1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. MK-8318

MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

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

MK-8318 Chemical Structure

MK-8318 Chemical Structure

CAS No. : 1416581-40-2

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Description

MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

IC50 & Target[1]

DP

5.0 nM (Ki)

β-arrestin

3.5 nM (IC50)

cAMP

8.0 nM (IC50)

CYP3A4

50 μM (IC50)

CYP2C9

50 μM (IC50)

CYP2D6

50 μM (IC50)

In Vitro

MK-8318 also inhibits β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 with IC50s of 3.5±2.1 nM, 8.0±6.8 nM, 50 µM, 50 µM and 50 µM[1].

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

In Vivo

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy. MK-8318 also displays good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing[1].

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

Molecular Weight

534.50

Formula

C27H26F4N2O5

CAS No.
SMILES

FC1=CC=C(N(C(C2=CC=C(OC(F)(F)F)C=C2)=O)[C@@H](CCC3)[C@@H]3[C@H]4N(C(CCC(O)=O)=O)C5CC5)C4=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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MK-8318 Related Classifications

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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.

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Product Name:
MK-8318
Cat. No.:
HY-112604
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