2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. NKCC Endogenous Metabolite
  4. 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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ML077

ML077 Chemical Structure

CAS No. : 1135304-61-8

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Description

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[1][2].

Cellular Effect
Cell Line Type Value Description References
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]
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]
Molecular Weight

356.47

Formula

C17H16N4OS2
CAS No.
SMILES

O=C(N(C)C1=NC(C)=CS1)CSC2=NN=C(C3=CC=CC=C3)C=C2
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ML077 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML0771135304-61-8ML 077ML-077NKCCEndogenous MetaboliteNa-K-Cl cotransporterNa(+)-K(+)-Cl(-) cotransporterNa+-K+-Cl− cotransporterPotassium-chlorideco-transporter 2KCC2NKCC1antagonistInhibitorinhibitorinhibit

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