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UK 78282 hydrochloride
Blocker of the KV1.3 and KV1.4 voltage-gated potassium channels in T lymphocytes (IC50 values are 0.28 and 0.17 μM respectively). Suppresses T lymphocyte mitogenesis; leads to membrane depolarization. Also blocks KV1.4 expressed in heart and brain.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 466.05. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.29 mL||21.46 mL||42.91 mL|
|2.5 mM||0.86 mL||4.29 mL||8.58 mL|
|5 mM||0.43 mL||2.15 mL||4.29 mL|
|25 mM||0.09 mL||0.43 mL||0.86 mL|
References are publications that support the biological activity of the product.
Hanson et al (1999) UK-78,282, a novel piperidine compound that potently blocks the Kv1.3 voltage-gated potassium channel and inhibits human T cell activation. Br.J.Pharmacol. 126 1707 PMID: 10372812
Chandy et al (2001) Potassium channels in T lymphocytes: toxins to therapeutic immunosuppressants. Toxicon 39 1269 PMID: 11384714
Chandy et al (2004) K+ channels as targets for specific immunomodulation. Trends.Pharmacol.Sci. 25 280 PMID: 15120495
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Citations for UK 78282 hydrochloride
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Reviews for UK 78282 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Voltage gated Kv channel blocking can be assessed under lab conditions with this product. UK 78782 is an excellent compound to get an understanding of channel blocking of different kind of Kv channel. Was dissolved in ethanol and easy to carry out HPLC on.
Literature in this Area
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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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.