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| ln Vitro |
With an IC50 of 61 nM and higher selectivity than the closely related Na-K-2Cl cotransporter 1 (NKCC1) > 100-fold, VU0463271 is a strong antagonist of neuron-specific potassium chloride cotransporter 2 (KCC2). It also exhibits superior selectivity across a broader range of GPCRs, ion channels, and transporters. Additionally, it has been discovered to be quickly removed in vitro [1]. When VU0463271 was applied to transected CNS preparations, 1 μM VU0463271 significantly increased the Drosophila CNS firing rate, leading to peak firing rates for the OR and rdl strains that were 2.5 and 2.7 times higher than baseline firing rates, respectively [2]. VU0463271 (10-100 nM) decreases the frequency of firing in the central nervous system by about 20% in a small fraction of formulations [2].
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| ln Vivo |
VU0463271 had a low volume of distribution at steady state (Vss 0.4 L/kg) and a moderate to high clearance rate, which together result in a relatively short half-life (t1/2) of 9 minutes in the body after intravenous administration (1 mg/kg) of the compound in rats (CL=57 mL/min/kg) [1].
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| References |
[1]. Delpire E, et al. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4532-5.
[2]. Rui Chen, et al. Functional Coupling of K +-Cl - Cotransporter (KCC) to GABA-Gated Cl - Channels in the Central Nervous System of Drosophila melanogaster Leads to Altered Drug Sensitivities. ACS Chem Neurosci. 2019 Jun 19;10(6):2765-2776. |
| Molecular Formula |
C19H18N4OS2
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|---|---|
| Molecular Weight |
382.5
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| Exact Mass |
382.0922
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| CAS # |
1391737-01-1
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| Related CAS # |
VU0463271 quarterhydrate
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| SMILES |
S1C=C(C)N=C1N(C(CSC1=CC=C(C2C=CC=CC=2)N=N1)=O)C1CC1
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| Synonyms |
VU 0463271; VU-0463271; VU0463271
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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 : ~25 mg/mL (~65.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6144 mL | 13.0719 mL | 26.1438 mL | |
| 5 mM | 0.5229 mL | 2.6144 mL | 5.2288 mL | |
| 10 mM | 0.2614 mL | 1.3072 mL | 2.6144 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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