规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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体外研究 (In Vitro) |
RSV604 抑制噬菌斑减少实验中 EC50 范围为 0.5 至 0.9 μM 的四种实验室 RSV 菌株(RSS、Long、A2 和 B)的生长(5 天)[1]。 RSV604(6 天)的 EC50 为 0.86 μM,可防止 RSV 引起的 HEp-2 细胞死亡[1]。在 RSV 感染的 HEp-2 细胞中,RSV604(3 天)可减少病毒抗原合成,EC50 为 1.7 μM [1]。 RSV604(1-20 μM;7 天)以剂量依赖性方式抑制人气道上皮 (HAE) 细胞免受 RSV 感染,且未表现出任何细胞毒性、基底外侧液体渗漏至顶端表面或纤毛跳动频率改变 [1]。
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参考文献 | |
其他信息 |
RSV-604 is under investigation in clinical trial NCT00416442 (Safety, Tolerability and Pharmacokinetic Study of Single and Multiple Intravenous Doses of RSV604 in Healthy Subjects.).
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精确质量 |
388.134
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CAS号 |
676128-63-5
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相关CAS号 |
RSV604 racemate;676128-62-4;RSV604 (R enantiomer);932108-20-8
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PubChem CID |
5279172
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外观&性状 |
White to off-white solid powder
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LogP |
3.8
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tPSA |
82.59
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氢键供体(HBD)数目 |
3
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氢键受体(HBA)数目 |
4
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可旋转键数目(RBC) |
3
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重原子数目 |
29
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分子复杂度/Complexity |
634
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定义原子立体中心数目 |
1
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SMILES |
FC1=C([H])C([H])=C([H])C([H])=C1N([H])C(N([H])[C@]1([H])C(N([H])C2=C([H])C([H])=C([H])C([H])=C2C(C2C([H])=C([H])C([H])=C([H])C=2[H])=N1)=O)=O
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InChi Key |
MTPVBMVUENFFLL-HXUWFJFHSA-N
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InChi Code |
InChI=1S/C22H17FN4O2/c23-16-11-5-7-13-18(16)25-22(29)27-20-21(28)24-17-12-6-4-10-15(17)19(26-20)14-8-2-1-3-9-14/h1-13,20H,(H,24,28)(H2,25,27,29)/t20-/m1/s1
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化学名 |
(S)-1-(2-fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea
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别名 |
RSV-604 A-60444 RSV604 A60444 RSV 604 A 60444
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~100 mg/mL (~257.47 mM)
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (6.44 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (6.44 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (6.44 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00416442 | COMPLETED | Drug: RSV604 | Healthy | Novartis Pharmaceuticals | 2006-10 | Phase 1 |
NCT05913700 | RECRUITING | Respiratory Syncytial Virus (RSV) Acute Disease Respiratory Viral Infection | Institute for Clinical Effectiveness, Japan | 2023-07-01 |
Antiviral effect of delayed addition of inhibitor. Dose-dependent anti-RSV activities of RSV604 (A) and the fusion inhibitor BMS-433771 (B) were determined in vitro by plaque reduction assay; compounds were added either 2 h prior to infection (−2 h) or at 6 h postinfection (+6 h). The mean of duplicate wells per compound dilution was used to calculate the percent plaque reduction compared to compound-free, virus-infected control wells. Results shown are the means and SD for four independent experiments.[1].Chapman J, et al. RSV604, a novel inhibitor of respiratory syncytial virus replication. Antimicrob Agents Chemother. 2007 Sep;51(9):3346-53. td> |
Sensitivities of WT and RSV mutant viruses to RSV604. Dose-dependent anti-RSV activities of RSV604 were determined by plaque reduction assay. Results are representative of three independent experiments. Mean EC50 values (± SD) for RSV604 against WT and mutant viruses can be found in Table Table33.[1].Chapman J, et al. RSV604, a novel inhibitor of respiratory syncytial virus replication. Antimicrob Agents Chemother. 2007 Sep;51(9):3346-53. td> |
Dose-dependent inhibition of RSV replication in an in vitro model of human ciliated epithelium. RSV replication was measured visually by the expression of GFP from the virus genome (21). The top two panels show control cultures in the absence of drug. Compound (RSV604 or ribavirin) was added to the basolateral medium concomitantly with the virus at the concentrations indicated.[1].Chapman J, et al. RSV604, a novel inhibitor of respiratory syncytial virus replication. Antimicrob Agents Chemother. 2007 Sep;51(9):3346-53. td> |