0.5 nM.

For research use only. We do not sell to patients.

MK-7246 Chemical Structure

CAS No. : 1218918-62-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 319	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 319	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 97	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of MK-7246:

MK-7246 S enantiomer Get quote

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DP EP FP IP TXA₂/TP TXB₂

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

MK-7246 is a potent and selective CRTH2 antagonist with a K_i of 2.5±0.5 nM.

IC₅₀ & Target^[1]

2.5 nM (Ki)

3804 nM (Ki)

In Vitro

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 (K_i, 2.5 nM). MK-7246 displays a relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (K_i, 373±96 nM) and ≥1500-fold lower for the other prostanoid receptors (K_i, 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.

In Vivo

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). Mast cell derived production of Prostaglandin D₂ (PGD₂) is believed to be a prime mediator of allergic inflammation. Since CRTH2 plays an important role in the early aspects of the allergic inflammation cascade, the effect of the CRTH2 antagonist is examined on A. alternate elicited pulmonary inflammatory responses. 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

416.47

Formula

C₂₁H₂₁FN₂O₄S

CAS No.

1218918-62-7

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4011 mL	12.0057 mL	24.0113 mL
5 mM	0.4802 mL	2.4011 mL	4.8023 mL
10 mM	0.2401 mL	1.2006 mL	2.4011 mL

View the 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.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 3.75 mg/mL (9.00 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 3.75 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.63%

Select Batch:

Data Sheet (281 KB) SDS (392 KB)

COA (253 KB) LCMS (93 KB)

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]

Kinase Assay ^[1]	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 (K_obs) and dissociation rate (k_off) constants, and t_1/2 of on and off rates^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

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

Inflammation/Immunology Endocrinology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-72461218918-62-7MK7246MK 7246Prostaglandin ReceptorInhibitorinhibitorinhibit

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