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Tomeglovir

Tomeglovir

产品编号 TQ0030   CAS 233254-24-5
别名: 托美洛韦, BAY 38-4766

Tomeglovir is a potent anti-CMV agent, inhibiting the processing of viral DNA-concatemers (IC50s: 0.34/0.039 μM for HCMV and MCMV).

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Tomeglovir Chemical Structure
Tomeglovir, CAS 233254-24-5
规格 价格/CNY 货期 数量
2 mg ¥ 542 5日内发货
5 mg ¥ 913 6-8周
10 mg ¥ 1,410 6-8周
100 mg ¥ 6,490 6-8周
1 mL * 10 mM (in DMSO) ¥ 983 6-8周
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产品目录号及名称: Tomeglovir (TQ0030)
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参考文献
产品描述 Tomeglovir is a potent anti-CMV agent, inhibiting the processing of viral DNA-concatemers (IC50s: 0.34/0.039 μM for HCMV and MCMV).
靶点活性 HCMV:0.34 μM, MCMV:0.039 μM
体外活性 Tomeglovir suppresses HELF and NIH 3T3 cells (CC50s: 85 μM/62.5 μM) [1]. Tomeglovir inhibits HCMV Davis and various monkey CMV strains with EC50s of 1.03 μM and < 1 μM [2].
体内活性 Tomeglovir (3, 10, 30, 100 mg/kg, p.o.) dose-dependently reduces MCMV-DNA in livers, salivary glands and kidneys of MCMV-infected NOD-SCID mice, and prolongs the survival of the mice. Tomeglovir (10, 25 and 50 mg/kg) shows antiviral activity in the hollow fiber mouse model [1]. Tomeglovir shows antiviral activity in SCID mice with MCMV, and the LD50 is >2000 mg/kg in mice and rats [2].
细胞实验 In order to evaluate drug toxicity, 96-well microtitre plates are prepared with 100 μL of EMEM/10 per well. After addition of 2 μL of 50 mM Tomeglovir stock solutions in duplicate into 198 μL in row 2, serial two-fold dilutions are made with 100 μL up to row 12 and 100 μL of a HELF, NHDF or 3T3 cell suspension (5 × 10^3 cells/mL) are added per well. Row 1 serves as an untreated cell control. After incubation for 6 days at 37°C and 5% CO2, the cells are washed once with phosphate-buffered saline (PBS), and 200 μL of a 10 μg/mL fluorescent dye solution in PBS, pH 7.2 (fluorescein diacetate) are dispensed per well. After 45 min, the fluorescence signal is measured with a Fluorskan Ascent fluorimeter (excitation filter 485 ± 11 nm, emission filter 530 ± 15 nm). The relative fluorescence units (RFUs) of treated cells are expressed as percentages of untreated cell controls and CC50 values are determined graphically [2].
动物实验 NOD/LtSz-scid/j mice, 20-30 g body weight, are anesthetized with 0.015-0.017 mL/g body weight Avertin 2.5% (Avertin 100% consists of 10 g tribromoethyl alcohol in 10 mL tertiary amyl alcohol). After shaving and cleaning the belly aseptically, the abdomens are opened and the fibers inserted intra-abdominally. The abdomens are closed with two suture layers. Only asymptomatic animals are included in the study. Starting 1 day after transplantation, the mice are treated with the Tomeglovir at indicated dosages twice daily for four consecutive days per os. In preliminary experiments, viral peak titers are observed on day 5 under these conditions [1].
别名 托美洛韦, BAY 38-4766
分子量 441.54
分子式 C23H27N3O4S
CAS No. 233254-24-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 105 mg/mL (237.81 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2648 mL 11.324 mL 22.648 mL 56.62 mL
5 mM 0.453 mL 2.2648 mL 4.5296 mL 11.324 mL
10 mM 0.2265 mL 1.1324 mL 2.2648 mL 5.662 mL
20 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.831 mL
50 mM 0.0453 mL 0.2265 mL 0.453 mL 1.1324 mL
100 mM 0.0226 mL 0.1132 mL 0.2265 mL 0.5662 mL

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TargetMol Library Books参考文献

1. Weber O, et al. Inhibition of murine cytomegalovirus and human cytomegalovirus by a novel non-nucleosidic compound in vivo. Antiviral Res. 2001 Mar;49(3):179-89. 2. Reefschlaeger J, et al. Novel non-nucleoside inhibitors of cytomegaloviruses (BAY 38-4766): in vitro and in vivo antiviral activity and mechanism of action. J Antimicrob Chemother. 2001 Dec;48(6):757-67.
PSI-6206 Methyl 2-amino-5-bromobenzoate MK-8325 Ruzasvir FGI-106 tetrahydrochloride Maribavir U18666A Tris(4-aminophenyl)methane

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Keywords

Tomeglovir 233254-24-5 Microbiology/Virology Proteases/Proteasome HCV Protease 托美洛韦 BAY 38-4766 Inhibitor inhibitor inhibit

 

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