ML077
ML007 is a selective antagonist targeting the neuron-specific potassium-chloride co-transporter 2 (KCC2) with an IC50 for KCC2 is 537 nM, while its inhibitory activity on KCC1 is extremely weak (IC50 > 50 μM). ML077 inhibits the chloride ion excretion function of KCC2, increasing the intracellular chloride ion concentration, thereby enhancing the depolarization mediated by chloride ion channels. ML007 can promote glucose-stimulated insulin secretion (GSIS) without relying on KATP channels. ML007 can be used to study the functions related to pain, epilepsy, and insulin secretion.
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- No. CAS: 1135304-61-8
- Fòrmula: C17H16N4OS2
- Peso molecular:356.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Ver todos los productos específicos de isoformas Endogenous Metabolite
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>50 μM
Compound: 2, VU0255011, ML077
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Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting
Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting
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[PMID: 22727639] |
| HEK293 | IC50 |
537 nM
Compound: 2, VU0255011, ML077
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Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis
Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis
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[PMID: 22727639] |
Chemical Information
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No. CAS 1135304-61-8
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Peso molecular 356.47
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Fòrmula C17H16N4OS2
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SMILES
O=C(N(C)C1=NC(C)=CS1)CSC2=NN=C(C3=CC=CC=C3)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ML077 Related Classifications
HY-115606 Related Classifications
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