| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
VU0240551 selectively inhibits the neuronal K-Cl cotransporter KCC2 (SLC12A5). It exhibits high selectivity for KCC2 over the closely related Na-K-2Cl cotransporter NKCC1 (IC50 > 50 µM). It binds competitively to the K+ site and noncompetitively to the Cl- site of KCC2. At higher concentrations, VU0240551 also inhibits L-type calcium channels, hERG potassium channels, and shows activity at adenosine A1 and A3 receptors.
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| ln Vitro |
In a concentration-dependent way, VU 0240551 decreases P cells' response to GABA; treatment at 75 and 100 μM significantly inhibits GABA-induced hyperpolarization, while 25 μM has no discernible impact [2].
In vitro, VU0240551 potently inhibits KCC2-mediated K+ uptake in KCC2-overexpressing HEK293 cells with an IC50 of 560–568 nM. At 1 µM, it decreases potassium ion uptake by 70% in KCC2-expressing HEK293 cells. It significantly inhibits KCC2-mediated K+ uptake at 10 µM and attenuates GABA-induced hyperpolarization in P cells, shifting the GABA reversal potential positively. In rat neocortical neurons, 1 µM VU0240551 reversibly prolongs the recovery time constant of IPSC amplitudes from 5.7 to 8.1 seconds. |
| ln Vivo |
In Eu rat cells, VU 0240551 (10 μM) greatly inhibits the influx of chloride ions, while it has no effect on SL rat cells [3].
In vivo, VU0240551 has been shown to reverse the attenuating effects of BDNF and 7,8-dihydroxyflavone on alcohol consumption after withdrawal in rats. It reverses the analgesic effect of HDAC2-targeting therapeutics in rat models of bone cancer pain. Intrathecal administration of VU0240551 reduces the effect of dexmedetomidine on SMIR-induced postsurgical pain rats. It can balance potassium currents in miR-137 knockout neurons and has been used to study spasticity and hyperreflexia after chronic spinal cord injury. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for VU0240551 typically measure its inhibition of KCC2-mediated ion transport. The standard assay involves measuring K+ (or Rb+) uptake in KCC2-overexpressing cells, where the compound's IC50 is determined by incubating cells with varying concentrations and measuring intracellular radioactive K+ uptake. Selectivity is assessed by comparing its activity against NKCC1 and other related transporters. Off-target profiling against a panel of receptors, ion channels, and transporters (e.g., 68 targets) is performed to characterize its selectivity.
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| Cell Assay |
In vitro cell-based experiments with VU0240551 are performed using various neuronal and non-neuronal cell models. For KCC2 function studies, KCC2-overexpressing HEK293 cells are commonly used. In neuronal cultures, the compound (typically 1–10 µM) is applied to study its effects on chloride homeostasis, GABAergic signaling, and neuronal excitability. Electrophysiological techniques such as patch-clamp recordings are used to measure changes in GABA reversal potential and ion flux.
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| Animal Protocol |
In vivo animal studies for VU0240551 typically involve administration via intraperitoneal (i.p.) or intrathecal (i.t.) injection in rodent models. For example, in alcohol consumption studies, it is injected i.p. to evaluate its effects on ethanol intake. In pain research, it is administered intrathecally to study its role in modulating pain pathways. Organotypic brain slice preparations are also used to study its effects on neuronal migration and epileptiform activity.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic data for VU0240551 is limited in the public domain. The compound has a molecular weight of 342.44 g/mol and is typically prepared as stock solutions in DMSO (soluble at >20 mg/mL, or 25 mg/mL) for in vitro and in vivo experiments. For optimal stability, it should be stored as a solid at -20°C for long-term storage or at 2-8°C for short-term storage.
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| Toxicity/Toxicokinetics |
The toxicological profile of VU0240551 has not been extensively characterized in the literature. As a potent research compound, it is considered hazardous and contains a pharmaceutically active ingredient. Handling should only be performed by trained personnel. Under fire conditions, it may decompose and emit toxic fumes. It has been shown to induce ferroptosis in cancer cells. VU0240551 is not for human or veterinary use.
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| References |
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| Additional Infomation |
N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide is a pyridazine compound and a cyclic compound.
VU0240551 (also known as VU-0240551) is a prototypical KCC2 antagonist and serves as the benchmark tool compound against which newer-generation KCC2 modulators are measured. It is the only small molecule with specificity for a KCC family member. Its primary research applications include studying the role of KCC2 in epilepsy, neuropathic pain, spasticity, alcohol use disorders, and neuronal development. It is not approved for clinical use and is intended for laboratory research purposes only. |
| Molecular Formula |
C16H14N4OS2
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|---|---|
| Molecular Weight |
342.43856
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| Exact Mass |
342.061
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| CAS # |
893990-34-6
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| PubChem CID |
7211972
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| Appearance |
White to off-white solid powder
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| LogP |
4.288
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WJRWSLORVIHRNX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N4OS2/c1-11-9-23-16(17-11)18-14(21)10-22-15-8-7-13(19-20-15)12-5-3-2-4-6-12/h2-9H,10H2,1H3,(H,17,18,21)
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| Chemical Name |
N-(4-methyl-1,3-thiazol-2-yl)-2-(6-phenylpyridazin-3-yl)sulfanylacetamide
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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) |
DMSO : ≥ 50 mg/mL (~146.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: 2.5 mg/mL (7.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9202 mL | 14.6011 mL | 29.2022 mL | |
| 5 mM | 0.5840 mL | 2.9202 mL | 5.8404 mL | |
| 10 mM | 0.2920 mL | 1.4601 mL | 2.9202 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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