UCL 2077

Sub-type selective Kv channel effects; slow afterhyperpolarization (sAHP) channel blocker CAS# 918311-87-2

UCL 2077

Catalog No. BCC7446----Order now to get a substantial discount!

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Chemical structure

UCL 2077

3D structure

Chemical Properties of UCL 2077

Cas No. 918311-87-2 SDF Download SDF
PubChem ID 24868317 Appearance Powder
Formula C25H22N2 M.Wt 350.46
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO and to 25 mM in ethanol
Chemical Name 1,1,1-triphenyl-N-(pyridin-3-ylmethyl)methanamine
SMILES C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3)NCC4=CN=CC=C4
Standard InChIKey PQFNWDHABGBCHB-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H22N2/c1-4-12-22(13-5-1)25(23-14-6-2-7-15-23,24-16-8-3-9-17-24)27-20-21-11-10-18-26-19-21/h1-19,27H,20H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of UCL 2077

DescriptionSlow afterhyperpolarization (sAHP) channel blocker; reduces sAHP in hippocampal slice preparations. Displays no effect on Ca2+ currents or the time course of sAHP/sIAHP. Exhibits potent inhibition of KCNQ1 and KCNQ2, but differential effects at other KCNQs. Rescues memory retrieval in dopamine β-hydroxylase knockout mice.

UCL 2077 Dilution Calculator

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Preparing Stock Solutions of UCL 2077

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8534 mL 14.267 mL 28.5339 mL 57.0679 mL 71.3348 mL
5 mM 0.5707 mL 2.8534 mL 5.7068 mL 11.4136 mL 14.267 mL
10 mM 0.2853 mL 1.4267 mL 2.8534 mL 5.7068 mL 7.1335 mL
50 mM 0.0571 mL 0.2853 mL 0.5707 mL 1.1414 mL 1.4267 mL
100 mM 0.0285 mL 0.1427 mL 0.2853 mL 0.5707 mL 0.7133 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on UCL 2077

The slow afterhyperpolarization: a target of beta1-adrenergic signaling in hippocampus-dependent memory retrieval.[Pubmed:23486971]

J Neurosci. 2013 Mar 13;33(11):5006-16.

In rodents, adrenergic signaling by norepinephrine (NE) in the hippocampus is required for the retrieval of intermediate-term memory. NE promotes retrieval via the stimulation of beta1-adrenergic receptors, the production of cAMP, and the activation of both protein kinase A (PKA) and the exchange protein activated by cAMP. However, a final effector for this signaling pathway has not been identified. Among the many targets of adrenergic signaling in the hippocampus, the slow afterhyperpolarization (sAHP) is an appealing candidate because its reduction by beta1 signaling enhances excitatory neurotransmission. Here we report that reducing the sAHP is critical for the facilitation of retrieval by NE. Direct blockers of the sAHP, as well as blockers of the L-type voltage-dependent calcium influx that activates the sAHP, rescue retrieval in mutant mice lacking either NE or the beta1 receptor. Complementary to this, a facilitator of L-type calcium influx impairs retrieval in wild-type mice. In addition, we examined the role of NE in the learning-related reduction of the sAHP observed ex vivo in hippocampal slices. We find that this reduction in the sAHP depends on the induction of persistent PKA activity specifically in conditioned slices. Interestingly, this persistent PKA activity is induced by NE/beta1 signaling during slice preparation rather than during learning. These observations suggest that the reduction in the sAHP may not be present autonomously in vivo, but is likely induced by neuromodulatory input, which is consistent with the idea that NE is required in vivo for reduction of the sAHP during memory retrieval.

Enhancement of hippocampal pyramidal cell excitability by the novel selective slow-afterhyperpolarization channel blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077).[Pubmed:16877678]

Mol Pharmacol. 2006 Nov;70(5):1494-502.

The slow afterhyperpolarization (sAHP) in hippocampal neurons has been implicated in learning and memory. However, its precise role in cell excitability and central nervous system function has not been explicitly tested for 2 reasons: 1) there are, at present, no selective inhibitors that effectively reduce the underlying current in vivo or in intact in vitro tissue preparations, and 2) although it is known that a small conductance K(+) channel that activates after a rise in [Ca(2+)](i) underlies the sAHP, the exact molecular identity remains unknown. We show that 3-(triphenylmethylaminomethyl)pyridine (UCL2077), a novel compound, suppressed the sAHP present in hippocampal neurons in culture (IC(50) = 0.5 microM) and in the slice preparation (IC(50) approximately 10 microM). UCL2077 was selective, having minimal effects on Ca(2+) channels, action potentials, input resistance and the medium afterhyperpolarization. UCL2077 also had little effect on heterologously expressed small conductance Ca(2+)-activated K(+) (SK) channels. Moreover, UCL2077 and apamin, a selective SK channel blocker, affected spike firing in hippocampal neurons in different ways. These results provide further evidence that SK channels are unlikely to underlie the sAHP. This study also demonstrates that UCL2077, the most potent, selective sAHP blocker described so far, is a useful pharmacological tool for exploring the role of sAHP channels in the regulation of cell excitability in intact tissue preparations and, potentially, in vivo.

The specific slow afterhyperpolarization inhibitor UCL2077 is a subtype-selective blocker of the epilepsy associated KCNQ channels.[Pubmed:20843955]

Mol Pharmacol. 2010 Dec;78(6):1088-95.

Mutations in members of the KCNQ channel family underlie multiple diseases affecting the nervous and cardiovascular systems. Despite their clinical relevance, research into these channels is limited by the lack of subtype-selective inhibitors, making it difficult to differentiate the physiological function of each family member in vivo. We have proposed that KCNQ channels might partially underlie the calcium-activated slow afterhyperpolarization (sAHP), a neuronal conductance whose molecular components are uncertain. Here, we investigated whether 3-(triphenylmethylaminomethyl)pyridine (UCL2077), identified previously as an inhibitor of the sAHP in neurons, acts on members of the KCNQ family expressed in heterologous cells. We found that 3 muM UCL2077 strongly inhibits KCNQ1 and KCNQ2 channels and weakly blocks KCNQ4 channels in a voltage-independent manner. In contrast, UCL2077 potentiates KCNQ5 channels at more positive membrane potentials, with little effect at negative membrane potentials. We found that the effect of UCL2077 on KCNQ3 is bimodal: currents are enhanced at negative membrane potentials and inhibited at positive potentials. We found that UCL2077 facilitates KCNQ3 currents by inducing a leftward shift in the KCNQ3 voltage-dependence, a shift dependent on tryptophan 265. Finally, we show that UCL2077 has intermediate effects on KCNQ2/3 heteromeric channels compared with KCNQ2 and KCNQ3 homomers. Together, our data demonstrate that UCL2077 acts on KCNQ channels in a subtype-selective manner. This feature should make UCL2077 a useful tool for distinguishing KCNQ1 and KCNQ2 from less-sensitive KCNQ family members in neurons and cardiac cells in future studies.

Description

UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.

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