| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
VU0405601 targets the human Ether-à-go-go-Related Gene (hERG) encoded Kv11.1 potassium channel. As a hERG agonist and positive allosteric modulator, it enhances hERG channel activity. It increases the IC50 of dofetilide from 38.7 to 76.3 nM and mitigates the effects of hERG blockers primarily by reducing inactivation.
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| ln Vitro |
Thirty minutes before administering 100 nm dofetilide, VU0405601 (5 µM) shields cardiac tissue from the ventricular tachycardia caused by dofetilide [2]. As a hERG agonist, VU0405601 (50 µM) raises test pulse and tail currents, which raises dofetilide's IC50 value from 38.7 nm to 76.3 nm [2].
In vitro, VU0405601 is a potent Kv11.1 (hERG) channel activator. At 5 µM (pretreated for 30 min before 100 nM dofetilide), it protects cardiac tissue from dofetilide-induced ventricular tachycardia. It increases the IC50 of dofetilide from 38.7 to 76.3 nM. |
| ln Vivo |
In vivo activity data for VU0405601 are limited in the available literature. As a hERG agonist, it has been reported to protect cardiac tissue from dofetilide-induced ventricular tachycardia. Its ability to reduce the sensitivity of hERG to inhibitors suggests potential for preventing drug-induced arrhythmias.
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| Enzyme Assay |
In vitro channel binding/activation assays for VU0405601 are performed using cells expressing hERG channels. Channel activity is measured using electrophysiological techniques such as patch-clamp recordings. The compound is applied to cells, and the enhancement of hERG current amplitude is measured. The EC50 for channel activation is calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for VU0405601 are performed using cells expressing hERG channels or cardiac tissue preparations. Cells are treated with the compound, and hERG channel activity is measured using electrophysiological techniques. The compound's ability to protect against hERG blocker-induced current reduction is assessed by co-application with inhibitors such as dofetilide.
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| Animal Protocol |
In vivo animal experiments for VU0405601 are conducted in animal models of drug-induced arrhythmias. A typical protocol involves administration of the compound prior to challenge with a hERG-blocking agent such as dofetilide. Cardiac function is monitored by electrocardiography (ECG) to assess protection against ventricular tachycardia and other arrhythmias.
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| ADME/Pharmacokinetics |
VU0405601 has a molecular weight of 357.20 and molecular formula C₁₇H₁₃BrN₂O₂. It has a purity of ≥98% (HPLC) and 99.93%. It is a small-molecule activator of the Kv11.1 (hERG) potassium channel. It should be stored appropriately to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological data for VU0405601 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Egly CL, et al. A High-Throughput Screening Assay to Identify Drugs that Can Treat Long QT Syndrome Caused by Trafficking-Deficient KV11.1 (hERG) Variants. Mol Pharmacol. 2022 Apr;101(4):236-245.
[2]. Potet F, et al. Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias. J Biol Chem. 2012 Nov 16;287(47):39613-25. |
| Additional Infomation |
VU0405601 is a potent pharmacological activator and positive allosteric modulator of the hERG/Kv11.1 potassium channel. It protects cardiac tissue from hERG-related drug-induced arrhythmias and ventricular tachycardia. This product is for research use only.
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| Molecular Formula |
C17H13N2O2BR
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|---|---|
| Molecular Weight |
357.201
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| Exact Mass |
356.016
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| CAS # |
712325-30-9
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| PubChem CID |
1301094
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
584.8±35.0 °C at 760 mmHg
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| Flash Point |
307.5±25.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.698
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| LogP |
3.71
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
380
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=CN=C1)COC2=CC=C3C=CC=CC3=C2Br
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| InChi Key |
WLLRAGBPCSOJNH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13BrN2O2/c18-17-14-6-2-1-4-12(14)7-8-15(17)22-11-16(21)20-13-5-3-9-19-10-13/h1-10H,11H2,(H,20,21)
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| Chemical Name |
2-(1-bromonaphthalen-2-yl)oxy-N-pyridin-3-ylacetamide
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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 | 2.7996 mL | 13.9978 mL | 27.9955 mL | |
| 5 mM | 0.5599 mL | 2.7996 mL | 5.5991 mL | |
| 10 mM | 0.2800 mL | 1.3998 mL | 2.7996 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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