Doxazosin mesylate(UK 33274 mesylate)

Molecular Weight (MW)	547.58
Formula	C23H25N5O5.CH4O3S
CAS No.	77883-43-3
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 15 mg/mL (27.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)	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
Synonyms	UK-33274 mesylate; UK33274 mesylate; UK 33274 mesylate

Molecular Weight (MW)

547.58

Formula

C23H25N5O5.CH4O3S

CAS No.

77883-43-3

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 15 mg/mL (27.4 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In vivo)

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

Synonyms

UK-33274 mesylate; UK33274 mesylate; UK 33274 mesylate

In Vitro	In vitro activity: Doxazosin-induced apoptosis is blocked by specific caspase-8 inhibitors, supporting the functional involvement of caspase-8 in doxazosin-induced apoptosis. Doxazosin increases FADD recruitment and subsequent caspase-8 activation, implicating Fas-mediated apoptosis as the underlying mechanism of the effect of Doxazosin in prostate cells. Doxazosin and cholestyramine similarly decreases plasma total and LDL plus VLDL cholesterols, and total triglycerides on average by 46%, 61% and 45% respectively. Doxazosin induces DNA damage and cell death in HL-1 cell line. Doxazosin treatment decreases cell viability in primary cultures of neonatal rat cardiomyocytes, and Hoechst dye vital staining demonstrates doxazosin-induced apoptosis in primary cultures of human adult cardiomyocytes. Doxazosin antagonizes the VEGF-mediated angiogenic response of HUVEC cells, by abrogating cell adhesion to fibronectin and collagen-coated surfaces and inhibiting cell migration, via a potential downregulation of VEGF expression.
In Vivo	Doxazosin also reduces mean arterial pressure by 18% without affecting heart rate in all hamsters. Doxazosin causes a significant reduction in the wet weight of BabeTGF-beta 1-infected mouse prostate reconstitution (MPR).
Animal model
Formulation & Dosage
References	Cancer Res. 2006 Jan 1;66(1):464-72; Atherosclerosis. 1991 Nov;91(1-2):35-49; Prostate. 1997 Nov 1;33(3):157-63.

In Vitro

In vitro activity: Doxazosin-induced apoptosis is blocked by specific caspase-8 inhibitors, supporting the functional involvement of caspase-8 in doxazosin-induced apoptosis. Doxazosin increases FADD recruitment and subsequent caspase-8 activation, implicating Fas-mediated apoptosis as the underlying mechanism of the effect of Doxazosin in prostate cells. Doxazosin and cholestyramine similarly decreases plasma total and LDL plus VLDL cholesterols, and total triglycerides on average by 46%, 61% and 45% respectively. Doxazosin induces DNA damage and cell death in HL-1 cell line. Doxazosin treatment decreases cell viability in primary cultures of neonatal rat cardiomyocytes, and Hoechst dye vital staining demonstrates doxazosin-induced apoptosis in primary cultures of human adult cardiomyocytes. Doxazosin antagonizes the VEGF-mediated angiogenic response of HUVEC cells, by abrogating cell adhesion to fibronectin and collagen-coated surfaces and inhibiting cell migration, via a potential downregulation of VEGF expression.

In Vivo

Doxazosin also reduces mean arterial pressure by 18% without affecting heart rate in all hamsters. Doxazosin causes a significant reduction in the wet weight of BabeTGF-beta 1-infected mouse prostate reconstitution (MPR).

Animal model

Formulation & Dosage

References

Cancer Res. 2006 Jan 1;66(1):464-72; Atherosclerosis. 1991 Nov;91(1-2):35-49; Prostate. 1997 Nov 1;33(3):157-63.

CAS NO:	77883-43-3
规格:	≥98%

包装	价格(元)
500mg	电议
1g	电议
2g	电议
5g	电议
10g	电议
25g	电议