RS 17053 hydrochloride (Synonyms: RS-17053)

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

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RS 17053 hydrochloride is a potent and selective α1_A adrenoceptor antagonist, with a pK_i 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

CAS No. : 169505-93-5

Size	Price	Stock	Quantity

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Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Protocol
Purity & Documentation
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Description

RS 17053 hydrochloride is a potent and selective α1_A adrenoceptor antagonist, with a pK_i value of 9.1 in native cell membrane and a pA₂ value of 9.8 in functional assays.

IC₅₀ & Target

pKi: 9.1 (α1_A adrenoceptor in native cell membrane)
pA2: 9.8 (α1_A adrenoceptor)^[1].

In Vitro

In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pK_i and pA₂ estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pK_i 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.

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.

169505-93-5

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
10 mM	0.2225 mL	1.1126 mL	2.2251 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

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

Handling Instructions (2659 KB)

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.

Complete Stock Solution Preparation Table

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

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-17053RS17053Inhibitorinhibitorinhibit

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