1. GPCR/G Protein
  2. Prostaglandin Receptor

MK-8318 

Cat. No.: HY-112604
Handling Instructions

MK-8318 is 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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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

CRTH2/DP2 Receptor

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].

In Vivo

In a sheep model, MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mpk. MK-8318 shows 76% LAR efficacy and 114% AHR efficacy[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8709 mL 9.3545 mL 18.7091 mL
5 mM 0.3742 mL 1.8709 mL 3.7418 mL
10 mM 0.1871 mL 0.9355 mL 1.8709 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

534.50

Formula

C₂₇H₂₆F₄N₂O₅

CAS No.

1416581-40-2

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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

Cat. No.: HY-112604