Cat. No. 1310
Chemical Name: 6,12,19,20,25,26-Hexahydro-5,27:13,
Biological ActivityHighly potent, non-peptidic blocker of the apamin-sensitive Ca2+-activated K+ channel (KCa2.1) (IC50 = 3 nM in rat sympathetic neurons). Blocks hKCa2.1 and rKCa2.2 channels expressed in HEK 293 cells with IC50 values of 762 and 364 pM respectively.
Licensing InformationSold with the permission of University College, London
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.
Certificate of Analysis / Safety Data Sheet
Campos Rosa et al (2000) Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca2+-activated K+ channel. J.Med.Chem. 43 420. PMID: 10669569.
Malik-Hall et al (2000) Compounds that block intermediate-conductance (IKCa) and small-conductance (SKCa) calcium-activated potassium channels. Br.J.Pharmacol. 129 1431. PMID: 10742299.
Strobaek et al (2000) Pharmacological characterization of small-conductance Ca2+-activated K+ channels stably expressed in HEK 293 cells. Br.J.Pharmacol. 129 991. PMID: 10696100.
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Citations are publications that use Tocris products. Selected citations for UCL 1684 include:
Abdulkareem et al (2016) Knockdown of the small conductance Ca(2+) -activated K(+) channels is potently cytotoxic in breast cancer cell lines. Heart Rhythm 173 177. PMID: 26454020.
Chien and Su (2015) 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts. J Biol Chem 22 42. PMID: 26076928.
Kurahashi et al (2014) Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles. Am J Physiol Cell Physiol 307 C561. PMID: 25055825.
Alpert and Alford (2013) Synaptic NMDA receptor-dependent Ca2+ entry drives membrane potential and Ca2+ oscillations in spinal ventral horn neurons. PLoS One 8 e63154. PMID: 23646190.
Benton et al (2013) Iberiotoxin-sensitive and -insensitive BK currents in Purkinje neuron somata. J Neurophysiol 109 2528. PMID: 23446695.
Hsueh et al (2013) Proarrhythmic effect of blocking the small conductance calcium activated potassium channel in isolated canine left atrium. J Biomed Sci 10 891. PMID: 23376397.
Geier et al (2011) Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol 300 C937. PMID: 21228322.
Hilgers et al (2010) Twenty-four-hour exposure to altered blood flow modifies endothelial Ca2+-activated K+ channels in rat mesenteric arteries. J Pharmacol Exp Ther 333 210. PMID: 20040579.
Lamy et al (2010) Allosteric block of KCa2 channels by apamin. PLoS One 285 27067. PMID: 20562108.
Giachini et al (2009) Upregulation of intermediate calcium-activated potassium channels counterbalance the impaired endothelium-dependent vasodilation in stroke-prone spontaneously hypertensive rats. Transl Res 154 183. PMID: 19766962.
Szollosi et al (2007) Glucose stimulates Ca2+ influx and insulin secretion in 2-week-old β-cells lacking ATP-sensitive K+ channels. Br J Pharmacol 282 1747. PMID: 17138557.
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Keywords: UCL 1684, supplier, potent, blockers, SKCa, Potassium, Channels, K+, ca2+-activated, ca2+-dependent, SK1, SK2, UCL1684, Tocris Bioscience, Calcium-Activated Potassium (KCa) Channel Blocker products
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