497926-94-0
Chemical Structure
KM822
- CAS. Nr.: 497926-94-0
- Formula:C21H22N6O3S2
- Molecular Weight:470.57
IUPAC Name: N-(4-(N-(2-((8-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)ethyl)sulfamoyl)phenyl)acetamide
InChIKey: NYMDWVPBMFMAQC-UHFFFAOYSA-N
SMILES: O=C(C)NC1=CC=C(S(=O)(NCCSC2=NC3=C(C(C=C(CC)C=C4)=C4N3)N=N2)=O)C=C1
Biological Activity: KM822 is a dopamine transporter (DAT) inhibitor with an IC50 of 2.2 μM against hDAT and an IC50 of 10.4 μM against C. elegans DAT-1. KM822 binds to the allosteric A2 site in the extracellular vestibule of outward-facing DAT, reduces the affinity of psychostimulants and phenethylamine psychostimulants for DAT, and inhibits dopamine transport function. KM822 attenuates the behaviors induced by psychostimulants and phenethylamine psychostimulants in planarians and C. elegans, does not induce locomotor effects on its own, and exhibits specificity for DAT. KM822 can serve as a molecular probe for investigating the allosteric regulation of DAT function. KM822 is applicable to studies related to psychostimulant use disorders[1][2][3][4].
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KM822 | KM822 is a dopamine transporter (DAT) inhibitor with an IC50 of 2.2 μM against hDAT and an IC50 of 10.4 μM against C. elegans DAT-1. KM822 binds to the allosteric A2 site in the extracellular vestibule of outward-facing DAT, reduces the affinity of psychostimulants and phenethylamine psychostimulants for DAT, and inhibits dopamine transport function. KM822 attenuates the behaviors induced by psychostimulants and phenethylamine psychostimulants in planarians and C. elegans, does not induce locomotor effects on its own, and exhibits specificity for DAT. KM822 can serve as a molecular probe for investigating the allosteric regulation of DAT function. KM822 is applicable to studies related to psychostimulant use disorders. | |||||||||||||||||||||
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- [1]. Nguyen H, et al. Allosteric modulation of serotonin and dopamine transporters: New insights from computations and experiments. Current research in physiology. 2024;7:100125. [Content Brief]
- [2]. Aggarwal S, et al. Identification of a Novel Allosteric Modulator of the Human Dopamine Transporter. ACS chemical neuroscience. 2019 Aug 21;10(8):3718-3730. [Content Brief]
- [3]. Refai O, et al. Allosteric Modulator KM822 Attenuates Behavioral Actions of Amphetamine in Caenorhabditis elegans through Interactions with the Dopamine Transporter DAT-1. Mol Pharmacol. 2022 Mar;101(3):123-131. [Content Brief]
- [4]. Aggarwal S, et al. Functional Characterization of the Dopaminergic Psychostimulant Sydnocarb as an Allosteric Modulator of the Human Dopamine Transporter. Biomedicines. 2021 Jun 02;9(6):634. [Content Brief]
Keywords
