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编 号：F747766
分子式：C47H80FN17O11
分子量：1078.24
分子式：C47H80FN17O11
分子量：1078.24
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CAS No: 1894081-09-4
产品详情
生物活性：
NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties.
体内研究：
NOSO-502 (1.3-40 mg/kg；皮下注射；单剂量) 在感染大肠杆菌 EN122 的 NMRI 小鼠中显示出抗菌作用。NOSO-502 (4-24 mg/kg；皮下注射；单剂量) 在感染大肠杆菌 UTI89 的 C3H/HeN 小鼠中显示出保护作用。NOSO-502 (2-80 mg/kg；皮下注射；单剂量) 在感染肺炎克雷伯菌 NCTC 13442 的 CD-1/ICR 小鼠中显示出保护作用。NOSO-502 的药代动力学 (PK) 参数SpeciesRouteDose (mg/kg)Cmax (mg/L)AUC0-Tlast (mg/L?h)Vd (L/kg)T1/2 (min)Clearance (L/h/kg)
MouseIntravenous injection3023.468.880.66251.13
RatIntravenous injection1540.707.990.94901.92
Animal Model:Female NMRI mice infected E. coli EN122.
Dosage:1.3, 2.5, 5, 10, 20, and 40 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Showed anti-infective effect.
Animal Model:Female C3H/HeN mice infected E. coli UTI89.
Dosage:4, 12 and 24 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Significantly attenuated E. coli UTI89 damage to urine, bladder, kidneys, and improved survival rates.
Animal Model:Male CD-1/ICR mice infected K. pneumoniae NCTC 13442.
Dosage:2, 6, 20 and 80 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Significantly improved lung tissue damage.
体外研究：
NOSO-502 (16 μg/mL 和 32 μg/mL；24 h) 使大肠杆菌 ATCC 25922 和肺炎克雷伯菌 ATCC 43816 菌株对 NOSO-502 产生抗性。NOSO-502 (100 μM) 降低了 HRPTEpiC 细胞活性，但不显著增加热休克蛋白 27 (HSP27) 和肾损伤分子 1 (KIM-1) 的表达。NOSO-502 的体外抗菌活性Citrobacter freundii DSM 30039Citrobacter kozeri DSM 4595Enterobacter aerogenes DSM 30053Enterobacter cloacae DSM 14563Escherichia coli ATCC 25922
MIC (μg/mL)22224
Klebsiella pneumoniae ATCC 43816Serratia marcescens DSM 17174Stenotrophomonas maltophilia ATCC 13637Staphylococcus aureus ATCC 29213Staphylococcus epidermidis ATCC 12228
MIC (μg/mL)141610.25
NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties.
体内研究：
NOSO-502 (1.3-40 mg/kg；皮下注射；单剂量) 在感染大肠杆菌 EN122 的 NMRI 小鼠中显示出抗菌作用。NOSO-502 (4-24 mg/kg；皮下注射；单剂量) 在感染大肠杆菌 UTI89 的 C3H/HeN 小鼠中显示出保护作用。NOSO-502 (2-80 mg/kg；皮下注射；单剂量) 在感染肺炎克雷伯菌 NCTC 13442 的 CD-1/ICR 小鼠中显示出保护作用。NOSO-502 的药代动力学 (PK) 参数SpeciesRouteDose (mg/kg)Cmax (mg/L)AUC0-Tlast (mg/L?h)Vd (L/kg)T1/2 (min)Clearance (L/h/kg)
MouseIntravenous injection3023.468.880.66251.13
RatIntravenous injection1540.707.990.94901.92
Animal Model:Female NMRI mice infected E. coli EN122.
Dosage:1.3, 2.5, 5, 10, 20, and 40 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Showed anti-infective effect.
Animal Model:Female C3H/HeN mice infected E. coli UTI89.
Dosage:4, 12 and 24 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Significantly attenuated E. coli UTI89 damage to urine, bladder, kidneys, and improved survival rates.
Animal Model:Male CD-1/ICR mice infected K. pneumoniae NCTC 13442.
Dosage:2, 6, 20 and 80 mg/kg.
Administration:Subcutaneous injection; single dose.
Result:Significantly improved lung tissue damage.
体外研究：
NOSO-502 (16 μg/mL 和 32 μg/mL；24 h) 使大肠杆菌 ATCC 25922 和肺炎克雷伯菌 ATCC 43816 菌株对 NOSO-502 产生抗性。NOSO-502 (100 μM) 降低了 HRPTEpiC 细胞活性，但不显著增加热休克蛋白 27 (HSP27) 和肾损伤分子 1 (KIM-1) 的表达。NOSO-502 的体外抗菌活性Citrobacter freundii DSM 30039Citrobacter kozeri DSM 4595Enterobacter aerogenes DSM 30053Enterobacter cloacae DSM 14563Escherichia coli ATCC 25922
MIC (μg/mL)22224
Klebsiella pneumoniae ATCC 43816Serratia marcescens DSM 17174Stenotrophomonas maltophilia ATCC 13637Staphylococcus aureus ATCC 29213Staphylococcus epidermidis ATCC 12228
MIC (μg/mL)141610.25
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