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.
28201509
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.
In vitro and in vivo antifungal activities of T-2307, a novel arylamidine, against Cryptococcus gattii: an emerging fungal pathogen
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
2017 Jun;
26620102
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.
The novel arylamidine T-2307 demonstrates in vitro and in vivo activity against echinocandin-resistant Candida glabrata
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
2016 Mar;
25451054
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.
The Novel Arylamidine T-2307 Maintains In Vitro and In Vivo Activity against Echinocandin-Resistant Candida albicans
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
2015 Feb;
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