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	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

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

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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, β-arrestin:3.5 nM, CYP3A4:50 μM, 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/Shipping at ambient temperature.

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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% Saline/PBS/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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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