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[1][2].

Product Specifications

CAS Number

[1135304-61-8]

UNSPSC

12352005

Target

Endogenous Metabolite; NKCC

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C(N(C)C1=NC(C)=CS1)CSC2=NN=C(C3=CC=CC=C3)C=C2

Molecular Formula

C17H16N4OS2

Molecular Weight

356.47

References & Citations

[1]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. |[2]Kursan S, McMillen TS, Beesetty P, Dias-Junior E, Almutairi MM, Sajib AA, Kozak JA, Aguilar-Bryan L, Di Fulvio M. The neuronal K+Cl- co-transporter 2 (Slc12a5) modulates insulin secretion. Sci Rep. 2017 May 11;7 (1) :1732. doi: 10.1038/s41598-017-01814-0. PMID: 28496181; PMCID: PMC5431760.