AFN-1252

Research use only, not for human use.

A potent inhibitor of bacterial enoyl-ACP reductase FabI.

A potent inhibitor of bacterial enoyl-ACP reductase FabI; demonstrates MICs of 0.015 and 0.008 ug/ml for S. aureus ATCC 29213 and S. aureus ATCC 33592 (MRSA), respectively; demonstrates a Staphylococcus-specific spectrum of activity.Bacterial Infection Phase 2 Clinical.

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Animal Model:Female 5- to 6-week-old CD-1 mice (18 to 22 g) with S. aureus Smith bacterial inoculumDosage:0.03, 0.1, 0.3, 1, 3 mg/kg Administration:Oral gavage; single dose Result:Was efficacious in a mouse model of septicemia, with 100% survival obtained with a single oral dose of 1 mg/kg. The calculated ED50s (95% confidence limits) were 0.15 (0.11 to 0.21) mg/kg.

API-1252 | Debio-1452

GPCR/G Protein

Antibacterial

enoyl-acylcarrierproteinreductase(FabI)

Infection

Bacterial Infection

620175-39-5

375.4204

C22H21N3O3

>98% (HPLC)

DMSO: 5.8 mg/mL (Need ultrasonic)

O=C(N(C)CC1=C(C)C2=CC=CC=C2O1)/C=C/C3=CC(CC4)=C(N=C3)NC4=O

2-Propenamide, N-methyl-N-[(3-methyl-2-benzofuranyl)methyl]-3-(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-3-yl)-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years