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MK-8318

MK-8318
MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).
Catalog No. T16097Cas No. 1416581-40-2

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MK-8318

Catalog No. T16097Cas No. 1416581-40-2

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).
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.
Pack SizePriceAvailabilityQuantity
25 mg$2,27010-14 weeks
50 mg$2,98010-14 weeks
100 mg$4,00010-14 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
CYP2D6:50 μM, cAMP:8.0 nM, CYP3A4:50 μM, CYP2C9:50 μM, β-arrestin:3.5 nM, CRTH2/DP2 receptor:5.0 nM (ki)
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 Weight534.5
FormulaC27H26F4N2O5
Cas No.1416581-40-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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