Sertaconazole nitrate

Modify Date: 2024-01-02 02:08:25

Sertaconazole nitrate Structure
Sertaconazole nitrate structure
Common Name Sertaconazole nitrate
CAS Number 99592-39-9 Molecular Weight 500.783
Density N/A Boiling Point 614.1ºC at 760mmHg
Molecular Formula C20H16Cl3N3O4S Melting Point 158-160°
MSDS Chinese USA Flash Point 325.2ºC

 Use of Sertaconazole nitrate


Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.Target: AntifungalSertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL [1]. Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death [2].The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin [1]. Clinical trials with sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections [2]. Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema [3].

 Names

Name 1-[2-[(7-chloro-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl]imidazole,nitric acid
Synonym More Synonyms

 Sertaconazole nitrate Biological Activity

Description Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.Target: AntifungalSertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL [1]. Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death [2].The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin [1]. Clinical trials with sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections [2]. Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema [3].
Related Catalog
References

[1]. Liebel, F., et al., Anti-inflammatory and anti-itch activity of sertaconazole nitrate. Arch Dermatol Res, 2006. 298(4): p. 191-9.

[2]. Pfaller, M.A. and D.A. Sutton, Review of in vitro activity of sertaconazole nitrate in the treatment of superficial fungal infections. Diagn Microbiol Infect Dis, 2006. 56(2): p. 147-52.

[3]. Sur, R., et al., Anti-inflammatory activity of sertaconazole nitrate is mediated via activation of a p38-COX-2-PGE2 pathway. J Invest Dermatol, 2008. 128(2): p. 336-44.

 Chemical & Physical Properties

Boiling Point 614.1ºC at 760mmHg
Melting Point 158-160°
Molecular Formula C20H16Cl3N3O4S
Molecular Weight 500.783
Flash Point 325.2ºC
Exact Mass 498.992706
PSA 121.34000
LogP 7.19160
Storage condition ?20°C
Water Solubility DMSO: soluble20mg/mL, clear

 Safety Information

RIDADR NONH for all modes of transport
HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Salpetersäure--1-{2-[(7-chlor-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorphenyl)ethyl}-1H-imidazol(1:1)
Dermofix
Dermoseptic
1H-Imidazole, 1-[2-[(7-chlorobenzo[b]thien-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl]-, nitrate (1:1)
T56 BSJ IG D1OYR BG DG&1- AT5N CNJ &&HNO3
1-{2-[(7-Chloro-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole nitrate (1:1)
FI 7056
1-(2-((7-Chlorobenzo[b]thien-3-yl)methoxy)-2-(2,4-dichlorophenyl)ethyl)-1H-imidazole mononitrate
Ertaczo
sertaconazole nitrate
sertaconazole mononitrate
Zalain
Ginedermofix
Sertaconazole (nitrate)
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