VU0463271 quarterhydrate
VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC50 of 61 nM.
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- Formule: C19H18N4OS2.1/4H2O
- Masse moléculaire:387.00
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 61 nM (KCC2)[1].
VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters. It is also found rapidly cleared in vitro[1].
VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively[2].
VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within a
small percentage of preparations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 387.00
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Formule C19H18N4OS2.1/4H2O
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Color Light yellow to yellow
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SMILES
O=C(N(C1CC1)C2=NC(C)=CS2)CSC3=NN=C(C4=CC=CC=C4)C=C3.[1/4].O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 19 mg/mL (49.10 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5840 mL | 12.9199 mL | 25.8398 mL | 64.5995 mL |
| 5 mM | 0.5168 mL | 2.5840 mL | 5.1680 mL | 12.9199 mL | |
| 10 mM | 0.2584 mL | 1.2920 mL | 2.5840 mL | 6.4599 mL | |
| 15 mM | 0.1723 mL | 0.8613 mL | 1.7227 mL | 4.3066 mL | |
| 20 mM | 0.1292 mL | 0.6460 mL | 1.2920 mL | 3.2300 mL | |
| 25 mM | 0.1034 mL | 0.5168 mL | 1.0336 mL | 2.5840 mL | |
| 30 mM | 0.0861 mL | 0.4307 mL | 0.8613 mL | 2.1533 mL | |
| 40 mM | 0.0646 mL | 0.3230 mL | 0.6460 mL | 1.6150 mL |
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