Tomeglovir (BAY 38-4766)
(Synonyms: 托美洛韦; BAY 38-4766) 目录号 : GC32345
Tomeglovir (BAY 38-4766) 是一种有效的抗 CMV 剂，抑制病毒 DNA 多联体的加工，HCMV 和 MCMV 的 IC50 值为 0.34 μM 和 0.039 μM。
Cas No.:233254-24-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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 × 103 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]. |
Animal experiment: | Mice[1]NOD/LtSz-scid/j mice, 20-30 g body weight, are anesthesized 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]. |
References: [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. | |
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
Tomeglovir (BAY 38-4766) is a potent anti-CMV agent, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV. Tomeglovir also suppresses HELF and NIH 3T3 cells, with CC50s of 85 μM and 62.5 μM, respectively[1]. Tomeglovir (BAY 38-4766) inhibits HCMV Davis and various monkey CMV strains with EC50s of 1.03 ± 0.57 μM and < 1 μM[2].
Tomeglovir (BAY 38-4766; 3, 10, 30, 100 mg/kg, p.o.) dose-dependently reduces MCMV-DNA in salivary glands, livers 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 (BAY 38-4766) shows antiviral activity in SCID mice with MCMV, and the LD50 is >2000 mg/kg in mice and rats[2].
[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.
| Cas No. | 233254-24-5 | SDF | |
| 别名 | 托美洛韦; BAY 38-4766 | ||
| Canonical SMILES | CC(C)(CO)C(NC1=CC=C(NS(=O)(C2=C3C=CC=C(N(C)C)C3=CC=C2)=O)C=C1)=O | ||
| 分子式 | C23H27N3O4S | 分子量 | 441.54 |
| 溶解度 | DMSO : ≥ 108 mg/mL (244.60 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2648 mL | 11.324 mL | 22.648 mL |
| 5 mM | 0.453 mL | 2.2648 mL | 4.5296 mL |
| 10 mM | 0.2265 mL | 1.1324 mL | 2.2648 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Comparison of Cytomegalovirus Terminase Gene Mutations Selected after Exposure to Three Distinct Inhibitor Compounds
Antimicrob Agents Chemother 2017 Oct 24;61(11):e01325-17.PMID:28827420DOI:PMC5655092
Letermovir, GW275175X (a benzimidazole), and Tomeglovir (Bay38-4766) are chemically unrelated human cytomegalovirus (CMV) terminase complex inhibitors that have been tested in human subjects. UL56 gene mutations are the dominant pathway of letermovir resistance, while UL89 and UL56 mutations are known to confer benzimidazole resistance. This study compares the mutations elicited by the three inhibitors during in vitro CMV propagation. GW275175X consistently selected for UL89 D344E and sometimes selected for UL89 C347S, UL89 R351H, or UL56 Q204R. Tomeglovir consistently selected for UL89 V362M and sometimes selected for UL89 N329S, T350M, H389N, or N405D or UL56 L208M, E407D, H637Q, or V639M. Adding to known and novel UL56 mutations, letermovir occasionally selected for UL89 N320H, D344E, or M359I. Recombinant phenotyping confirmed that UL89 D344E conferred 9-fold resistance (an increased 50% effective concentration [EC50]) for GW275175X and increased the letermovir and Tomeglovir EC50s by 1.7- to 2.1-fold for the baseline virus and the UL56 Q204R, E237D, F261L, and M329T mutants. UL89 N320H and M359I conferred <2-fold letermovir resistance but 7-fold Tomeglovir resistance; the N320H mutant was also 4-fold resistant to GW275175X. UL89 N329S conferred Tomeglovir and letermovir cross-resistance. UL89 T350M conferred resistance to all three inhibitors. UL89 C347S conferred 27-fold GW275175X resistance. UL89 V362M and H389N conferred 98-fold and 29-fold Tomeglovir resistance, respectively, without conferring cross-resistance. Thus, characteristic UL89 mutations confer substantial resistance to GW275175X and Tomeglovir and are an uncommon accessory pathway of letermovir resistance. Instances of moderate cross-resistance and the proximity of the selected UL89 and UL56 mutations suggest targeting of a similar terminase functional locus involving UL56 and UL89 interaction.