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MK-7246 | Antagonist of PTGDR2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTGDR2
  • Ki:2.5 nM
  • IC50:3 nM
  • IC50:2.2 nM
  • IC50:2.3 nM
Antagonist
100 nM, up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
> 100-fold against related receptors; Hits in the GPCR scan are SLC6A3 (Ki = 283 nM), GABA/PBR (Ki = ...

Potency
Cellular
In Vitro

PTGDR2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2010.11.015

In Vivo Validations

Rat
Dose: 5 mg/Kg PO, 1 mg/Kg IV
Route of delivery: Oral, Intravenus
Plasma half life: 5.6 h
Systemic clearance: 2.2 mL/min/kg
Cmax: 12200 nM
Area Under the Curve:: 128 mM*h
Bioavailability: 138 %
Volume of Distribution at Steady-State: 0.98 L/Kg

DOI Reference: 10.1016/j.bmcl.2010.11.015

Dog
Dose: 5 mg/Kg PO, 1 mg/Kg IV
Route of delivery: Oral, Intravenus
Plasma half life: 8.4 h
Systemic clearance: 15 mL/min/kg
Cmax: 580 nM
Area Under the Curve:: 1.6 mM*h
Bioavailability: 67 %
Volume of Distribution at Steady-State: 2.3 L/Kg

DOI Reference: 10.1016/j.bmcl.2010.11.015

Negative Control Compounds

CRTH2-negative-control

Chemical Information

Molecular Formula C21H21FN2O4S
SMILEs CN([C@@H]1CCc2c(CC(=O)O)c3ccccc3n2C1)S(=O)(=O)c1ccc(F)cc1
InChI InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-21(25)26)17-4-2-3-5-19(17)24(20)13-15/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)/t15-/m1/s1
Molecular weight 416.12 Da
AlogP 3.043000000000002
HBond acceptors 6
HBond donors 1
Atoms 50
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Vendors

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Expert Reviews

No SERP comments found for MK-7246

Probe MK-7246 is in the process of SERP review.

Please continue to check back for new reviews and commentary.