289905-88-0

Basic information

• Product Name: TRAM-34
• Synonyms: Triarylmethane-34
• CAS NO: 289905-88-0
• Molecular Formula: C22H17ClN2
• Molecular Weight: 344.843
• Product Categories: Heterocyclic Compounds;Heterocycles;Inhibitors
• Mol File: 289905-88-0.mol

Chemical Properties

• Melting Point: 145-147°C
• Boiling Point: 510.2°C at 760 mmHg
• Flash Point: 262.4°C
• Appearance: off-white/solid
• Density: 1.13g/cm³
• Vapor Pressure: 5.04E-10mmHg at 25°C
• Refractive Index: 1.616
• Storage Temp.: 2-8°C
• Solubility: DMSO: ~11 mg/mL
• Water Solubility: Soluble in DMSO at 2mg/ml. Insoluble in water
• CAS DataBase Reference: TRAM-34(CAS DataBase Reference)
• NIST Chemistry Reference: TRAM-34(289905-88-0)
• EPA Substance Registry System: TRAM-34(289905-88-0)

Safety Data

• Hazard Codes: Xn
• Statements: 22
• WGK Germany: 3
• Hazardous Substances Data: 289905-88-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
TRAM-34 is used as a pharmacological tool for studying the role of IKCa1 channels in various physiological and pathological processes. Its ability to selectively block IKCa1 channels makes it a valuable compound for investigating the function of these channels in cellular signaling and disease mechanisms.
Used in Research Applications:
In research, TRAM-34 is used as a specific inhibitor of IKCa1 channels, allowing scientists to explore the effects of channel modulation on cellular functions. This can help in understanding the underlying mechanisms of various diseases and conditions related to IKCa1 channel activity.
Used in Drug Development:
Due to its high selectivity and potency, TRAM-34 can be utilized in the development of new drugs targeting IKCa1 channels for the treatment of diseases where these channels play a significant role. This includes conditions such as hypertension, cardiovascular diseases, and certain neurological disorders.
Used in Quality Control:
TRAM-34 is also used in the quality control of pharmaceutical products, as it can be employed to test the purity and potency of IKCa1 channel blockers. This ensures that the final drug product meets the required standards for efficacy and safety.

Biological Activity

Highly selective blocker of intermediate conductance Ca 2+ -activated K + channels (IK Ca 1, K Ca 3.1) (K d = 20 nM). Exhibits 200-1500-fold selectivity over K V , BK Ca , SK Ca , Na + , CRAC and Cl - channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.

Biochem/physiol Actions

TRAM-34 exhibits 100-fold selectivity (Kd = 20 nM) for IKCa1 channels over other K+ channels (Charybdotoxin, Kd = 5 nM, Clotrimazole, Kd = 70 nM; Nitrendipine Kd = 900 nM). Furthermore, TRAM-34 is known to suppress the activation of human T lymphocytes,.

InChI:InChI=1/C22H17ClN2/c23-21-15-8-7-14-20(21)22(25-17-9-16-24-25,18-10-3-1-4-11-18)19-12-5-2-6-13-19/h1-17H

Relevant articles and documents

Non-peptide inhibition of T-lymphocyte activation and therapies related thereto

Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K + channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca ++ activated K + channel (IKCa1) prevents the pre-Ca ++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.