2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. RS 17053 hydrochloride

RS 17053 hydrochloride  (Synonyms: RS-17053)

Cat. No.: HY-101336 Purity: 99.70%
SDS COA Handling Instructions

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RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

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

RS 17053 hydrochloride Chemical Structure

RS 17053 hydrochloride Chemical Structure

CAS No. : 169505-93-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

RS 17053 hydrochloride Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

IC50 & Target

pKi: 9.1 (α1A adrenoceptor in native cell membrane)
pA2: 9.8 (α1A adrenoceptor)[1].
In Vitro

In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8). However, in isolated smooth muscle preparations from human LUT tissues, RS 17053 hydrochloride antagonizes responses to NE only at high concentrations. Estimates of affinity (pA2) at α1-adrenoceptors mediating NE-induced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin), 6.9 in anterior fibromuscular stroma (prazosin, 8.9), and 7.1 in bladder neck (prazosin, 8.5)[1].

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

RS 17053 hydrochloride Related Antibodies
In Vivo

RS 17053 hydrochloride has a rapid onset of action, and a duration of action exceeding 60 min. RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4, 132) 5 6.28, p , 0.0001]. 10 mg/kg RS-17053 significantly suppresses food intake[2].

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

449.41

Formula

C24H30Cl2N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.ClC1=CC2=C(NC=C2CC(C)(C)NCCOC3=CC=CC=C3OCC4CC4)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°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: 

DMSO : 100 mg/mL (222.51 mM; Need ultrasonic; 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 2.2251 mL 11.1257 mL 22.2514 mL
5 mM 0.4450 mL 2.2251 mL 4.4503 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.70%

SDS (252 KB)

COA (251 KB) HNMR (211 KB) RP-HPLC (114 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2]

Rats[2]
Adult male rats (n=56 to 8 per group) are pretreated (IP) with either 0, 0.1, 0.5, 2.5, or 10.0 mg/kg RS 17053 hydrochloride or with 2.0 mg/kg of the prototypical α1-Adrenoceptor antagonist prazosin. Five minutes later, each rat was treated (IP) with either 0, 5, 10 or 15 mg/kg PPA. Food and water intakes are recorded for a 30 min period starting 10 min after the treatment injection. Rats pretreated with vehicle and then treated with PPA exhibite a dose-dependent suppression of feeding with a maximal effect evident at the 15 mg/kg dose of PPA. Pretreatment with 2.0 mg/kg prazosin reverses the anorexic activity of PPA[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 1 mM 2.2251 mL 11.1257 mL 22.2514 mL 55.6285 mL
5 mM 0.4450 mL 2.2251 mL 4.4503 mL 11.1257 mL
10 mM 0.2225 mL 1.1126 mL 2.2251 mL 5.5628 mL
15 mM 0.1483 mL 0.7417 mL 1.4834 mL 3.7086 mL
20 mM 0.1113 mL 0.5563 mL 1.1126 mL 2.7814 mL
25 mM 0.0890 mL 0.4450 mL 0.8901 mL 2.2251 mL
30 mM 0.0742 mL 0.3709 mL 0.7417 mL 1.8543 mL
40 mM 0.0556 mL 0.2781 mL 0.5563 mL 1.3907 mL
50 mM 0.0445 mL 0.2225 mL 0.4450 mL 1.1126 mL
60 mM 0.0371 mL 0.1854 mL 0.3709 mL 0.9271 mL
80 mM 0.0278 mL 0.1391 mL 0.2781 mL 0.6954 mL
100 mM 0.0223 mL 0.1113 mL 0.2225 mL 0.5563 mL
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RS 17053 hydrochloride Related Classifications

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.

Keywords:

RS 17053169505-93-5RS-17053RS17053Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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