Doxazosin mesylate

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Cat.No. 2964 - Doxazosin mesylate | C23H25N5O5.CH3SO3H | CAS No. 77883-43-3
Description: α1 antagonist
Alternative Names: UK 33274
Chemical Name: 4-Amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline methanesulfonate
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

Selective α1-adrenoceptor antagonist (pKi values are 9.0, 8.5 and 8.4 for human α1B, α1A and α1D receptors respectively). Displays antihypertensive activity.

Compound Libraries

Doxazosin mesylate is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 547.58
Formula C23H25N5O5.CH3SO3H
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 77883-43-3
PubChem ID 62978
InChI Key VJECBOKJABCYMF-UHFFFAOYSA-N
Smiles NC2=NC(N3CCN(C(C4COC(C=CC=C5)=C5O4)=O)CC3)=NC1=CC(OC)=C(OC)C=C12.CS(=O)(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.07 75

Preparing Stock Solutions

The following data is based on the product molecular weight 547.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 2.43 mL 12.17 mL 24.35 mL
3.75 mM 0.49 mL 2.43 mL 4.87 mL
7.5 mM 0.24 mL 1.22 mL 2.43 mL
37.5 mM 0.05 mL 0.24 mL 0.49 mL

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References

References are publications that support the biological activity of the product.

Alabaster and Davey (1986) The α1-adrenoceptor antagonist profile of doxazosin: preclinical pharmacology. Br.J.Clin.Pharmacol. 21 9S PMID: 2871857

Kenny et al (1996) Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: binding functional and in vivo studies. Br.J.Pharmacol. 118 871 PMID: 8799556

Ma et al (2006) Chiral selective effects of doxazosin enantiomers on blood pressure and urinaruy bladder pressure in anesthetized rats. Acta Pharmacol.Sinica 27 1423


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4 Citations for Doxazosin mesylate

Citations are publications that use Tocris products. Selected citations for Doxazosin mesylate include:

Jahchan et al (2013) A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov 3 1364 PMID: 24078773

Kahn et al (2016) The anti-hypertensive drug prazosin inhibits glioblastoma growth via the PKCδ-dependent inhibition of the AKT pathway. EMBO Mol Med 8 511 PMID: 27138566

Diaz et al (2014) Moderate Alcohol Exposure during the Rat Equivalent to the Third Trimester of Human Pregnancy Alters Regulation of GABAA Receptor-Mediated Synaptic Transmission by Dopamine in the Basolateral Amygdala. Front Cell Neurosci 2 46 PMID: 24904907

Cilz et al (2014) Dopaminergic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440


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