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VU0463271
🥰Excellent
Catalog No. T17243Cas No. 1391737-01-1
Alias N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective 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.
VU0463271
🥰Excellent
Purity: 99.75%
Catalog No. T17243Alias N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamideCas No. 1391737-01-1
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective 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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $43 | In Stock | |
| 10 mg | $73 | In Stock | |
| 25 mg | $163 | In Stock | |
| 50 mg | $263 | In Stock | |
| 100 mg | $389 | In Stock | |
| 200 mg | $553 | In Stock |
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Purity:99.75%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective 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. |
| Targets&IC50 | KCC2:61 nM |
| In vitro | VU0463271 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]. |
| In vivo | VU0463271(1 mg/kg; i.v.) is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg). The low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo[ |
| Alias | N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
| Molecular Weight | 382.5 |
| Formula | C19H18N4OS2 |
| Cas No. | 1391737-01-1 |
| Smiles | Cc1csc(n1)N(C1CC1)C(=O)CSc1ccc(nn1)-c1ccccc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.83 mg/mL (10 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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