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

Urapidil 

Cat. No.: HY-B0716 Purity: 99.89%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

Clinical Trial
Molecular Weight

387.48

Formula

C₂₀H₂₉N₅O₃

CAS No.

34661-75-1

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.52 mM; Need ultrasonic)

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
10 mM 0.2581 mL 1.2904 mL 2.5808 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
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Keywords:

Urapidil5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorInhibitorinhibitorinhibit

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