| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
EP4 receptor (E prostanoid receptor 4 / prostaglandin E2 receptor subtype 4).
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| ln Vitro |
MK-2894 sodium is a highly potent and selective second-generation EP4 antagonist. It is a full antagonist against the EP4 receptor with a high affinity (Ki=0.56 nM) and an IC50 of 2.5 nM. The compound's in vitro activity is characterized by its ability to bind to the EP4 receptor with high affinity and block PGE2-induced signaling.
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| ln Vivo |
MK-2894 sodium salt (oral, 20 mg/kg; intravenous, 5 mg/kg) exhibits good pharmacokinetic characteristics in mice, with moderate bioavailability F = 21% and slow to moderate clearance ( CL=23 mL/min/kg), volume of distribution (Vdss=7.6 L/kg), good elimination half-life (T1/2=15 h) and the maximum concentration reached in mice (Cmax=1.4 μM) [1] . MK-2894 sodium salt (oral, 20 mg/kg; intravenous, 5 mg/kg) exhibits good pharmacokinetic profiles in SD rats, with moderate bioavailability F = 29%, and slow to moderate clearance. rate (CL=9.2 mL/min/kg), volume of distribution (Vdss=2.6 L/kg), good elimination half-life (T1/2=4.5 h) and the maximum concentration reached in mice (Cmax=4.5 μM) [1]. MK-2894 sodium salt (oral, 5 mg/kg; intravenous, 1 mg/kg) exhibits good pharmacokinetic profiles in dogs, with moderate bioavailability F = 32% and slow to moderate clearance (CL =23 mL/min/kg), volume of distribution (Vdss=0.91 L/kg), good elimination half-life (T1/2=8.8 h) and the maximum concentration reached in mice (Cmax=3.3 μM) [1]. MK-2894 sodium salt (oral; 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, demonstrating a response to pain when measured Inhibition of plantar injection of carrageenan 3 hours later [1]. MK-2894 sodium salt (oral; 0.1 mg/kg-10 mg/kg; 5 days) demonstrated potent activity in inhibiting chronic paw swelling of the primary and secondary paws in a dose-dependent manner with an ED50 value of 0.02 mg/ kg/day. In a rat model of adjuvant-induced arthritis, an ED100 of 0.1 mg/kg/day and a plasma concentration of 4 nM completely inhibited secondary paw swelling 24 hours after the final dose [1].
Specific in vivo activity data for MK-2894 sodium is not detailed in the available literature. Based on its mechanism of action as a potent and selective EP4 receptor antagonist, it is expected to demonstrate anti-inflammatory, analgesic, and anti-tumor effects in preclinical models. The compound is described as orally active, suggesting it is suitable for oral administration in vivo. |
| Enzyme Assay |
In vitro receptor binding assays are performed using membrane preparations from cells expressing recombinant EP4 receptors, incubated with the compound and a labeled EP4 ligand (such as [3H]PGE2) to determine binding affinity (Ki). The assay measures competitive displacement of the radioligand.
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| Cell Assay |
Cell-based functional assays are conducted to evaluate EP4 receptor antagonism. Cells expressing EP4 receptors are treated with the compound and stimulated with PGE2, and receptor-mediated signaling (such as cAMP accumulation) is measured. The compound's ability to inhibit PGE2-induced signaling is assessed to determine antagonist potency (IC50). Standard protocols for studying EP4 antagonism are followed.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of inflammation, pain, or cancer. The compound is administered orally, and endpoints include inflammatory markers, pain behavior, and tumor growth. The compound's ability to reduce inflammation, alleviate pain, and inhibit tumor growth is assessed. Detailed in vivo protocols are not provided in the available literature.
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| References |
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| Molecular Formula |
C₂₅H₂₁F₃NNAO₃S
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|---|---|
| Molecular Weight |
495.48914
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| Exact Mass |
495.109
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| CAS # |
1006036-88-9
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| Related CAS # |
MK-2894; 1006036-87-8
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| PubChem CID |
24953972
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| Appearance |
White to off-white solid powder
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| LogP |
5.148
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
731
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O[Na])C1=CC=C(C2(NC(C3=C(C)SC(C)=C3CC4=CC=C(C(F)(F)F)C=C4)=O)CC2)C=C1
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| InChi Key |
RQRUUNKVGDVBFV-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C25H22F3NO3S.Na/c1-14-20(13-16-3-7-19(8-4-16)25(26,27)28)21(15(2)33-14)22(30)29-24(11-12-24)18-9-5-17(6-10-18)23(31)32;/h3-10H,11-13H2,1-2H3,(H,29,30)(H,31,32);/q;+1/p-1
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| Chemical Name |
sodium;4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoate
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| Synonyms |
MK-2894 sodium; MK 2894; MK2894 sodium
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~10.1 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0182 mL | 10.0910 mL | 20.1820 mL | |
| 5 mM | 0.4036 mL | 2.0182 mL | 4.0364 mL | |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0182 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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