MK-8318

Name: MK-8318
Brand: TargetMol
SKU: T16097
Rating: 4.5 (1 reviews)

😃Good

Catalog No. T16097Cas No. 1416581-40-2

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

MK-8318

😃Good

Catalog No. T16097Cas No. 1416581-40-2

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,120	10-14 weeks	10-14 weeks
50 mg	$2,780	10-14 weeks	10-14 weeks
100 mg	$3,700	10-14 weeks	10-14 weeks

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).
Targets&IC50	CRTH2/DP2 receptor:5.0 nM (ki), β-arrestin:3.5 nM, CYP2C9:50 μM, cAMP:8.0 nM, CYP2D6:50 μM, CYP3A4:50 μM
In vitro	MK-8318 suppresses β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 (IC50s: 3.5±2.1 nM, 8.0±6.8 nM, 50 μM, 50 μM and 50 μM).
In vivo	MK-8318 demonstrates 76% efficacy in late airway response (LAR) and 114% efficacy in airway hyperresponsiveness (AHR) by blocking LAR and AHR after intravenous infusion at 1 mg/kg in a sheep model. It also exhibits good efficacy on BAL cells/pulmonary function in ovalbumin-sensitized and -challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing.

Chemical Properties

Molecular Weight	534.5
Formula	C₂₇H₂₆F₄N₂O₅
Cas No.	1416581-40-2
Smiles	N(C(CCC(O)=O)=O)([C@H]1C=2C(N(C(=O)C3=CC=C(OC(F)(F)F)C=C3)[C@@]4([C@]1(CCC4)[H])[H])=CC=C(F)C2)C5CC5
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc