Sertaconazole nitrate

製品コードS3161 バッチS316101

印刷

化学情報

Chemical Structure Synonyms FI-7045,FI7056 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H15Cl3N2OS.HNO3

 
分子量 500.78 CAS No. 99592-39-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.68 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sertaconazole nitrate (FI-7045,FI7056) is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.
in vitro

Sertaconazole 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. This compound is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL. [1] It inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. This chemical 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] This compound (< 100 μg/mL) activates p38 MAP kinase and Hsp27 in keratinocytes. It induces (< 2 μg/mL) COX-2 protein expression and PGE2 production in keratinocytes, which dependent on p38 activation. PGE2 is involved in this compound (1 μg/mL)-mediated suppression of cytokine production in keratinocytes and PBMCs. [3]
in vivo

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. This compound elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with this chemical 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 this compound cream 2% show efficacy in the treatment of superficial cutaneous fungal infections. [2] It reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks it from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema. [3] The dermal administration of this chemical to rats, in which edema is induced by application of croton oil in the external ear, induced a 39.8% reduction of edema. [4]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/16868738/
  • https://pubmed.ncbi.nlm.nih.gov/16822638/
  • https://pubmed.ncbi.nlm.nih.gov/17637821/
  • https://pubmed.ncbi.nlm.nih.gov/8803954/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Terconazole, an Azole Antifungal Drug, Increases Cytotoxicity in Antimitotic Drug-Treated Resistant Cancer Cells with Substrate-Specific P-gp Inhibitory Activity [ Int J Mol Sci, 2022, 23(22)13809] PubMed: 36430288

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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