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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- Pureté: 99.34%
- CAS No.: 107756-30-9
- Formule: C14H20BrN3O3S
- Masse moléculaire:390.30
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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α1A-adrenergic receptor |
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.
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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CAS No. 107756-30-9
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Appearance Solid
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Masse moléculaire 390.30
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
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)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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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