VU 0240551 |
| Katalog-Nr.GC37927 |
VU 0240551 ist ein potenter Inhibitor des neuronalen K-Cl-Cotransporters KCC2 (IC50=560 nM) und ist selektiv gegenÜber NKCC1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 893990-34-6
Sample solution is provided at 25 µL, 10mM.
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VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).IC50 value: 560 nM [1]Target: K-Cl cotransporter(KCC2)VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. VU 0240551 also inhibits hERG and L-type Ca2+ channels [1]. Herein we report the discovery and SAR of an improved novel antagonist (VU0463271) of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC(50) 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 [2].
[1]. Delpire E, et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. [2]. 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.
| Cas No. | 893990-34-6 | SDF | |
| Canonical SMILES | O=C(CSC1=NN=C(C2=CC=CC=C2)C=C1)NC3=NC(C)=CS3 | ||
| Formula | C16H14N4OS2 | M.Wt | 342.44 |
| Löslichkeit | DMSO: ≥ 50 mg/mL (146.01 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9202 mL | 14.6011 mL | 29.2022 mL |
| 5 mM | 584 μL | 2.9202 mL | 5.8404 mL |
| 10 mM | 292 μL | 1.4601 mL | 2.9202 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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