| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
TRAM-34 (TRAM34; TRAM 34 Triarylmethane-34) is an inhibitor of Ca2+-activated K+ channel (IKCa1, KCa3.1) with important biological activity. It inhibits Ca2+-activated K+ channel with a Kd of 20 nM, and exhibits 200- to 1500-fold higher selectivity over cloasely related ion channels..
| ln Vitro |
TRAM-34 selectively blocks IKCa1 currents (Kd=25 nM), and TRAM-34 also blocks IKCa1 currents in human T84 colon epithelial cells with same efficacy (Kd= 22 nM). TRAM-34 blocks cloned and native IKCa1 channels in human T cells with a Kd of 20-25 nM and is 200 to 1500 times more selective than other ion channels. The dosage response curve demonstrates that 1 μM calcium in the pipette has a Kd of 20±3 nM and a Hill coefficient of 1.2 [1]. TRAM-34 is a selective inhibitor of KCa 3.1 channels that boosts or lowers cell proliferation depending on concentration. At intermediate concentrations (3-10 μM) TRAM-34 enhances cell proliferation, but at higher concentrations (20-100 μM) TRAM-34 lowers cell proliferation. The augmentation of cell proliferation generated by TRAM-34 was prevented by the estrogen receptor antagonists ICI182,780 and Tamoxifen. TRAM-34 also enhances progesterone receptor mRNA expression, decreases estrogen receptor-α mRNA expression, and diminishes the binding of radiolabeled estrogen to the MCF-7 estrogen receptor, in each case imitating 17β-estrogen receptor The involvement of glycol [2].
|
||
|---|---|---|---|
| ln Vivo |
Mice (n = 5) given a single intravenous dosage of TRAM-34 (0.5 mg/kg; 29 μM) for seven days showed no abnormalities in their clinical appearance. The TRAM-34 treatment group's body weight data (Day 1: 17.8 g; Day 7: 27.0 g) matched the vehicle-injected control mice's body weight data (Day 1: 17.4 g; Day 7: 23.4 g). Overall, at 500–1,000 times the amount required to block the channel, TRAM-34 is not acutely hazardous, according to results from these small toxicity experiments [1]. Hematoxylin and eosin (H&E) measurements of lesion area were considerably decreased with TRAM-34 treatment; the mean infarct size decreased from 22.6±3.6% in the control group (n=8) to 10 mg/kg TRAM-34. In rats treated with 40 mg/kg TRAM-34, the percentage decreased to 8.1±1.9% (n=8; P=0.004) from 11.3±2.8% in rats (n=6, mean±s.e.m., P=0.039). Additionally, this treatment helps to lessen brain shrinkage. But only the 40 mg/kg TRAM-34 group's results were statistically significant (P=0.013), but the 10 mg/kg group's results were not (P=0.11) [3].
|
||
| Animal Protocol |
|
||
| References |
[1]. Wulff H, et al. Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant. Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):8151-6.
[2]. Roy JW, et al. The intermediate conductance Ca2+-activated K+ channel inhibitor TRAM-34 stimulates proliferation of breast cancer cells via activation of oestrogen receptors. Br J Pharmacol. 2010 Feb 1;159(3):650-8. [3]. Chen YJ, et al. The KCa3.1 blocker TRAM-34 reduces infarction and neurological deficit in a rat model of ischemia/reperfusion stroke. J Cereb Blood Flow Metab. 2011 Dec;31(12):2363-74 |
| Molecular Formula |
C22H17CLN2
|
|
|---|---|---|
| Molecular Weight |
344.84
|
|
| CAS # |
289905-88-0
|
|
| Related CAS # |
|
|
| SMILES |
ClC1=CC=CC=C1C(N2N=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4
|
|
| Synonyms |
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 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 |
*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.
|
|---|
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
