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Cat. No.: HY-115606

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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.

For research use only. We do not sell to patients.

CAS No.: 1135304-61-8
Formula: C₁₇H₁₆N₄OS₂
Molecular Weight:356.47

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

ML077 Chemical Structure

CAS No.: 1135304-61-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
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- Cellular Effect
Chemical Information
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Biological Activity

Description

All Endogenous Metabolite Isoforms :

Cellular Effect

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

CAS No. 1135304-61-8
Molecular Weight 356.47
Formula C₁₇H₁₆N₄OS₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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Purity & Documentation
References

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ML077

All Endogenous Metabolite Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ML077 Related Classifications

HY-115606 Related Classifications