[CAS NO. 1006036-87-8] MK-2894
PRODUCTS SPECIFICATIONS [1006036-87-8]
DESCRIPTION [1006036-87-8]
Overview
| MDL | MFCD18251427 |
|---|---|
| Molecular Weight | 473.51 |
| Molecular Formula | C25H22F3NO3S |
| SMILES | O=C(O)C1=CC=C(C2(NC(C3=C(C)SC(C)=C3CC4=CC=C(C(F)(F)F)C=C4)=O)CC2)C=C1 |
1 Publications Citing Use of MCE
Summary
MK-2894 is a potent, selective, orally active and high affinity ( K i =0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) ( IC 50 =2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis [1] [2] .
In Vitro
MK-2894 shows inhibitory effects on PGE2-induced cAMP accumulation, the EP4 functional potency in HEK 293 and HWB cells with IC
50
values of 2.5 nM and 11 nM, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MK-2894 (oral administration, 20 mg/kg; intravenous injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in mice, the moderate bioavailability F=21%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (V
dss
=7.6 L/kg), good elimination half-lives (T
1/2
=15 h) and the maximum concentration reached (C
max
=1.4 μM) in mice
[1]
.
MK-2894 (oral administration, 20 mg/kg; intravenous injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in SD-rats, the moderate bioavailability F=29%, and slow to moderate clearance rate (CL=9.2 mL/min/kg), the volume of distribution (V
dss
=2.6 L/kg), good elimination half-lives (T
1/2
=4.5 h) and the maximum concentration reached (C
max
=4.5 μM) in mice
[1]
.
MK-2894 (oral administration, 5 mg/kg; intravenous injection, 1 mg/kg) exhibits a favorable pharmacokinetic profile in dogs, the moderate bioavailability F=32%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (V
dss
=0.91 L/kg), good elimination half-lives (T
1/2
=8.8 h) and the maximum concentration reached (C
max
=3.3 μM) in mice
[1]
.
MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg; single dose) inhibits the acute carrageenan-induced mechanical hyperalgesia model in SD rats in a dose-dependent manner, it displays a inhibition of pain response when measured at 3 h post subplantar injection of carrageenan
[1]
.
MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg;5 days) exhibits potent activity in inhibiting chronic paw swelling, in both the primary paw and the secondary paw, in a dose-dependent manner, the ED
50
value is 0.02 mg/kg/day. The complete inhibition of the secondary paw swelling is at an ED
100
of 0.1 mg/kg/day with a plasma concentration of 4 nM at 24 h after the final dose in an adjuvant-induced arthritis rat model
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 105.59 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1119 mL | 10.5594 mL | 21.1189 mL |
| 5 mM | 0.4224 mL | 2.1119 mL | 4.2238 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1119 mL |
References
- [1] Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, O'Neill G, Ducharme Y, Friesen R. The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluorometh
- [2] Tijana Markovič, et al. Structural features of subtype-selective EP receptor modulators. Drug Discov Today. 2017 Jan;22(1):57-71.
