Ro-0335
(Synonyms: Ro-0335) 目录号 : GC62223
An NNRTI and active metabolite of elsulfavirine
Cas No.:867365-76-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ro 0335 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and an active metabolite of the antiviral prodrug elsulfavirine.1 It inhibits HIV-1 reverse transcriptase in a cell-free assay and the replication of HIV-1 in MT-4 cells (IC50s = 8.1 and 1.1 nM, respectively). Ro 0335 also selectively inhibits human carbonic anhydrase VII (CAVII; Ki = 9.7 nM) over human CAI and CAIII-VI (Kis = >125 nM for all) but also inhibits human CAII, CAIX, CAXII, CAXIII, and CAXIV (Kis = 35.5, 72.1, 62.3, 52.2, and 15.4 nM, respectively).2
1.Javanbakht, H., Ptak, R., G., Chow, E., et al.In vitro resistance development for RO-0335, a novel diphenylether nonnucleoside reverse transcriptase inhibitorAntiviral Res.86(2)212-219(2010) 2.Supuran, C.T., Nocentini, A., Yakubova, E., et al.Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida?) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoformsJ. Enzyme Inhib. Med. Chem.36(1)1056-1060(2021)
| Cas No. | 867365-76-2 | SDF | |
| 别名 | Ro-0335 | ||
| 分子式 | C21H13BrCl2FN3O4S | 分子量 | 573.22 |
| 溶解度 | DMSO : 250 mg/mL (436.13 mM; Need ultrasonic) | 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 | 1.7445 mL | 8.7227 mL | 17.4453 mL |
| 5 mM | 0.3489 mL | 1.7445 mL | 3.4891 mL |
| 10 mM | 0.1745 mL | 0.8723 mL | 1.7445 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。
In vitro resistance development for Ro-0335, a novel diphenylether nonnucleoside reverse transcriptase inhibitor
Antiviral Res 2010 May;86(2):212-9.PMID:20219553DOI:10.1016/j.antiviral.2010.02.323
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are important components of current combination therapies for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. However, their low genetic barriers against resistance development, cross-resistance and serious side effects can compromise the benefits of the first generation compounds in this class (efavirenz and nevirapine). To study potential pathways leading to resistance against the novel diphenylether NNRTI, Ro-0335, sequential passage experiments at low multiplicity of infection (MOI) were performed to solicit a stepwise selection of resistance mutations. Two pathways to loss of susceptibility to Ro-0335 were observed, containing patterns of amino acid changes at either V106I/A plus F227C (with additional contributions from A98G, V108I, E138K, M230L and P236L) or V106I/Y188L (with a potential contribution from L100I, E138K and Y181C). Characterization of the observed mutations by site-directed mutagenesis in the isogenic HXB2D background demonstrated that a minimum of two or more mutations were required for significant loss of susceptibility, with the exception of Y188L, which requires a two-nucleotide change. Patterns containing F227C or quadruple mutations selected by Ro-0335 showed a low relative fitness value when compared to wild-type HXB2D.