Doxazosin mesylate | CAS#77883-43-3 | Selective α-1-Adrenergic Blocker

MedKoo Cat#: 561778 | Name: Doxazosin mesylate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Doxazosin Mesylate is an alpha-Adrenergic receptor blocker.

Chemical Structure

Doxazosin mesylate

CAS#77883-43-3 (mesylate)

Theoretical Analysis

MedKoo Cat#: 561778

Name: Doxazosin mesylate

CAS#: 77883-43-3 (mesylate)

Chemical Formula: C24H29N5O8S

Exact Mass: 0.0000

Molecular Weight: 547.58

Elemental Analysis: C, 52.64; H, 5.34; N, 12.79; O, 23.37; S, 5.85

Price and Availability

Size	Price	Availability	Quantity
1g	USD 250.00	2 Weeks
5g	USD 650.00	2 Weeks

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Related CAS #

70918-01-3 (HCl) 77883-43-3 (mesylate) 74191-85-8 (free base)

Synonym

Doxazosin mesylate; Doxazosin methanesulfonate; Cardura; Carduran; Cardular; UK-33274; UK33274; UK 33274; UK 33274-27; UK33274-27; UK-33274-27;

IUPAC/Chemical Name

(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanone methanesulfonate

InChi Key

VJECBOKJABCYMF-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4)

SMILES Code

O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4COC5=CC=CC=C5O4.OS(=O)(C)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Doxazosin mesylate (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.

In vitro activity:

Expression of Col1α1 was significantly decreased by DX (doxazosin) (10 μmol/L) at mRNA (-30 %) and protein level (-50 %) in TGF-β treated aHSCs. DX significantly reduced aHSCs proliferation and increased expression of senescence and SASP markers. PMA and m-3M3FBS reversed the effect of DX on senescence markers. Reference: Mech Ageing Dev. 2022 Jan;201:111617. https://pubmed.ncbi.nlm.nih.gov/34958827/

In vivo activity:

Doxazosin treatment protected against the rat kidney damage and attenuated the associated biochemical changes. Doxazosin has a direct renoprotective effect possibly by down-regulating SGLT2. Reference: Basic Clin Pharmacol Toxicol. 2020 May;126(5):413-423. https://pubmed.ncbi.nlm.nih.gov/31788938/

	Solvent	mg/mL	mM
Solubility
	DMF	0.5	0.91
	DMSO	25.9	47.21
	DMSO:PBS (pH 7.2) (1:1)	0.5	0.91
	Water	1.0	1.83

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Serna-Salas SA, Arroyave-Ospina JC, Zhang M, Damba T, Buist-Homan M, Muñoz-Ortega MH, Ventura-Juárez J, Moshage H. α-1 Adrenergic receptor antagonist doxazosin reverses hepatic stellate cells activation via induction of senescence. Mech Ageing Dev. 2022 Jan;201:111617. doi: 10.1016/j.mad.2021.111617. Epub 2021 Dec 24. PMID: 34958827. 2. Xiu AY, Ding Q, Li Z, Zhang CQ. Doxazosin Attenuates Liver Fibrosis by Inhibiting Autophagy in Hepatic Stellate Cells via Activation of the PI3K/Akt/mTOR Signaling Pathway. Drug Des Devel Ther. 2021 Aug 21;15:3643-3659. doi: 10.2147/DDDT.S317701. PMID: 34456560; PMCID: PMC8387324. 3. Rezq S, Nasr AM, Shaheen A, Elshazly SM. Doxazosin down-regulates sodium-glucose cotransporter-2 and exerts a renoprotective effect in rat models of acute renal injury. Basic Clin Pharmacol Toxicol. 2020 May;126(5):413-423. doi: 10.1111/bcpt.13371. Epub 2019 Dec 22. PMID: 31788938. 4. Sun JA, Kong DZ, Zhen YQ, Li Q, Zhang W, Zhang JH, Yin ZW, Ren LM. Stereoselective binding of doxazosin enantiomers to plasma proteins from rats, dogs and humans in vitro. Acta Pharmacol Sin. 2013 Dec;34(12):1568-74. doi: 10.1038/aps.2013.120. Epub 2013 Nov 18. PMID: 24241343; PMCID: PMC4002564.

In vitro protocol:

In vivo protocol:

1. Rezq S, Nasr AM, Shaheen A, Elshazly SM. Doxazosin down-regulates sodium-glucose cotransporter-2 and exerts a renoprotective effect in rat models of acute renal injury. Basic Clin Pharmacol Toxicol. 2020 May;126(5):413-423. doi: 10.1111/bcpt.13371. Epub 2019 Dec 22. PMID: 31788938. 2. Sun JA, Kong DZ, Zhen YQ, Li Q, Zhang W, Zhang JH, Yin ZW, Ren LM. Stereoselective binding of doxazosin enantiomers to plasma proteins from rats, dogs and humans in vitro. Acta Pharmacol Sin. 2013 Dec;34(12):1568-74. doi: 10.1038/aps.2013.120. Epub 2013 Nov 18. PMID: 24241343; PMCID: PMC4002564.

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