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1416581-40-2

1416581-40-2 structure
1416581-40-2 structure
  • Name: MK-8318
  • Chemical Name: MK-8318
  • CAS Number: 1416581-40-2
  • Molecular Formula: C27H26F4N2O5
  • Molecular Weight: 534.50
  • Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
  • Create Date: 2019-02-18 18:09:46
  • Modify Date: 2024-01-31 18:38:41
  • MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

Name MK-8318
Description MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Related Catalog
Target

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].
References

[1]. Huang X, et al. Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684.

Molecular Formula C27H26F4N2O5
Molecular Weight 534.50
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