2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. MK-2894

MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=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.

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

MK-2894 Chemical Structure

MK-2894 Chemical Structure

CAS No. : 1006036-87-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 167 In-stock
Solution
10 mM * 1 mL in DMSO USD 167 In-stock
Solid
5 mg USD 160 In-stock
10 mg USD 280 In-stock
50 mg USD 1180 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MK-2894:

MK-2894 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MK-2894

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=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 IC50 values of 2.5 nM and 11 nM, respectively[1].

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

MK-2894 Related Antibodies
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 (Vdss=7.6 L/kg), good elimination half-lives (T1/2=15 h) and the maximum concentration reached (Cmax=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 (Vdss=2.6 L/kg), good elimination half-lives (T1/2=4.5 h) and the maximum concentration reached (Cmax=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 (Vdss=0.91 L/kg), good elimination half-lives (T1/2=8.8 h) and the maximum concentration reached (Cmax=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 ED50 value is 0.02 mg/kg/day. The complete inhibition of the secondary paw swelling is at an ED100 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].

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

473.51

Formula

C25H22F3NO3S
CAS No.
Appearance

Solid

Color

White to light brown

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (105.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.28 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.31%

COA (251 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1119 mL 10.5594 mL 21.1189 mL 52.7972 mL
5 mM 0.4224 mL 2.1119 mL 4.2238 mL 10.5594 mL
10 mM 0.2112 mL 1.0559 mL 2.1119 mL 5.2797 mL
15 mM 0.1408 mL 0.7040 mL 1.4079 mL 3.5198 mL
20 mM 0.1056 mL 0.5280 mL 1.0559 mL 2.6399 mL
25 mM 0.0845 mL 0.4224 mL 0.8448 mL 2.1119 mL
30 mM 0.0704 mL 0.3520 mL 0.7040 mL 1.7599 mL
40 mM 0.0528 mL 0.2640 mL 0.5280 mL 1.3199 mL
50 mM 0.0422 mL 0.2112 mL 0.4224 mL 1.0559 mL
60 mM 0.0352 mL 0.1760 mL 0.3520 mL 0.8800 mL
80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6600 mL
100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5280 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

MK-2894 Related Classifications

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.

Keywords:

MK-28941006036-87-8MK2894MK 2894Prostaglandin ReceptorAIAarthrititinflammationpainInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MK-2894
Cat. No.:
HY-10413
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.