Urapidil HCl

Alias: Urapidil hydrochloride; Urapidil HCl

Cat No.:V1025 Purity: ≥98%

COA Product Data Instructions for use SDS

Urapidil HCl, the hydrochloride salt of uradipil which is a sympatholytic antihypertensive drug, is potent α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.

Urapidil HCl Chemical Structure CAS No.: 64887-14-5
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Urapidil HCl:

Urapidil

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Biological Activity I Assay Protocols (From Reference)

Targets

5-HT_1A Receptor; α adrenergic receptor; α1-adrenergic receptor ( pIC50 = 6.13 ); α2-adrenergic receptor ( pIC50 = 4.38 )

ln Vitro

In vitro activity: Urapidil hydrochloride is urapidil in hydrochloride salt form, a α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 values of 6.13 and 6.4, according to the substance. On top of its alpha-blocking effects, urapidil also stimulates serotonin 5HT1A receptors in the central nervous system, which is how it produces its central sympatholytic effect, which sets it apart from other alpha-blockers. On top of its alpha-blocking effects, urapidil also stimulates serotonin 5HT1A receptors in the central nervous system, which is how it produces its central sympatholytic effect, which sets it apart from other alpha-blockers. In patients whose blood pressure is not adequately controlled by other medications, oral urapidil has been shown in multiple studies to be both effective and well-tolerated as a second-line treatment. In hypertensive patients with co-occurring diabetes and/or hyperlipidemia, urapidil has also been demonstrated to enhance glucose and lipid metabolism.

ln Vivo

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

Animal Protocol

References

[1]. 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.

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

[3]. Neonatal transient respiratory depression after maternal urapidil infusion for hypertension. Eur J Pediatr. 2009 Feb;168(2):221-3.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C20H30CLN5O3

Molecular Weight

423.94

Exact Mass

423.2

Elemental Analysis

C, 56.66; H, 7.13; Cl, 8.36; N, 16.52; O, 11.32

CAS #

64887-14-5

Related CAS #

Urapidil; 34661-75-1

Appearance

Solid powder

SMILES

CN1C(=CC(=O)N(C1=O)C)NCCCN2CCN(CC2)C3=CC=CC=C3OC.Cl

InChi Key

KTMLZVUAXJERAT-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H29N5O3.ClH/c1-22-18(15-19(26)23(2)20(22)27)21-9-6-10-24-11-13-25(14-12-24)16-7-4-5-8-17(16)28-3;/h4-5,7-8,15,21H,6,9-14H2,1-3H3;1H

Chemical Name

6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethylpyrimidine-2,4-dione;hydrochloride

Synonyms

Urapidil hydrochloride; Urapidil HCl

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 14.3~24 mg/mL (33.7~56.6 mM)

Water: ~85 mg/mL (~200.5 mM)

Ethanol: <1 mg/mL

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03790800	Completed	Drug: urapidil	Stroke, Acute Cerebrovascular Disorders	The George Institute for Global Health, China	March 20, 2020	Phase 3
NCT03497351	Completed	Drug: Nicardipine Drug: Urapidil	General Surgery	Chinese PLA General Hospital	April 15, 2018	Not Applicable

Biological Data

Effects of intravenous urapidil on (A) SBP, (B) DBP and (C) HR within 7 days of treatment, as compared with nitroglycerin, in elderly patients with hypertension and acute decompensated heart failure.Exp Ther Med. 2016 Jul; 12(1): 115–122.

Urapidil HCl — Effects of intravenous urapidil on the serum level of NT-proBNP within 7 days of treatment, as compared with nitroglycerin, in elderly patients with hypertension and acute decompensated heart failure.Exp Ther Med. 2016 Jul; 12(1): 115–122.