2. GPCR/G Protein Neuronal Signaling Cell Cycle/DNA Damage
  3. Dopamine Receptor PERK
  4. MLS6357

MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.

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MLS6357

MLS6357 Chemical Structure

CAS No. : 932544-59-7

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MLS6357 Related Antibodies

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Description

MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder[1].

IC50 & Target[1]

Dopamine D3 receptor

13 μM (IC50)

Dopamine D1 receptor

 

Dopamine D2 receptor

 

Dopamine D4 receptor

 

Dopamine D5 receptor

 

In Vitro

MLS6357 fully antagonizes the attenuation of cAMP accumulation induced by an EC80 concentration of Dopamine (HY-B0451) with an IC50 of 4.5 μM and D3R-stimulation of ERK1/2 phosphorylation (pERK) with an IC50 of 5.6 μM in HEK293 cells[1].
MLS6357 exhibits moderate microsomal stability in human liver microsome (CLint = 51 μL/min/mg; t1/2 = 13.6 min)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MLS6357 Related Antibodies
Molecular Weight

395.90

Formula

C18H22ClN3O3S
CAS No.
SMILES

O=C(C1=C(NC(C)=C1S(NC2=CC(Cl)=C(C=C2)C)(=O)=O)C)N3CCCC3
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
References
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MLS6357 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:

MLS6357932544-59-7MLS 6357MLS-6357Dopamine ReceptorPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasePositive Allosteric Modulator-Antagonistβ-Arrestin RecruitmentPharmacokineticStructure-Activity RelationshipInhibitorinhibitorinhibit

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