Naftifine HCl(AW-105843 SN 105843)

Molecular Weight (MW)	323.86
Formula	C21H21N.HCl
CAS No.	65473-14-5
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: 8 mg/mL (24.7 mM)
Other info	Chemical Name: (E)-N-methyl-N-(naphthalen-1-ylmethyl)-3-phenylprop-2-en-1-amine hydrochloride InChi Key: PGYDRGZVXVVZQC-LLVKDONJSA-N InChi Code: InChI=1S/C15H19N5/c1-11(15(2,3)4)19-14(18-10-17)20-13-7-5-12(9-16)6-8-13/h5-8,11H,1-4H3,(H2,18,19,20)/t11-/m1/s1 SMILES Code: CN(CC1=C2C=CC=CC2=CC=C1)C/C=C/C3=CC=CC=C3.[H]Cl
Synonyms	SN 105843; SN105843; SN-105843; AW 105843; AW105843; AW-105843; AW 105-843; Naftifine hydrochloride; Naftin

Molecular Weight (MW)

323.86

Formula

C21H21N.HCl

CAS No.

65473-14-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: <1 mg/mL

Water: <1 mg/mL

Ethanol: 8 mg/mL (24.7 mM)

Other info

Chemical Name: (E)-N-methyl-N-(naphthalen-1-ylmethyl)-3-phenylprop-2-en-1-amine hydrochloride

InChi Key: PGYDRGZVXVVZQC-LLVKDONJSA-N

InChi Code: InChI=1S/C15H19N5/c1-11(15(2,3)4)19-14(18-10-17)20-13-7-5-12(9-16)6-8-13/h5-8,11H,1-4H3,(H2,18,19,20)/t11-/m1/s1

SMILES Code: CN(CC1=C2C=CC=CC2=CC=C1)C/C=C/C3=CC=CC=C3.[H]Cl

Synonyms

SN 105843; SN105843; SN-105843; AW 105843; AW105843; AW-105843; AW 105-843; Naftifine hydrochloride; Naftin

In Vitro	In vitro activity: Naftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration (MIC) range 0.1 to 0.2 mg/mL), aspergilli (6 strains; MIC range, 0.8 to 12.5 mg/mL), Sporothrix schenckii (2 strains; MICs, 0.8 and 1.5 mg/mL), and yeasts of the genus Candida (77 strains; MIC range, 1.5 to greater than 100 mg/mL). The MIC of naftifine for C. albicans Δ63 is 100 mg/L in Sabouraud medium (initial pH 6.5). Naftifine (50 mg/L) gives greater than 99% inhibition of sterol biosynthesis both in whole cells and in cell extracts of C. albicans. The primary action of naftifine appears to be the blocking of fungal squalene epoxidation.
In Vivo	Naftifine HCl 2% cream results in clinical cure rate and clinical success rate of 33% and 84% after treatment for 4 weeks, and week 2 efficacy response rates in Naftifine HCl 2% subjects are all lower than at week 4 but are significantly higher than week 2 vehicle-treated counterparts. Naftifine causes interruption of fungal ergosterol synthesis and accumulation of squalene in fungal organisms. Naftifine also has demonstrated anti-inflammatory properties such as a reduction in superoxide production and a reduction in polymorphonuclear leukocyte chemotaxis/endothelial adhesion. Naftifine has shown good efficacy and safety for a variety of conditions and is a useful treatment that provides both antifungal action and relief of inflammatory signs and symptoms. Few adverse events have been noted with naftifine use, the most frequent being mild and transient burning, stinging, or itching in the application area.
Animal model
Formulation & Dosage
References	Antimicrob Agents Chemother. 1981 Mar;19(3):386-9; Antimicrob Agents Chemother. 1984 Apr;25(4):483-7; J Drugs Dermatol. 2011 Oct;10(10):1142-7.

In Vitro

In vitro activity: Naftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration (MIC) range 0.1 to 0.2 mg/mL), aspergilli (6 strains; MIC range, 0.8 to 12.5 mg/mL), Sporothrix schenckii (2 strains; MICs, 0.8 and 1.5 mg/mL), and yeasts of the genus Candida (77 strains; MIC range, 1.5 to greater than 100 mg/mL). The MIC of naftifine for C. albicans Δ63 is 100 mg/L in Sabouraud medium (initial pH 6.5). Naftifine (50 mg/L) gives greater than 99% inhibition of sterol biosynthesis both in whole cells and in cell extracts of C. albicans. The primary action of naftifine appears to be the blocking of fungal squalene epoxidation.

In Vivo

Naftifine HCl 2% cream results in clinical cure rate and clinical success rate of 33% and 84% after treatment for 4 weeks, and week 2 efficacy response rates in Naftifine HCl 2% subjects are all lower than at week 4 but are significantly higher than week 2 vehicle-treated counterparts. Naftifine causes interruption of fungal ergosterol synthesis and accumulation of squalene in fungal organisms. Naftifine also has demonstrated anti-inflammatory properties such as a reduction in superoxide production and a reduction in polymorphonuclear leukocyte chemotaxis/endothelial adhesion. Naftifine has shown good efficacy and safety for a variety of conditions and is a useful treatment that provides both antifungal action and relief of inflammatory signs and symptoms. Few adverse events have been noted with naftifine use, the most frequent being mild and transient burning, stinging, or itching in the application area.

Animal model

Formulation & Dosage

References

Antimicrob Agents Chemother. 1981 Mar;19(3):386-9; Antimicrob Agents Chemother. 1984 Apr;25(4):483-7; J Drugs Dermatol. 2011 Oct;10(10):1142-7.

CAS NO:	65473-14-5
规格:	≥98%

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议
1g	电议
5g	电议
10g	电议