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TP0480066
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TP0480066图片
CAS NO:2245693-15-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TP0480066 是一种具有选择性的topoisomerase II抑制剂,其对DNA gyrasetopo IVIC50值分别为 1.10 和 62.89 nM。TP0480066 对包括耐药菌株在内的多种细菌都具有较好的活性。TP0480066 也对N. gonorrhoeae具有较好的抑制活性,可用于淋病的研究。
生物活性

TP0480066 is a selectivetopoisomeraseIIinhibitor withIC50s of 1.10 and 62.89 nM forDNA gyraseandtopo IV, respectively. TP0480066 shows good activity of againsting variousbacterialspecies including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity toN. gonorrhoeae, can be used in study of gonorrhea[1][2].

IC50& Target

Topoisomerase II

 

DNA gyrase

1.10 nM (IC50)

topo IV

62.89 nM (IC50)

体外研究
(In Vitro)

TP0480066 (compound 32) (0-2048 μg/mL; 18-24 h) demonstrats favorable antimicrobial activities against various bacterial species including some clinically isolated drug-resistant strains : MRSA (n=24), gPRSP (n=30), and VRE (n=34)[1].
TP0480066 (0-2048 μg/mL; 18-24 h) shows good antibacterial activity againstClostridioides difficile[1].
TP0480066 (0-2048 μg/mL; 24-48 h) demonstrates potent antibacterial activity toN. gonorrhoeae, including strains with decreased susceptibility or resistance to currently available antimicrobial agents[2].
TP0480066 (1.25×10-4, 5×10-4and 2×10-3μg/mL; 24 h) shows good time-kill activity when concentration up to (or more than) MIC (5×10-4μg/mL) inN. gonorrhoeaeATCC 49226[2].

Cell Viability Assay[1]

Cell Line:Clinically isolated Methicillin-resistantS. aureus(24 strains), Vancomycin-resistantenterococci(E. faecium(29 strains) andE. faecalis(5 strains), vanA positive (18 strains), vanB positive (14 strains) and vanA/vanB negative (2 strains)), Genotype penicillin-resistantS. pneumonia(30 strains)
Concentration:0-2048 μg/mL
Incubation Time:18-24 h
Result:Showed favorable antimicrobial activities to drug-resistant strains with MIC ranges of 0.03-0.5, 0.015-0.25 and 0.002-0.015 μg/mL for MRSA (n=24), gPRSP (n=30), and VRE (n=34), respectively.

Cell Viability Assay[2]

Cell Line:N. gonorrhoeaeATCC (49226, 43069, BAA-1846, 700717, 700825),N. gonorrhoeaeNCTC (13477, 13478, 13479, 13480, 13481, 13482, 13483, 13818, 13821)
Concentration:0-2048 μg/mL
Incubation Time:24-48 h
Result:Exhibited significant antimicrobial activities to bothN. gonorrhoeaeand drug-resistantN. gonorrhoeae(MIC ranges both were ≤0.00012-0.0005 μg/mL)

Cell Viability Assay[2]

Cell Line:N. gonorrhoeaeATCC 49226
Concentration:1.25×10-4, 5×10-4and 2×10-3μg/mL
Incubation Time:24 h
Result:Reduced the viableN. gonorrhoeaeATCC 49226 counts by more than 3-log10CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively.
体内研究
(In Vivo)

TP0480066 (100 mg/kg; s.c; once) demonstrates Cmax, Tmax, t1/2, and AUC0-24 hvalues of 12400 ng/mL, 0.250 h, 6.79 h, 16000 hong/mL, respectively[2].
TP0480066 (1, 3, 10, 30, 100 mg/kg; s.c.; single) inhibits (30, 100 mg/kg) bothN. gonorrhoeaeATCC 49226 and NCTC 13479 at 24 h and in a dose-dependent manner in mice[2].

Animal Model:Female Slc:ICR mice[1]
Dosage:100 mg/kg
Administration:Subcutaneous injection, once.
Result:1.19Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3)[1].
Tmax(h)Cmax(ng/mL)AUC0-24(ng/mLoh)t1/2(h)
SC (100 mg/kg)0.25012400160006.79
Animal Model:Female BALB/c mice (6-week-old; genital tract infection model)[2]
Dosage:1, 3, 10, 30 and 100 mg/kg
Administration:Subcutaneous administration; single.
Result:Significantly decreased mean viable cell counts ofN. gonorrhoeaeATCC 49226 and NCTC 13479 when at 30, 100 mg/kg.
分子量

371.32

Formula

C18H14FN3O5

CAS 号

2245693-15-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.