2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Adrenergic Receptor
  4. Urapidil

Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

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

Urapidil Chemical Structure

Urapidil Chemical Structure

CAS No. : 34661-75-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
50 mg USD 60 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Urapidil:

Urapidil Related Antibodies

Top Publications Citing Use of Products

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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

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

IC50 & Target[1]

5-HT1A Receptor

 

α1-adrenoreceptor

 

In Vitro

Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist. Urapidil does not affect vascular tone at concentrations up to 10-5 M. Urapidil (10-5 M) markedly inhibits the alpha 1-adrenergic agonist (phenylephrine)-induced concentration-dependent contractions in aortic rings without endothelium and also to some extent in those with endothelium. Moreover, the inhibitory effect of Urapidil is more pronounced in rings without endothelium than in those with endothelium. Urapidil (10-5 M) affects neither the vascular tone nor the concentration-dependent contraction to serotonin[1].

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

Urapidil Related Antibodies
Clinical Trial
Molecular Weight

387.48

Formula

C20H29N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5808 mL 12.9039 mL 25.8078 mL
5 mM 0.5162 mL 2.5808 mL 5.1616 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).
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
References
Cell Assay

The rat aorta is placed in Krebs solution and stripped of connective tissue, then subsequently cut into rings (2 to 3 mm in length). As indicated, the endothelium is removed by rubbing the intimal surface of rings with a pair of forceps. The rings are suspended in organ baths containing oxygenated (95% O2 and 5% CO2) Krebs bicarbonate solution. Following equilibration for 90 min under a resting tension of 2 g, the rings are contracted with KCl (80 mM) to assess their reactivity. After a 30-min washout period, the rings are contracted with the α1-adrenergic receptor agonist phenylephrine (10-6 M) to about 80% of the maximal contraction before addition of acetylcholine (10-6 M) to check for the presence of a functional endothelium. After a 30-min equilibration period, the rings with or without endothelium are exposed to Urapidil (10-5 M) for 25 min before inducing a concentration-contraction curve to phenylephrine[1].

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5808 mL 12.9039 mL 25.8078 mL 64.5195 mL
5 mM 0.5162 mL 2.5808 mL 5.1616 mL 12.9039 mL
10 mM 0.2581 mL 1.2904 mL 2.5808 mL 6.4519 mL
15 mM 0.1721 mL 0.8603 mL 1.7205 mL 4.3013 mL
20 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2260 mL
25 mM 0.1032 mL 0.5162 mL 1.0323 mL 2.5808 mL
30 mM 0.0860 mL 0.4301 mL 0.8603 mL 2.1506 mL
40 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2904 mL
60 mM 0.0430 mL 0.2151 mL 0.4301 mL 1.0753 mL
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Urapidil 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:

Urapidil34661-75-15-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorInhibitorinhibitorinhibit

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