Urapidil hydrochloride

Cat. No.: HY-B0354A Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Urapidil hydrochloride is an orally active α1-adrenoceptor antagonist and 5-HT_1A receptor agonist with a pIC₅₀ of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect.

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

Urapidil hydrochloride Chemical Structure

CAS No. : 64887-14-5

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
50 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of Urapidil hydrochloride:

Urapidil In-stock

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

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α adrenergic receptor β adrenergic receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT_1A Receptor

α adrenergic receptor

α1-adrenergic receptor

6.13 (pIC₅₀)

α2-adrenergic receptor

4.38 (pIC₅₀)

In Vivo

Urapidil (p.o. or i.v.) causes sedation and decreased tonus in mice and rats^[3].

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

Clinical Trial

Molecular Weight

423.94

Formula

C₂₀H₃₀ClN₅O₃

CAS No.

64887-14-5

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C)C(C=C(NCCCN2CCN(C3=CC=CC=C3OC)CC2)N1C)=O.Cl

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:

H₂O : 100 mg/mL (235.88 mM; Need ultrasonic)

DMSO : 14.29 mg/mL (33.71 mM; ultrasonic and warming and heat to 60°C; 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	2.3588 mL	11.7941 mL	23.5882 mL
5 mM	0.4718 mL	2.3588 mL	4.7176 mL
10 mM	0.2359 mL	1.1794 mL	2.3588 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)

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: ≥ 1.25 mg/mL (2.95 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.95 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.95 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (117.94 mM); Clear solution; Need ultrasonic

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.

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: 99.97%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (249 KB) HNMR (270 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Gross, G., G. Hanft, and N. Kolassa, Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for alpha 1-adrenoceptor binding sites. Naunyn Schmiedebergs Arch Pharmacol, 1987. 336(6): p. 597-601. [Content Brief]

[2]. Buch, J., Urapidil, a dual-acting antihypertensive agent: Current usage considerations. Adv Ther, 2010. 27(7): p. 426-43. [Content Brief]

[3]. Vanhaesebrouck S, et al. Neonatal transient respiratory depression after maternal urapidil infusion for hypertension. Eur J Pediatr. 2009 Feb;168(2):221-3. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.3588 mL	11.7941 mL	23.5882 mL	58.9706 mL
	5 mM	0.4718 mL	2.3588 mL	4.7176 mL	11.7941 mL
	10 mM	0.2359 mL	1.1794 mL	2.3588 mL	5.8971 mL
	15 mM	0.1573 mL	0.7863 mL	1.5725 mL	3.9314 mL
	20 mM	0.1179 mL	0.5897 mL	1.1794 mL	2.9485 mL
	25 mM	0.0944 mL	0.4718 mL	0.9435 mL	2.3588 mL
	30 mM	0.0786 mL	0.3931 mL	0.7863 mL	1.9657 mL
H₂O	40 mM	0.0590 mL	0.2949 mL	0.5897 mL	1.4743 mL
	50 mM	0.0472 mL	0.2359 mL	0.4718 mL	1.1794 mL
	60 mM	0.0393 mL	0.1966 mL	0.3931 mL	0.9828 mL
	80 mM	0.0295 mL	0.1474 mL	0.2949 mL	0.7371 mL
	100 mM	0.0236 mL	0.1179 mL	0.2359 mL	0.5897 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.