| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
TRPC5[1]
Evifacotrep targets the short transient receptor potential channel 5 (TRPC5) as an antagonist. TRPC5 is a non-selective cation channel involved in various physiological processes including neuronal excitability, pain sensation, and anxiety. The compound also targets TRPC4 channels with an IC50 ≤50 nM. By antagonizing TRPC5, the compound may modulate calcium signaling and neuronal function. It can be used for research of neurological diseases. The compound is a small molecule with drug-like properties. |
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| ln Vitro |
In HEK-TRExhTRPC4 ICLN-1694 cells, evifacotrep (1 μM) suppresses cell proliferation for a duration of 24 hours [1].
In vitro studies demonstrate that Evifacotrep is an antagonist of short transient receptor potential channel 5 (TRPC5). It targets TRPC5/TRPC4 with an IC50 ≤50 nM. The compound's potent antagonism of TRPC5 makes it a valuable tool for studying the role of TRPC5 channels in neuronal function and disease. Evifacotrep can be used for research of neurological diseases. Detailed in vitro characterization data, including binding affinity and functional assays, are available in the primary literature (WO2020061162, compound 100). |
| ln Vivo |
Following puromycin aminonucleoside (PAN) damage, evifacotrep (30 mg/kg; subcutaneous injection; once or twice daily for 10 days) reduces the excretion of albumin in the urine [1].
In vivo studies of Evifacotrep are limited in publicly available literature. As a TRPC5 antagonist, the compound has potential for in vivo investigations of neurological diseases. TRPC5 channels are involved in various neurological processes including anxiety, pain, and neurodegeneration. However, specific in vivo efficacy data and detailed animal model studies are not extensively reported. Further research is needed to establish its in vivo activity profile, pharmacokinetic properties, and therapeutic potential. The compound remains a research tool for TRPC5 channel biology. |
| Enzyme Assay |
For TRPC5 channel binding and functional assays, cells expressing TRPC5 channels (e.g., HEK293 cells) are cultured and loaded with calcium-sensitive fluorescent dyes. Evifacotrep is dissolved in DMSO and diluted in assay buffer to varying concentrations. Cells are treated with the compound and TRPC5 activation is induced by appropriate agonists. Calcium flux is measured using fluorescence plate readers. IC50 values (≤50 nM) are calculated from dose-response curves. For selectivity assays, similar protocols are used with other TRP channels. Assays are performed in replicate with appropriate vehicle controls and positive controls.
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| Cell Assay |
For in vitro cellular assays, cells expressing TRPC5 channels (e.g., HEK293 cells or neuronal cells) are cultured in appropriate media under standard conditions (37°C, 5% CO2). Evifacotrep is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. TRPC5 channel activity is assessed by measuring intracellular calcium flux using fluorescent indicators upon agonist stimulation. Cell viability and cytotoxicity can be assessed using MTT or similar assays. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies of Evifacotrep, no specific published protocols are available. For general in vivo administration of TRPC5 antagonists, compounds are typically formulated in suitable vehicles and administered via oral gavage, intraperitoneal (i.p.) injection, or intravenous (i.v.) injection. Dosing regimens vary by study objective. For neurological disease models, animals may be treated with compound and behavioral or pathological endpoints are assessed. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Evifacotrep are characteristic of a small-molecule TRPC5 antagonist. The compound has a molecular weight of 441.77, formula C18H12ClF4N5O2, and CAS number 2413739-88-3. Purity: high. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO (10 mM in DMSO available). Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources.
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| Toxicity/Toxicokinetics |
According to available safety information, Evifacotrep is intended for research purposes only and cannot be sold to patients. 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 | |
| Additional Infomation |
Evifacotrep is a small molecule drug. The INN prefix "-cotrep" in its name indicates that Evifacotrep is a transient receptor potential classical channel 5 (TRPC5) antagonist. The monoisotopic molecular weight of Evifacotrep is 441.06 Da.
Evifacotrep is a short transient receptor potential channel 5 (TRPC5) antagonist with an IC50 ≤50 nM. It targets TRPC5/TRPC4 channels and can be used for research of neurological diseases. It has a molecular weight of 441.77 and formula C18H12ClF4N5O2. It is for research use only with no clinical development or regulatory approvals reported. |
| Molecular Formula |
C18H12CLF4N5O2
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|---|---|
| Molecular Weight |
441.77
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| Exact Mass |
441.061
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| CAS # |
2413739-88-3
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| PubChem CID |
146448026
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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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 |
30
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| Complexity |
734
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=O)NN=CC(N2CC3C(CC2)=C(OC2=CC=C(F)C=C2C(F)(F)F)N=CN=3)=C1Cl
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| InChi Key |
IQFZADSTVFSHDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12ClF4N5O2/c19-15-13(6-26-27-16(15)29)28-4-3-10-12(7-28)24-8-25-17(10)30-14-2-1-9(20)5-11(14)18(21,22)23/h1-2,5-6,8H,3-4,7H2,(H,27,29)
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| Chemical Name |
5-chloro-4-[4-[4-fluoro-2-(trifluoromethyl)phenoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-1H-pyridazin-6-one
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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) |
DMSO: 50 mg/mL (113.18 mM)
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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 | 2.2636 mL | 11.3181 mL | 22.6362 mL | |
| 5 mM | 0.4527 mL | 2.2636 mL | 4.5272 mL | |
| 10 mM | 0.2264 mL | 1.1318 mL | 2.2636 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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