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4-Amino-N-methylphthalimide

$58

  • Brand : BIOFRON

  • Catalogue Number : BN-O1162

  • Specification : 98%(HPLC)

  • CAS number : 2307-00-8

  • Formula : C9H8N2O2

  • Molecular Weight : 176.17

  • PUBCHEM ID : 726931

  • Volume : 5mg

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Catalogue Number

BN-O1162

Analysis Method

Specification

98%(HPLC)

Storage

2-8°C

Molecular Weight

176.17

Appearance

Botanical Source

Structure Type

Category

SMILES

CN1C(=O)C2=C(C1=O)C=C(C=C2)N

Synonyms

N-Methyl-4-aminophthalimide/5-Amino-2-methyl-isoindolin-1,3-dion/5-Amino-2-methyl-isoindole-1,3-dione/1H-Isoindole-1,3(2H)-dione, 5-amino-2-methyl-/5-amino-2-methylisoindoline-1,3-dione/4-Amino-N-methylphthalimide/4-amino-N-methylphthalimide dimer/5-Amino-2-methyl-1H-isoindole-1,3(2H)-dione/4-amino-N-methylphtalimide

IUPAC Name

5-amino-2-methylisoindole-1,3-dione

Density

1.4±0.1 g/cm3

Solubility

Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.

Flash Point

176.6±23.2 °C

Boiling Point

368.3±25.0 °C at 760 mmHg

Melting Point

246-248ºC

InChl

InChl Key

KMEBUNSLFRQSEM-UHFFFAOYSA-N

WGK Germany

RID/ADR

HS Code Reference

Personal Projective Equipment

Correct Usage

For Reference Standard and R&D, Not for Human Use Directly.

Meta Tag

provides coniferyl ferulate(CAS#:2307-00-8) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate

No Technical Documents Available For This Product.

PMID

28201509

Abstract

Objectives: T-2307, a novel arylamidine, exhibits potent broad-spectrum activities against the majority of fungal pathogens. In this study, the antifungal activity of T-2307 against Cryptococcus gattii was evaluated in comparison with those of amphotericin B, fluconazole and voriconazole in vitro and in vivo.

Methods: The MICs for 15 clinical isolates were determined according to CLSI guidelines and time-kill studies were performed using C. gattii YF2784. In a murine model for intranasal pulmonary infection caused by C. gattii YF2784, the test compounds were administered once daily for 7 days from 2 h or 14 days post-infection. The viable counts in the lungs and brain were determined at 21 days post-infection.

Results: The MIC range, MIC50, MIC90 and geometric mean MIC of T-2307 were 0.0078-0.0625, 0.0313, 0.0625 and 0.0394 mg/L, respectively. The MIC of T-2307 was significantly lower than those of fluconazole, voriconazole and amphotericin B. T-2307 showed concentration-dependent fungicidal activity at 4 times the MIC or higher. Administration of T-2307 at 2 mg/kg/day, amphotericin B at 1 mg/kg/day and fluconazole at 160 mg/kg/day from 2 h post-infection significantly reduced viable counts in the lungs and brain. However, when the administration was started 14 days post-infection, only T-2307 significantly reduced the viable counts in both the lungs and the brain at 1 mg/kg/day.

Conclusions: T-2307 shows excellent in vitro and in vivo antifungal activities against C. gattii and would be a promising new candidate for the treatment of cryptococcosis.

Title

In vitro and in vivo antifungal activities of T-2307, a novel arylamidine, against Cryptococcus gattii: an emerging fungal pathogen

Author

Hiroshi Nishikawa,1 Yoshiko Fukuda,1 Junichi Mitsuyama,1 Masato Tashiro,2 Akitaka Tanaka,3 Takahiro Takazono,2 Tomomi Saijo,4 Kazuko Yamamoto,3,4 Shigeki Nakamura,5 Yoshifumi Imamura,4 Taiga Miyazaki,2,4 Hiroshi Kakeya,6 Yoshihiro Yamamoto,7 Katsunori Yanagihara,8 Hiroshi Mukae,4,9 Shigeru Kohno,4,9 and Koichi Izumikawa2

Publish date

2017 Jun;

PMID

26620102

Abstract

Objectives
Candida species are major causes of invasive mycoses in immunocompetent and immunocompromised hosts. Treatment options are limited in the setting of antifungal resistance and increased rates of echinocandin-resistant Candida glabrata have been reported. The novel arylamidine T-2307 demonstrates potent in vitro antifungal activity against Candida species. Our objective was to evaluate the in vitro and in vivo activity of T-2307 against resistant C. glabrata.

Methods
In vitro activity was determined against 42 clinical C. glabrata isolates, including 17 echinocandin-resistant strains. Neutropenic ICR mice were inoculated intravenously with an echinocandin-resistant C. glabrata isolate (T-2307; caspofungin MICs ≤0.008 and 0.5 mg/L, respectively). Therapy with vehicle control, T-2307 (0.75, 1.5, 3 or 6 mg/kg subcutaneously once daily) or caspofungin (1 or 10 mg/kg intraperitoneally once daily) began 1 day post-challenge. Kidneys were collected on day 8 and fungal burden was assessed by counting cfu.

Results
T-2307 demonstrated potent in vitro activity against C. glabrata (geometric mean MIC 0.0135 mg/L), which was maintained against echinocandin-resistant isolates (geometric mean MIC 0.0083 mg/L). T-2307 also demonstrated in vivo efficacy in mice infected with echinocandin-resistant C. glabrata. Significant reductions in fungal burden were observed at each dosage level of T-2307 compared with control. Reductions in fungal burden were also observed with high-dose caspofungin.

Conclusions
T-2307 demonstrated potent in vitro activity against C. glabrata, including echinocandin-resistant isolates, which translated into in vivo efficacy against invasive candidiasis caused by an echinocandin-resistant C. glabrata strain. These results demonstrate the potential for T-2307 as therapy against echinocandin-resistant Candida.

Title

The novel arylamidine T-2307 demonstrates in vitro and in vivo activity against echinocandin-resistant Candida glabrata

Author

Nathan P. Wiederhold,1,* Laura K. Najvar,1,2 Annette W. Fothergill,1 Rosie Bocanegra,1,2 Marcos Olivo,1,2 Dora I. McCarthy,1 Yoshiko Fukuda,3 Junichi Mitsuyama,3 and Thomas F. Patterson1,2

Publish date

2016 Mar;

PMID

25451054

Abstract

We evaluated the in vitro and in vivo activities of the investigational arylamidine T-2307 against echinocandin-resistant Candida albicans. T-2307 demonstrated potent in vitro activity, and daily subcutaneous doses between 0.75 and 6 mg/kg of body weight significantly improved survival and reduced fungal burden compared to placebo control and caspofungin (10 mg/kg/day) in mice with invasive candidiasis caused by an echinocandin-resistant strain. Thus, T-2307 may have potential use in the treatment of echinocandin-resistant C. albicans infections.

Title

The Novel Arylamidine T-2307 Maintains In Vitro and In Vivo Activity against Echinocandin-Resistant Candida albicans

Author

Nathan P. Wiederhold,corresponding authora Laura K. Najvar,a,b Annette W. Fothergill,a Rosie Bocanegra,a,b Marcos Olivo,a,b Dora I. McCarthy,a William R. Kirkpatrick,a,b Yoshiko Fukuda,c Junichi Mitsuyama,c and Thomas F. Pattersona,b

Publish date

2015 Feb;


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