| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
TRAM-39 specifically targets the intermediate-conductance calcium-activated potassium channel KCa3.1 (also known as IKCa1). It acts as a potent and selective blocker of this channel. By inhibiting KCa3.1, TRAM-39 modulates calcium-dependent potassium efflux, which is crucial for regulating membrane potential and cellular excitability in various cell types. This blockade helps in studying the channel's role in diseases like neurological disorders and inflammation.
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| ln Vitro |
In sympathetic LAH neurons of BAE cells, TRAM-39 (1 μM) lowers the peak amplitude of gKCa2 (mean percent change: 56%) [2]. In Paneth cells, lipopolysaccharide (LPS)-induced cryptin release is lessened by TRAM-39 (200 nM) [3].
In vitro, TRAM-39 is a potent blocker of KCa3.1 channels with an IC50 of 60 nM. In electrophysiological studies on sympathetic LAH neurons, TRAM-39 at a concentration of 1 μM was shown to lower the peak amplitude of gKCa2 (calcium-activated potassium current) by a mean of 56%. In Paneth cells, it inhibits secretion stimulated by bacteria or bacterial lipopolysaccharide. It has no effect on cytochrome p450 activity, indicating a degree of selectivity. |
| ln Vivo |
In multicellular preparations, TRAM-39 (1 μM) entirely blocks all IKCa channels when introduced to the perfusate [1].
In vivo, TRAM-39 has been shown to inhibit I-EBIO-stimulated increases in rat artery membrane potential ex vivo. This demonstrates its ability to modulate vascular function by blocking KCa3.1 channels in a tissue preparation. This ex vivo activity supports its potential for use in studying the role of KCa3.1 channels in cardiovascular and other systemic conditions. |
| Enzyme Assay |
In vitro binding or functional assays for TRAM-39 typically involve electrophysiological techniques. To determine its potency and selectivity, researchers use patch-clamp electrophysiology on cells (e.g., HEK-293 cells) that have been transfected to express the KCa3.1 channel. The compound is applied at various concentrations, and the inhibition of potassium currents through the channel is measured. The concentration required to inhibit 50% of the current (IC50) is then calculated, which for TRAM-39 is 60 nM.
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| Cell Assay |
In vitro cell-based assays for TRAM-39 are performed to study its functional effects on cellular processes. For example, its effect on calcium signaling and secretion can be studied in Paneth cells. Cells are treated with TRAM-39 (e.g., 1 μM), and the resulting changes in membrane potential, calcium influx, or downstream secretory responses are measured. These assays help to confirm the compound's mechanism of action and its impact on KCa3.1-dependent cellular functions.
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| Animal Protocol |
In vivo animal experiments for TRAM-39 have been conducted to study its effects on vascular function. In one ex vivo study, rat arteries were treated with TRAM-39, and the compound was shown to inhibit I-EBIO-stimulated increases in membrane potential. This indicates that TRAM-39 can effectively block KCa3.1 channels in a tissue setting, suggesting its potential for further in vivo studies in models of cardiovascular or neurological diseases.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TRAM-39 indicate it is a small, lipophilic molecule. The compound has a molecular weight of 303.78 and a molecular formula of C20H14ClN. Its chemical name is 2-(2-chlorophenyl)-2,2-diphenylacetonitrile. It is soluble in DMSO up to 15.44 mg/mL. The powder is stable when stored at -20°C for up to 3 years or at 4°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicology data for TRAM-39 are limited. The compound is intended for research use only and is not for human therapeutic use. It has been shown to have no effect on cytochrome p450 activity, which could indicate a lower potential for drug-drug interactions. However, its full toxicological profile, including potential off-target effects and long-term safety, has not been extensively characterized.
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| References |
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| Additional Infomation |
Other information: TRAM-39 is also known as TRAM 39. Its IUPAC name is 2-(2-chlorophenyl)-2,2-diphenylacetonitrile. It is supplied as a solid powder with a purity of ≥98%. The compound is primarily used as a pharmacological tool to study the function of KCa3.1 channels in various biological systems, including neurological and inflammatory conditions.
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| Molecular Formula |
C20H14CLN
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|---|---|
| Molecular Weight |
303.78
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| Exact Mass |
303.081
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| CAS # |
197525-99-8
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| PubChem CID |
9861261
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.197
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C(C#N)(C2=CC=CC=C2)C3=CC=CC=C3Cl
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| InChi Key |
JHNRTPKGSCVKKC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H14ClN/c21-19-14-8-7-13-18(19)20(15-22,16-9-3-1-4-10-16)17-11-5-2-6-12-17/h1-14H
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| Chemical Name |
2-(2-chlorophenyl)-2,2-diphenylacetonitrile
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| Synonyms |
TRAM 39 TRAM-39 TRAM39
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~164.59 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 | 3.2919 mL | 16.4593 mL | 32.9186 mL | |
| 5 mM | 0.6584 mL | 3.2919 mL | 6.5837 mL | |
| 10 mM | 0.3292 mL | 1.6459 mL | 3.2919 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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