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Chemical Structure| 289905-88-0 Chemical Structure| 289905-88-0

Structure of TRAM-34
CAS No.: 289905-88-0

Chemical Structure| 289905-88-0

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TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM).

Synonyms: Triarylmethane-34

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Product Details of TRAM-34

CAS No. :289905-88-0
Formula : C22H17ClN2
M.W : 344.84
SMILES Code : ClC1=C(C=CC=C1)C(N1C=CC=N1)(C1=CC=CC=C1)C1=CC=CC=C1
Synonyms :
Triarylmethane-34
MDL No. :MFCD09842562
InChI Key :KBFUQFVFYYBHBT-UHFFFAOYSA-N
Pubchem ID :656734

Safety of TRAM-34

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H412
Precautionary Statements:P273

Isoform Comparison

Biological Activity

Target
  • Potassium Channel

    IKCa1 (KCa3.1), Kd:20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human T lymphocytes 25 nM 3–6 minutes TRAM-34 selectively blocks the IKCa1 channel with a Kd of 25 nM PMC16685
COS-7 cells 20 nM 3–6 minutes TRAM-34 selectively blocks the IKCa1 channel with a Kd of 20 nM PMC16685
PAS T cells 1 µM 48-72 hours TRAM-34 only partially suppressed proliferation of PAS cells PMC61146
Murine CLL B cells from Eμ-TCL1 mice 10 μM Reduced cell viability PMC8848658
Primary human chronic lymphocytic leukemia (CLL) cells 10 μM Decreased CLL cell proliferation PMC8848658
Acutely activated T cells 1 µM 72 hours TRAM-34 completely suppressed proliferation of acutely activated T cells PMC61146
Quiescent T cells 1 µM 72 hours TRAM-34 completely suppressed proliferation of quiescent T cells PMC61146
Bone marrow-derived macrophages (BMDMs) 5 µM 3 hours To investigate the effect of TRAM-34 on DSS-enhanced ATP or nigericin-induced NLRP3 inflammasome activation. Results showed that TRAM-34 significantly inhibited DSS-enhanced NLRP3 inflammasome activation and subsequent pyroptosis. PMC9338299
Human lung mast cells (HLMC) 20 or 200 nM 3 hours TRAM-34 markedly inhibited HLMC migration towards CXCL10, SCF, and ASM supernatants in a dose-dependent manner. PMC2104766
Human cardiac micro-vascular endothelial cells (HCMVECs) 1 μM 30 minutes To investigate the effect of TRAM-34 on IKCa oxidation/tyrosine nitration in HCMVECs treated with high glucose and homocysteine. Results showed that TRAM-34 inhibited EDHF-induced vascular relaxation. PMC5854893
Human T84 colonic epithelial cells 22 nM 3–6 minutes TRAM-34 blocks IKCa1 currents in human T84 colonic epithelial cells with a Kd of 22 nM PMC16685
Murine renal fibroblasts (TFB) 100 nM 24 hours Inhibited bFGF-induced renal fibroblast proliferation via G0/G1 arrest PMC2726862
Human microglial cells 1 μM TRAM-34 significantly reduced the ATP-induced current potentiation but did not completely abolish it PMC7883449

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice DSS-induced colitis model Intraperitoneal injection 40 mg/kg body weight Twice daily until the endpoint To investigate the effect of TRAM-34 on DSS-induced colitis. Results showed that TRAM-34 significantly alleviated DSS-induced colitis symptoms, including weight loss, increased disease activity index (DAI), and colon shortening. Additionally, TRAM-34 reduced inflammasome activation in the colon. PMC9338299
Eμ-TCL1 mice Chronic lymphocytic leukemia (CLL) model Intraperitoneal injections 10 nmol/g Once a day for 2 weeks TRAM-34 did not show any beneficial effect in vivo PMC8848658
Mice Db/db mice (Type 2 diabetes model) In vitro administration (vascular ring assay) 1 μM Single dose, 30 minutes To investigate the effect of TRAM-34 on EDHF-induced vascular relaxation in small mesenteric arteries (SMAs) of db/db mice. Results showed that TRAM-34 inhibited EDHF-induced vascular relaxation. PMC5854893
Rat Mesenteric artery In vitro perfusion 1 μM To investigate the role of TRPC3 channels in rat mesenteric artery. Pyr3 significantly reduced the ACh-induced endothelium-dependent vasodilation. PMC3422079
CF-1BR mice Acute toxicity test Intravenous injection 0.5 mg/kg Single dose, observed for 7 days TRAM-34 is not acutely toxic at ~500–1,000 times the channel-blocking dose PMC16685
Rat Isolated perfused heart model Perfusate 1 μM 25–30 minutes To evaluate the effect of TRAM-34 on SKA-31-induced increases in coronary flow. Results showed that TRAM-34 alone or in combination with apamin significantly inhibited the increases in coronary flow induced by SKA-31, bradykinin, and adenosine. PMC3543990
Mice and rats Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 120 mg/kg Once daily for 3 weeks Attenuated progression of UUO-induced renal fibrosis, reduced collagen deposition and αSMA-positive cells PMC2726862
Apoe–/– mice Atherosclerosis model Subcutaneous injection 120 mg/kg/d Once daily for 12 weeks To study the effect of TRAM-34 on the development of atherosclerosis. Results showed that TRAM-34 significantly reduced atherosclerotic lesion area in aortas and carotid arteries, suppressed VSMC proliferation, macrophage and T lymphocyte infiltration, and reduced oxidative stress. PMC2496961
Lewis rats Adoptive transfer experimental autoimmune encephalomyelitis (AT-EAE) Intraperitoneal injection 170 µg/kg Three more injections at 4-hr intervals on day 0, three injections on day 1, and two injections on days 2–5 TRAM-34 alone had no effect on preventing AT-EAE, but enhanced the effect when combined with ShK-Dap22 PMC61146

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.50mL

2.90mL

1.45mL

29.00mL

5.80mL

2.90mL

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