Prazosin [19216-56-9]

Referentie T22406-50mg

Formaat : 50mg

Merk : TargetMol


Prazosin

(Synonyms: Prazosine, Prazocin, Furazosin) Copy Product Info
Prazosin (Prazosine), an α1-blocker, acts as an inverse agonist at alpha-1 adrenergic receptors and is used to treat hypertension.
Prazosin
Cas No. 19216-56-9
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.89%
Appearance:Solid
Color:White
COA LCMS HNMR

Product Information

Prazosin AI Summary
Prazosin exhibits strong alpha-1 adrenergic receptor antagonism with a very high binding affinity, demonstrated by Ki values ranging from 0.19 nM to 0.32 nM across different assays. It shows a significantly lower affinity for the alpha-2 adrenergic receptor, with Ki values up to 4830.0 nM. This compound is highly selective for alpha-1 receptors over alpha-2 receptors, indicated by a selectivity ratio of around 1258.9. Prazosin effectively reduces blood pressure in spontaneously hypertensive rats, showing dose-dependent antihypertensive activity with a maximum reduction of 45.0 mmHg at an oral dose of 30 mg/kg. It also exhibits significant vasorelaxant activity, blocking norepinephrine-induced contractions in rat and rabbit arterial tissues. Furthermore, Prazosin demonstrates robust antagonist activity in various adrenergic subtypes, notably alpha-1A, alpha-1B, and alpha-1D adrenergic receptors. Along with the cardiovascular functions, it also shows potential in modulating neurotransmitter responses, given its efficacy in displacing radioligands like [3H]prazosin from rat cerebral cortex membranes and displaying antagonist activity at the dopamine D2 receptors. Prazosin's effective oral bioavailability and selective inhibition properties make it a promising candidate for addressing cardiovascular conditions such as hypertension..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Prazosin (Prazosine), an α1-blocker, acts as an inverse agonist at alpha-1 adrenergic receptors and is used to treat hypertension.
SynonymsPrazosine, Prazocin, Furazosin
Chemical Properties
Molecular Weight383.4
FormulaC19H21N5O4
Cas No.19216-56-9
SmilesNC=1C2=C(N=C(N1)N3CCN(C(=O)C4=CC=CO4)CC3)C=C(OC)C(OC)=C2
Relative Density.1.352g/cm3
Storage & Solubility Information
StorageStore under nitrogen, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (130.41 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.04 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 mM2.6082 mL13.0412 mL26.0824 mL130.4121 mL
5 mM0.5216 mL2.6082 mL5.2165 mL26.0824 mL
10 mM0.2608 mL1.3041 mL2.6082 mL13.0412 mL
20 mM0.1304 mL0.6521 mL1.3041 mL6.5206 mL
50 mM0.0522 mL0.2608 mL0.5216 mL2.6082 mL
100 mM0.0261 mL0.1304 mL0.2608 mL1.3041 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.