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Urapidil [34661-75-1]

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Referentie NB-64-00308-1mL

Formaat : 1mLx10mM(inDMSO)

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Urapidil

(Synonyms: Mediatensyl, Eupressyl, Ebrantil) Copy Product Info

Synonyms: Mediatensyl, Eupressyl, Ebrantil

Catalog No. T0165 Copy Product Info

Purity: 99.98%

Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.

Cas No. 34661-75-1

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.98%

Appearance:Solid

Color:White

Product Introduction

Urapidil AI Summary

Urapidil exhibits various pharmacokinetic properties and bioactivities. It has a partition coefficient (logD6.5) of 0.9 and a pKa of 7.1. It demonstrates an oral bioavailability of 79.0% in humans, suggesting its good absorption and significant metabolism and elimination, with hepatic and renal clearance, and a volume of distribution at steady state of 0.75 L.kg-1. After intravenous administration, Urapidil has a clearance of 3.1 mL.min-1.kg-1, a half-life of 3.5 hours, and a mean residence time of 4.0 hours. It shows a moderate tendency to partition into the cell membrane with a log Kmemb value of 0.2. Notably, the compound is a potent Alpha-1 adrenergic receptor antagonist with a Kd of 79.43 nM against phenylephrine-induced contraction in rabbit prostate. Urapidil additionally inhibits several targets such as Tau fibril formation, ERK signaling pathway, as well as various enzymes including Cytochrome P450 3A4, mammalian Selenoprotein Thioredoxin Reductase 1, and others. It shows binding affinity to the 5-HT1A receptor with a Ki of 213.0 nM, and the adrenergic receptor alpha1 with a Ki of 127.9 nM. Despite its broad enzymatic and receptor activity, Urapidil has limited inhibitory activity against BSEP, MRP2, MRP3, and MRP4, with IC50 values exceeding 133,000 nM. It also has antiviral activity against SARS-CoV-2 in certain assays, although the potency is relatively weak with IC50 values greater than 20,000 nM. Moreover, it shows weak inhibitory activity against human HDAC6 enzyme. Overall, Urapidil exhibits a range of pharmacological activities and properties that could be explored for potential therapeutic applications, particularly in modulating adrenergic receptors, enzymatic pathways, and antiviral domains..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.
Synonyms	Mediatensyl, Eupressyl, Ebrantil

Chemical Properties

Molecular Weight	387.48
Formula	C₂₀H₂₉N₅O₃
Cas No.	34661-75-1
Smiles	O(C)C1=C(C=CC=C1)N2CCN(CCCNC=3N(C)C(=O)N(C)C(=O)C3)CC2
Relative Density.	1.2058 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 41.25 mg/mL (106.46 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.16 mM), Sonication is recommended.

10% DMSO+90% Saline: 4.13 mg/mL (10.66 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5808 mL	12.9039 mL	25.8078 mL	129.0389 mL
5 mM	0.5162 mL	2.5808 mL	5.1616 mL	25.8078 mL
10 mM	0.2581 mL	1.2904 mL	2.5808 mL	12.9039 mL
20 mM	0.1290 mL	0.6452 mL	1.2904 mL	6.4519 mL
50 mM	0.0516 mL	0.2581 mL	0.5162 mL	2.5808 mL
100 mM	0.0258 mL	0.1290 mL	0.2581 mL	1.2904 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

α1-adrenergic receptorUrapidilSerotonin ReceptorInhibitorinhibitBeta ReceptorAdrenergicReceptorAdrenergic Receptor5-hydroxytryptamine Receptor5HTReceptor5-HT Receptor5HT Receptor5-HT

Related Tags: Urapidil chemical structure | Urapidil formula | Urapidil molecular weight

Urapidil [34661-75-1]

Referentie NB-64-00308-1mL

Neem contact op met een lokale distributeur :

Neem contact op met een lokale distributeur :

Urapidil

Product Introduction

Calculator

In Vivo Formulation Calculator (Clear solution)

Dose Conversion

Keywords

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