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MK-8318

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

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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	Availability
25 mg	$2,120	10-14 weeks
50 mg	$2,780	10-14 weeks
100 mg	$3,700	10-14 weeks

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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), cAMP:8.0 nM, CYP2D6:50 μM, CYP3A4:50 μM, β-arrestin:3.5 nM, CYP2C9:50 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
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.

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In Vivo Formulation Calculator (Clear solution)

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

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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

Keywords

β-arrestinMK-8318MK8318MK 8318CYP3A4CYP2D6CYP2C9CRTH2/DP2 ReceptorcAMP