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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- CAS No.: 1135304-61-8
- 화학식: C17H16N4OS2
- 분자량:356.47
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Endogenous Metabolite Isoforms
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Biological Activity
제품 설명
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>50 μM
Compound: 2, VU0255011, ML077
|
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
|
[PMID: 22727639] |
| HEK293 | IC50 |
537 nM
Compound: 2, VU0255011, ML077
|
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
|
[PMID: 22727639] |
Chemical Information
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CAS No. 1135304-61-8
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Appearance Solid
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분자량 356.47
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화학식 C17H16N4OS2
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Color White to light yellow
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
순도&문서
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Data Sheet (267 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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)