Biological Activity
Potent intermediate conductance Ca2+-activated K+ channel (KCa3.1) blocker (Kd = 60 nM). Has no effect on cytochrome p450 activity. Inhibits I-EBIO-stimulated increases in rat artery membrane potential ex vivo. Also diminishes LPS-induced cryptidin (mammalian α-defensin) release from paneth cells in vitro.
Compound Libraries
TRAM 39 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 303.78 |
| Formula | C20H14ClN |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 197525-99-8 |
| PubChem ID | 9861261 |
| InChI Key | JHNRTPKGSCVKKC-UHFFFAOYSA-N |
| Smiles | ClC(C=CC=C3)=C3C(C2=CC=CC=C2)(C#N)C1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 15.44 | 50 | |
| ethanol | 3.09 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 303.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.29 mL | 16.46 mL | 32.92 mL |
| 5 mM | 0.66 mL | 3.29 mL | 6.58 mL |
| 10 mM | 0.33 mL | 1.65 mL | 3.29 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wulff et al (2000) 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. 97 8151 PMID: 10884437
Burnham et al (2006) Impaired small-conductance Ca2+-activated K+ channel-dependent EDHF responses in Type II diabetic ZDF rats. Br.J.Pharmacol. 148 434 PMID: 16682967
Ayabe et al (2002) Modulation of mouse Paneth cell alpha-defensin secretion by mIKCa1, a Ca2+-activated, intermediate conductance potassium channel. J.Biol.Chem. 277 3793 PMID: 11724775
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