化合物 TP0480066|T61481|TargetMol

價(jià)格	￥13800	￥10600	￥17500
包裝	50mg	25mg	100mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:化合物 TP0480066	英文名稱:TP0480066
CAS:2245693-15-4	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號(hào): T61481

Product Introduction

Bioactivity

名稱	TP0480066
描述	TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].
體外活性	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 against Clostridioides difficile [1]. TP0480066 (0-2048 μg/mL; 24-48 h) demonstrates potent antibacterial activity to N. gonorrhoeae, including strains with decreased susceptibility or resistance to currently available antimicrobial agents [2]. TP0480066 (1.25×10 -4, 5×10 -4 and 2×10 -3 μg/mL; 24 h) shows good time-kill activity when concentration up to (or more than) MIC (5×10 -4 μg/mL) in N. gonorrhoeae ATCC 49226 [2]. Cell Viability Assay [1] Cell Line: Clinically isolated Methicillin-resistant S. aureus (24 strains), Vancomycin-resistant enterococci ( E. faecium (29 strains) and E. faecalis (5 strains), vanA positive (18 strains), vanB positive (14 strains) and vanA/vanB negative (2 strains)), Genotype penicillin-resistant S. 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. gonorrhoeae ATCC (49226, 43069, BAA-1846, 700717, 700825), N. gonorrhoeae NCTC (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 both N. gonorrhoeae and drug-resistant N. gonorrhoeae (MIC ranges both were ≤0.00012-0.0005 μg/mL) Cell Viability Assay [2] Cell Line: N. gonorrhoeae ATCC 49226 Concentration: 1.25×10 -4, 5×10 -4 and 2×10 -3 μg/mL Incubation Time: 24 h Result: Reduced the viable N. gonorrhoeae ATCC 49226 counts by more than 3-log 10 CFU/mL (99.9%) after 6 h at 4× MIC and after 24 h at the MIC, respectively.
體內(nèi)活性	TP0480066 (100 mg/kg; s.c; once) demonstrates C max, T max, t 1/2, and AUC 0-24 h values of 12400 ng/mL, 0.250 h, 6.79 h, 16000 h ng/mL, respectively [2]. TP0480066 (1, 3, 10, 30, 100 mg/kg; s.c.; single) inhibits (30, 100 mg/kg) both N. gonorrhoeae ATCC 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: 1.19 Pharmacokinetic Parameters of TP0480066 in Female Slc:ICR mice (n=3) [1]. T max (h) C max (ng/mL) AUC 0-24 (ng/mL h) t 1/2 (h) SC (100 mg/kg) 0.250 12400 16000 6.79 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 of N. gonorrhoeae ATCC 49226 and NCTC 13479 when at 30, 100 mg/kg.
存儲(chǔ)條件	Shipping with blue ice.

關(guān)鍵字： TP0480066|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊(cè)資本	589.8595萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù)	經(jīng)營(yíng)模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：589.8595萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：抑制劑&激動(dòng)劑，天然產(chǎn)物，重組蛋白，化合物庫(kù)，技術(shù)服務(wù)
公司地址：上海市靜安區(qū)江場(chǎng)三路238號(hào)8樓

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