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Urapidil

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Catalog No. T0165Cas No. 34661-75-1
Alias Mediatensyl, Eupressyl, Ebrantil

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

Urapidil

Urapidil

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Purity: 99.85%
Catalog No. T0165Alias Mediatensyl, Eupressyl, EbrantilCas No. 34661-75-1
Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$33In StockIn Stock
50 mg$47In StockIn Stock
100 mg$68In StockIn Stock
500 mg$159InquiryInquiry
1 mL x 10 mM (in DMSO)$39In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.85%
Appearance:Solid
Color:White
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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.
SynonymsMediatensyl, Eupressyl, Ebrantil
Chemical Properties
Molecular Weight387.48
FormulaC20H29N5O3
Cas No.34661-75-1
SmilesO(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
StoragePowder: -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: 50 mg/mL (129.04 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.
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
1mg5mg10mg50mg
1 mM2.5808 mL12.9039 mL25.8078 mL129.0389 mL
5 mM0.5162 mL2.5808 mL5.1616 mL25.8078 mL
10 mM0.2581 mL1.2904 mL2.5808 mL12.9039 mL
20 mM0.1290 mL0.6452 mL1.2904 mL6.4519 mL
50 mM0.0516 mL0.2581 mL0.5162 mL2.5808 mL
100 mM0.0258 mL0.1290 mL0.2581 mL1.2904 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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