A-77636

Name: A-77636
Brand: TargetMol
SKU: T78644
Rating: 4.5 (1 reviews)

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Catalog No. T78644Cas No. 778546-51-3

A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1].

A-77636

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Catalog No. T78644Cas No. 778546-51-3

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1].
Targets&IC50	D1 receptor:1.1 nM (EC50), D1 receptor:39.8 nM (Ki)
In vivo	A-77636 (0-3.2 μmol/kg, subcutaneous injection) induced rotational behavior in rats with 6-OHDA lesions (ED50 = 0.32 μmol/kg sc) [1], attenuated drug-induced locomotor activity in a dose-dependent manner (1-10 mg/kg) [2], and elicited forelimb clonus in rats (ED50 = 12.3 μmol/kg s.c.) and mice (ED50 = 12.1 μmol/kg s.c.) [1]. In MPTP-treated marmosets, A-77636 (0.5, 1.0, or 2.0 μmol/kg, oral administration) increased motor activity and reduced Parkinsonian symptoms, demonstrating efficacy with both subcutaneous and oral administration [1].

Chemical Properties

Molecular Weight	329.43
Formula	C₂₀H₂₇NO₃
Cas No.	778546-51-3
Smiles	C(N)[C@@H]1O[C@H]([C@]23CC4(CC(C2)(CC(C3)(C4)[H])[H])[H])CC=5C1=CC=C(O)C5O

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc