1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. TRAM-34

TRAM-34 

Cat. No.: HY-13519 Purity: 99.71%
Handling Instructions

TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K+ channel (IKCa1) (Kd=20 nM).

For research use only. We do not sell to patients.

TRAM-34 Chemical Structure

TRAM-34 Chemical Structure

CAS No. : 289905-88-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K+ channel (IKCa1) (Kd=20 nM).

IC50 & Target

Kd: 20 nM (IKCa1)[1]

In Vitro

TRAM-34 selectively blocks the IKCa1 current (Kd=25 nM), TRAM-34 also blocks IKCa1 currents in human T84 colonic epithelial cells with equivalent potency (Kd=22 nM). TRAM-34 inhibits the cloned and the native IKCa1 channel in human T lymphocytes with a Kd of 20-25 nM and is 200- to 1,500-fold selective over other ion channels. The dose-response curve reveals a Kd of 20±3 nM and a Hill coefficient of 1.2 with 1 μM calcium in the pipette[1]. TRAM-34, a specific inhibitor of KCa 3.1 channels increased or decreased cell proliferation depending on the concentration. At intermediate concentrations (3-10 µM) TRAM-34 increased cell proliferation, whereas at higher concentrations (20-100 µM) TRAM-34 decreased cell proliferation. The enhancement of cell proliferation caused by TRAM-34 is blocked by the oestrogen receptor antagonists ICI182,780 and tamoxifen. TRAM-34 also increases progesterone receptor mRNA expression, decreased oestrogen receptor-α mRNA expression and reduced the binding of radiolabelled oestrogen to MCF-7 oestrogen receptor, in each case mimicking the effects of 17β-oestradiol[2].

In Vivo

Mice (n=5) injected intravenously with a single dose of TRAM-34 (0.5 mg/kg; 29 μM) appeared clinically normal during the 7-day study. The body-weight data of the TRAM-34-treated group (day 1:17.8 g; day 7: 27.0 g) are similar to control mice injected with the vehicle (day 1: 17.4 g; day 7: 23.4 g). Collectively, data from these limited toxicity studies suggest that TRAM-34 is not acutely toxic at ≈500-1,000 times the channel-blocking dose[1].Treatment with TRAM-34 results in a significant reduction in hematoxylin & eosin (H&E) defined lesion area with the mean infarct size being reduced from 22.6±3.6% in the controls (n=8) to 11.3±2.8% in rats treated with 10 mg/kg TRAM-34 (n=6, mean±s.e.m., P=0.039) and to 8.1±1.9% in rats treated with 40 mg/kg TRAM-34 (n=8; P=0.004). The treatment also tended to reduce brain shrinkage. However, the results are only statistically significant with 40 mg/kg TRAM-34 (P=0.013), but not for the 10 mg/kg group (P=0.11)[3].

Molecular Weight

344.84

Formula

C₂₂H₁₇ClN₂

CAS No.

289905-88-0

SMILES

ClC1=CC=CC=C1C(N2N=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (72.50 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8999 mL 14.4995 mL 28.9990 mL
5 mM 0.5800 mL 2.8999 mL 5.7998 mL
10 mM 0.2900 mL 1.4499 mL 2.8999 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.25 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

MCF-7 cell protein (250 µg) is incubated at room temperature for 2 h in TEDG buffer in the presence of 0.1 nM [2,4,6,7,16,17-3H(N)]-oestradiol ([3H]-E2) (110 Ci/mmol) in a total final volume of 500 µL. Non-specific binding is assessed in the presence of a 100-fold excess of non-radioactive E2. TRAM-34 and E2 standards are diluted in phenol red-free 5% DCC-FBS MEM containing supplements before being added to the cytosolic protein. A vehicle control comprised of 5% DCC-FBS MEM containing supplements with 0.7% DMSO. To separate ER-bound [3H]-E2 from unbound [3H]-E2, 250 µL of hydroxylapatite (HAP, 60% in TEDG buffer) is added, the mixture is vortexed every 5 min over 15 min and centrifuged at 1000×g for 10 min. The HAP-[3H]-E2-ER complex is washed with TEDG buffer, centrifuged and the wash step repeated. To elute [3H]-E2 from the HAP-[3H]-E2-ER complex, 500 µL of 100% ethanol is added and the mixture then incubated for 15 min and centrifuged at 1034×g for 10 min. The separated [3H]-E2 is removed and added to 2 mL of scintillation fluid. Radioactivity is quantified using a Beckman LS 5000TA scintillation counter. Competition of [3H]-E2 with TRAM-34 is assayed in quadruplicate on four independent protein extractions. An apparent dissociation constant of 0.135±0.034 nM (n=3) and a maximum binding capacity of 48.3±5.4 fmol/mg (n=3) are determined by Scatchard analysis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][3]

Mice[1]
Five CF-1BR mice (17-19 g) are injected intravenously with a single 1.0-ml dose of 0.5 mg/kg TRAM-34 (in mammalian Ringer solution with 1% ethanol and 2.5% BSA). Five control mice are injected with an equal volume of the vehicle. Mice are observed for adverse effects immediately after dosing, at 4 h after injection and daily for 7 days.
Rats[3]
Adult male Wistar rats weighing 160 to 180 g are used. Rats receive TRAM-34 at 10 mg/kg, 40 mg/kg or vehicle (Miglyol 812 neutral oil at 1 μL/g) twice daily intraperitoneally for 7 days starting 12 hours after reperfusion. Neurological deficits are scored according to a 4-score test and a tactile and proprioceptive limb-placing test as follows: (1) 4-score test (higher score for more severe neurological deficits): 0=no apparent deficit; 1=contralateral forelimb is consistently flexed during suspension by holding the tail; 2=decreasing grip ability on the contralateral forelimb while tail pulled; 3=spontaneous movement in all directions but circling to contralateral side when pulled by the tail; 4=spontaneous contralateral circling or depressed level of consciousness. (2) 14-score limb-placing test (lower score for more severe neurological deficits): proprioception, forward extension, lateral abduction, and adduction are tested with vision or tactile stimuli. For visual limb placing, rats are held and slowly moved forward or lateral toward the top of a table. Normal rats placed both forepaws on the tabletop. Tactile forward and lateral limb placing are tested by lightly contacting the table edge with the dorsal or lateral surface of a rat's paw while avoiding whisker contact and covering the eyes to avoid vision.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TRAM-34
Cat. No.:
HY-13519
Quantity: