Orally active Ca2+ channel blocker; inhibits K+- and carbachol-stimulated Ca2+ influx (IC50 values are 500 and 935 nM respectively). Exhibits antiproliferative, antiangiogenic and antimetastatic activity in vivo and displays selectivity towards numerous mismatch repair-deficient tumor cell lines in vitro.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 424.67. 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||2.35 mL||11.77 mL||23.55 mL|
|5 mM||0.47 mL||2.35 mL||4.71 mL|
|10 mM||0.24 mL||1.18 mL||2.35 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References are publications that support the biological activity of the product.
Hupe et al (1991) The inhibition of receptor-mediated and voltage-dependent calcium entry by the antiproliferative L-651,582 J.Biol.Chem. 266 10136 PMID: 1645340
Yang et al (2008) Selective sensitivity to carboxyamidotriazole by human tumor cell lines with DNA mismatch repair deficiency. Int.J.Cancer. 123 258 PMID: 18464258
Felder et al (1991) The antiproliferative and antimetastatic compound L651582 inhibits muscarinic acetylcholine receptor-stimulated calcium influx and arachidonic acid release. J.Pharm.Exp.Ther. 257 967
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Keywords: L-651,582, L-651,582 supplier, Ca2+, channel, blockers, Calcium, CaV, Channels, voltage-gated, voltage-dependent, L651582, Carboxyamidotriazole, Voltage-gated, 3086, Tocris Bioscience
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.