1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. A-61603

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.

For research use only. We do not sell to patients.

A-61603

A-61603 Chemical Structure

CAS No. : 107756-30-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

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.

In Vivo

A-61603 (0.01-0.1 µg/kg; i.v.) potently elevates intraurethral prostatic tone to a greater degree than mean arterial blood pressure in anesthetized male Beagle dogs[1].
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.

Animal Model: Beagle dogs (male, aged >2 yr, anesthetized with isoflurane)[1]
Dosage: 0.01 µg/kg; 0.1 µg/kg
Administration: i.v.
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.
Animal Model: Rats[1]
Dosage: 0.01 µg/kg; 0.03 µg/kg; 0.06 µg/kg; 0.1 µg/kg
Administration: i.v.
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.
Molecular Weight

390.30

Formula

C14H20BrN3O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(NC1=C2CCCC(C3=NCCN3)C2=CC=C1O)=O.Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5621 mL 12.8107 mL 25.6213 mL
5 mM 0.5124 mL 2.5621 mL 5.1243 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.34%

References

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.

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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.

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A-61603
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HY-101366
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