ML077 is a selective antagonist of the potassium-chloride co-transporter 2 (KCC2), with an IC50 of 537 nM for KCC2, while exhibiting minimal activity on KCC1 (IC50 > 50 μM). By inhibiting the chloride ion excretion function of KCC2, ML077 increases intracellular chloride concentrations, resulting in enhanced depolarization through chloride channels. This compound has demonstrated the ability to promote glucose-stimulated insulin secretion (GSIS) independent of KATP channels and is valuable for studying the physiological processes related to pain, epilepsy, and insulin secretion.
ML077 is a selective antagonist of the potassium-chloride co-transporter 2 (KCC2), with an IC50 of 537 nM for KCC2, while exhibiting minimal activity on KCC1 (IC50 > 50 μM). By inhibiting the chloride ion excretion function of KCC2, ML077 increases intracellular chloride concentrations, resulting in enhanced depolarization through chloride channels. This compound has demonstrated the ability to promote glucose-stimulated insulin secretion (GSIS) independent of KATP channels and is valuable for studying the physiological processes related to pain, epilepsy, and insulin secretion.
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