| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
UCL-1684 targets the apamin-sensitive Ca2+-activated K+ channel (KCa2.1/SK1) with an IC50 of 3 nM in rat sympathetic neurons. It is a potent and selective blocker of small-conductance calcium-activated potassium (SK or KCa2) channels. It also causes atrial-selective inhibition of sodium channel current (INa).
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| ln Vitro |
UCL 1684 (dibromide) (0.5 μM; HEK cells) modifies SS inactivation of cardiac sodium channels and causes direct atrial-selective inhibition of sodium channel current (INa). UCL 1684 (dibromide) at 0.5 μM lengthens the shortest S1-S1 gap, causes PRR, lowers V max, and increases DTE [1].
In vitro, UCL-1684 blocks KCa2.1 channels with an IC50 of 3 nM in rat sympathetic neurons. At 0.5 µM in HEK cells, it produces direct atrial-selective inhibition of sodium channel current (INa) and shifts steady-state inactivation of cardiac sodium channels. It is widely used in neurophysiological and cardiovascular research. |
| ln Vivo |
The duration of the Wenckbach cycle is extended to 115.0±5.1% of baseline with UCL 1684 (dibromide) (3 mg/kg; iv) [3].
In vivo, UCL-1684 is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. It causes atrial-selective prolongation of the effective refractory period (ERP) secondary to induction of postrepolarization refractoriness. It is used in cardiovascular research to study SK channel functions. |
| Enzyme Assay |
In vitro binding assays for UCL-1684 typically involve evaluating its affinity for SK channels using radioligand binding with apamin or other SK channel ligands. Membrane preparations from cells expressing SK channel subtypes are incubated with radiolabeled ligands and varying concentrations of the compound. IC50 values are calculated from displacement curves. Functional activity is assessed by patch-clamp electrophysiology.
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| Cell Assay |
Cell-based assays for UCL-1684 involve culturing cells expressing recombinant SK channel subtypes (e.g., HEK-293 cells). Cells are treated with UCL-1684 at concentrations ranging from 0.1 nM to 10 µM. Channel activity is measured by patch-clamp electrophysiology or fluorescence-based membrane potential assays. Selectivity is assessed by comparing effects at different SK channel subtypes and other ion channels.
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| Animal Protocol |
In vivo animal experiments for UCL-1684 typically involve administration to rodent or larger animal models via intravenous injection. Atrial fibrillation is induced by electrical pacing or other methods. The compound's ability to prevent or terminate atrial fibrillation is evaluated. Electrocardiogram (ECG) parameters are monitored. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues.
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| ADME/Pharmacokinetics |
UCL-1684 Br (molecular weight ~700-800) has moderate aqueous solubility. It is typically administered parenterally in research settings. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Its half-life supports its use in acute cardiovascular research studies.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for UCL-1684 Br from the search results. As an ion channel blocker, potential toxicity may include effects on cardiac conduction and neurological function. Comprehensive toxicological evaluation has likely been conducted in preclinical development. The compound is for research use only. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
See also: Ucl 1684 (note moved to).
UCL-1684 Br (CAS#: 199934-16-2) is a potent and selective SK channel blocker. It blocks KCa2.1 channels with an IC50 of 3 nM. It is effective in preventing atrial fibrillation. It causes atrial-selective inhibition of INa. It is a research tool for neurophysiological and cardiovascular studies. |
| Molecular Formula |
C34H30N4+2.2[BR-]
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|---|---|
| Molecular Weight |
654.4368
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| Exact Mass |
720.217
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| CAS # |
199934-16-2
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| PubChem CID |
9852584
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| Appearance |
White to off-white solid powder
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| LogP |
5.075
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
40
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| Complexity |
689
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C2=CC=C(CNC3=CC=[N+](CC4=CC=CC(=C4)C[N+]5=CC=C(N1)C6=CC=CC=C65)C7=CC=CC=C37)C=C2.[Br-].[Br-]
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| InChi Key |
KPNMQIKQVCWNTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H28N4.2BrH/c1-3-10-33-29(8-1)31-16-18-37(33)23-27-6-5-7-28(20-27)24-38-19-17-32(30-9-2-4-11-34(30)38)36-22-26-14-12-25(13-15-26)21-35-31;;/h1-20H,21-24H2;2*1H
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| Chemical Name |
17,24-diaza-1,9-diazoniaheptacyclo[23.6.2.29,16.219,22.13,7.010,15.026,31]octatriaconta-1(32),3(38),4,6,9(37),10,12,14,16(36),19,21,25(33),26,28,30,34-hexadecaene;dibromide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~7.6 mM; with ultrasonication and warming by heating to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 0.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5280 mL | 7.6401 mL | 15.2802 mL | |
| 5 mM | 0.3056 mL | 1.5280 mL | 3.0560 mL | |
| 10 mM | 0.1528 mL | 0.7640 mL | 1.5280 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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