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Referencia número: HY-123828

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MLS6585

MLS6585 is a selective D1 dopamine receptor (D1R) positive allosteric modulator that enhances Dopamine (HY-B0451)-stimulated G protein/β-arrestin signaling and affinity without intrinsic D1R agonist activity. MLS6585 is inactive at D2R, D3R, D4R, and β2-adrenergic receptors. MLS6585 partially restores signaling of loss-of-function DRD1 variants and enhances responses to multiple agonists.

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No. CAS: 389080-71-1
Fòrmula: C₁₉H₂₃N₃O₂S
Peso molecular:357.47

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MLS6585 Chemical Structure

No. CAS: 389080-71-1

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Use of MCE Products

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

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^[1]

D₁ Receptor

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In Vitro

MLS6585 (50 µM; 90 min) is a low-micromolar-affinity orthosteric allosteric modulator of D1R in HEK293-D1R membranes, which increases dopamine affinity by approximately 7-fold and inhibits [³H]-SCH23390 binding by about 66% at 50 µM^[1].
MLS6585 (0.1-100 µM; 90 min) is a positive allosteric modulator of dopamine-stimulated β-arrestin recruitment in CHO-K1 D1R cells, enhancing dopamine potency by approximately 7-8 fold and displaying low micromolar affinity (K_b 5.4 µM)^[1].
MLS6585 (50 µM) enhances dopamine-induced D1R internalization in U2OS cells, increasing dopamine potency by 6-fold without increasing maximal internalization^[1].
MLS6585 increases DA affinity at D1R in radioligand binding assays^[4].

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

Chemical Information

No. CAS 389080-71-1
Peso molecular 357.47
Fòrmula C₁₉H₂₃N₃O₂S
SMILES

O=C(N)C1=C(SC2=C1CCC(C2)C(C)(C)C)NC(=O)C=3C=CN=CC3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Luderman KD, et al. Identification of Positive Allosteric Modulators of the D Dopamine Receptor That Act at Diverse Binding Sites. Molecular pharmacology. 2018 Oct;94(4):1197-1209. [Content Brief]

[2]. Wu C, et al. Pharmacological Characterization of Dopamine Receptor DRD1 Variants and Exploration of Their Allosteric Activation. Biochemistry. 2025 May 20;64(10):2200-2211.

[3]. Labouesse MA, et al. A chemogenetic approach for dopamine imaging with tunable sensitivity. Nature communications. 2024 Jul 02;15(1):5551.

[4]. Hanson J N, et al. Characterization of the Binding Pocket for a Novel Positive Allosteric Modulator of the D1 Dopamine Receptor[J]. The Journal of Pharmacology and Experimental Therapeutics, 2024, 389: 344.

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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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MLS6585

Ver todos los productos específicos de isoformas Dopamine Receptor

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