| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
TRPV1
MK-2295 targets the transient receptor potential vanilloid 1 (TRPV1) receptor as an antagonist. TRPV1 is activated by capsaicin, heat, and protons, and plays a key role in nociception and inflammatory pain. By antagonizing TRPV1, MK-2295 blocks pain signals and provides analgesic effects. The compound has been studied for its potential in pain management. TRPV1 antagonists are of interest for developing novel analgesics for various pain conditions. The compound's mechanism involves blocking TRPV1-mediated calcium influx and nociceptive signaling. |
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| ln Vitro |
In vitro studies demonstrate that MK-2295 (NGD-8243) is a TRPV1 antagonist. The compound has been characterized as an analgesic agent for pain research. TRPV1 antagonists like MK-2295 are used to study the role of TRPV1 in pain sensation and inflammatory pain pathways. The compound's activity against TRPV1 has been established through in vitro binding and functional assays. It is a valuable research tool for studying TRPV1-mediated mechanisms and pain pathways. Specific IC50 values and detailed in vitro characterization data are available in the primary literature.
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| ln Vivo |
In vivo studies of MK-2295 have been reported in the context of pain research. As a TRPV1 antagonist, the compound has been evaluated for analgesic efficacy in preclinical pain models. TRPV1 antagonists have been shown to reduce pain responses in various animal models of inflammatory and neuropathic pain. MK-2295 is used as an analgesic agent in pain research. Specific in vivo efficacy data and animal model studies are available in the primary literature. Further details can be found in the research publications on this compound.
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| Enzyme Assay |
For TRPV1 receptor binding and functional assays, cells expressing TRPV1 receptors (e.g., HEK293 cells) are cultured and loaded with calcium-sensitive fluorescent dyes. MK-2295 is dissolved in DMSO and diluted in assay buffer to varying concentrations. Cells are treated with the compound and TRPV1 activation is induced by capsaicin, heat, or protons. Calcium flux is measured using fluorescence plate readers. IC50 values are calculated from dose-response curves by measuring the reduction in agonist-induced calcium increases. For analgesic activity assessment, standard in vitro assays for pain pathways may be used. Assays are performed in replicate with vehicle controls and positive controls (e.g., capsazepine).
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| Cell Assay |
For in vitro cellular assays, cells expressing TRPV1 receptors (e.g., HEK293 cells or primary sensory neurons) are cultured in appropriate media under standard conditions (37°C, 5% CO2). MK-2295 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. TRPV1 channel activity is assessed by measuring intracellular calcium flux using fluorescent indicators upon capsaicin or heat stimulation. Cell viability and cytotoxicity can also be assessed. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies, MK-2295 is typically formulated in suitable vehicles and administered via appropriate routes (e.g., oral gavage, intraperitoneal injection, or intravenous injection). Dosing regimens vary by study objective. For pain models, animals are treated with compound prior to nociceptive testing (e.g., formalin test, von Frey test, or hot plate test). Analgesic efficacy and duration of action are evaluated. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MK-2295 are characteristic of a small-molecule TRPV1 antagonist. The compound has a molecular weight of 434.34, formula C21H12F6N4, and CAS number 573678-04-3. Storage: powder at -20°C for up to 3 years; at 4°C for up to 2 years; in solvent at -80°C for up to 6 months or at -20°C for up to 1 month. Purity: ≥98%. Appearance: typically exists as solid at room temperature. Solubility: soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters are reported in the primary literature.
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| Toxicity/Toxicokinetics |
According to available safety information, MK-2295 is intended for research use only and not for human therapeutic applications. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References |
[1]. Gunthorpe MJ, et al. Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway. Drug Discov Today. 2009 Jan;14(1-2):56-67.
[2]. Arthur Gomtsyan, et al. Chapter 8 - Clinical and Preclinical Experience with TRPV1 Antagonists as Potential Analgesic Agents. TRP Channels as Therapeutic Targets. From Basic Science to Clinical Use. 2015, Pages 129-144. |
| Additional Infomation |
See also: MK-2295 (Notes moved to).
MK-2295 (NGD-8243) is a TRPV1 antagonist and analgesic agent for pain research. The compound has a molecular weight of 434.34 and formula C21H12F6N4. TRPV1 is a non-selective cation channel involved in pain sensation and inflammation. MK-2295 is a valuable research tool for studying pain pathways and TRPV1-mediated mechanisms. It is for research use only with no clinical development or regulatory approvals reported. |
| Molecular Formula |
C21H12F6N4
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|---|---|
| Molecular Weight |
434.34
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| Exact Mass |
434.096
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| CAS # |
573678-04-3
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| PubChem CID |
11247522
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.440±0.06 g/cm3(Predicted)
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| Boiling Point |
500.9±50.0 °C(Predicted)
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| LogP |
5.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
589
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=CC=CN=C1C1C=CC2=C(N=CN=C2C=1)NC1C=CC(C(F)(F)F)=CC=1)(F)F
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| InChi Key |
VTANGSDRFFLTSQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H12F6N4/c22-20(23,24)13-4-6-14(7-5-13)31-19-15-8-3-12(10-17(15)29-11-30-19)18-16(21(25,26)27)2-1-9-28-18/h1-11H,(H,29,30,31)
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| Chemical Name |
N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3023 mL | 11.5117 mL | 23.0234 mL | |
| 5 mM | 0.4605 mL | 2.3023 mL | 4.6047 mL | |
| 10 mM | 0.2302 mL | 1.1512 mL | 2.3023 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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