| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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