A-61603
Based on 1 Customer Validation
A-61603 is a selective α1A/α1a-adrenergic receptor agonist with Ki of 8.89 nM for rat submaxillary gland α1A, Ki of 30.5 nM for cloned bovine α1a. A-61603 potentiates Ca2+ transients with EC50 of 6.9 nM. A-61603 stimulates phosphoinositide hydrolysis, induces contractile responses in vas deferens, prostate strips, and spleen strips, and exhibits low activity in aortic rings. A-61603 can be used for research on adrenergic function.
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- Pureza : 99.34%
- No. CAS: 107756-30-9
- Fòrmula: C14H20BrN3O3S
- Peso molecular:390.30
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
α1A-adrenergic receptor |
In Vitro
A-61603 (60-120 min) potently binds α1A/a adrenergic receptors (Ki = 8.89 nM for rat submaxillary gland α1A, Ki = 30.5 nM for cloned bovine α1a) with 35- to 150-fold selectivity over α1b, α1d, and α2 adrenoceptors[1].
A-61603 (60 min) potently stimulates phosphoinositide hydrolysis in mouse fibroblast LTK− cells transfected with bovine α1a receptors (EC50 = 14.5 nM), with minimal activity in cells transfected with hamster α1b or rat α1d receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
A-61603 (0.01-0.1 µg/kg; i.v.) is an 88-fold more potent pressor agent than Phenylephrine (HY-B0769) in conscious rats, with activity mediated primarily by α1A/a receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle dogs (male, aged >2 yr, anesthetized with isoflurane)[1]
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Dosage:0.01 µg/kg; 0.1 µg/kg
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Administration:i.v.
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Result:Increased intraurethral pressure to a greater extent than mean arterial blood pressure.
Was more potent than epinephrine at elevating intraurethral pressure, and nearly equipotent to epinephrine at elevating mean arterial blood pressure.
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Animal Model:Rats[1]
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Dosage:0.01 µg/kg; 0.03 µg/kg; 0.06 µg/kg; 0.1 µg/kg
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Administration:i.v.
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Result:Induced a pressor response at doses 50- to 100-fold lower than phenylephrine.
Required a dose of 0.05 µg/kg i.v. to increase mean arterial blood pressure by 30 mmHg, making it 88-fold more potent than phenylephrine (4.4 µg/kg i.v.).
Showed pressor response not attenuated by chloroethylclonidine pretreatment, but shifted 100-fold by YM-617 pretreatment.
Chemical Information
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No. CAS 107756-30-9
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Appearance Solid
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Peso molecular 390.30
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Fòrmula C14H20BrN3O3S
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Color White to off-white
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SMILES
CS(=O)(NC1=C2CCCC(C3=NCCN3)C2=CC=C1O)=O.Br
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
H2O : 50 mg/mL (128.11 mM; Need ultrasonic)
DMSO : 20 mg/mL (51.24 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Knepper SM, et al. A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype. J Pharmacol Exp Ther. 1995 Jul;274(1):97-103. [Content Brief]
[2]. Luo DL, et al. Receptor subtype involved in alpha 1-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta Pharmacol Sin. 2007 Jul;28(7):968-74. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.5621 mL | 12.8107 mL | 25.6213 mL | 64.0533 mL |
| 5 mM | 0.5124 mL | 2.5621 mL | 5.1243 mL | 12.8107 mL | |
| 10 mM | 0.2562 mL | 1.2811 mL | 2.5621 mL | 6.4053 mL | |
| 15 mM | 0.1708 mL | 0.8540 mL | 1.7081 mL | 4.2702 mL | |
| 20 mM | 0.1281 mL | 0.6405 mL | 1.2811 mL | 3.2027 mL | |
| 25 mM | 0.1025 mL | 0.5124 mL | 1.0249 mL | 2.5621 mL | |
| 30 mM | 0.0854 mL | 0.4270 mL | 0.8540 mL | 2.1351 mL | |
| 40 mM | 0.0641 mL | 0.3203 mL | 0.6405 mL | 1.6013 mL | |
| 50 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.2811 mL | |
| H2O | 60 mM | 0.0427 mL | 0.2135 mL | 0.4270 mL | 1.0676 mL |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3203 mL | 0.8007 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6405 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
A-61603 Related Classifications
HY-101366 Related Classifications
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