计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
VV116 (JT001) is a deuterated version of Remdesivir , a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus ( RSV ). VV116 retains the antiviral activity of Remdesivir against COVID-19 , and is the first domestically produced deuterium targeting the COVID-19
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs. Potential advantages of deuterated compounds: (1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration. (2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance. (3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism. (4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe. (5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay Cell Line: A549 (infected with RSV)Concentration: 0-1000 μM Incubation Time: 48 hours Result: Inhibited RSV replication in A549 cells with EC 50 of 1.20 ± 0.32 μM, CC 50 of 95.92 ± 9.27 μM and selectivity index (SI) of 80.
In Vivo
VV116 (25, 50 and 100 mg/kg; PO; b.i.d for 4 days) exhibits a stronger activity and decreases the virus titers below the detection limit at 50 mg/kg, also reduces lung injury after RSV infection . VV116 (25, 50 and 100 mg/kg; PO; single dosage) exhibits favorable PK properties and good safety profile . Pharmacokinetic Parameters of VV116 (JT001) in Balb/c mice . PO (25 mg/kg) PO (50 mg/kg) PO (100 mg/kg) T max (h) 0.42 ± 0.14 0.42 ± 0.14 0.42 ± 0.14 C max (ng/mL) 5360 ± 560 11617 ± 3443 24017 ± 6521 AUC 0-t (ng/mL·h) 11461 ± 1013 24594 ± 1059 47799 ± 6545 AUC 0-∞ (ng/mL·h) 11534 ± 992 24739 ± 1028 48014 ± 6696 MRT 0-∞ (ng/mL·h) 2.25 ± 0.32 2.15 ± 0.26 2.28 ± 0.53 T max (h) 2.30 ± 1.10 3.27 ± 1.92 4.25 ± 0.53 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c mice Dosage: 25, 50 and 100 mg/kg Administration: PO; single dosage (Pharmacokinetics Analysis) Result: Exhibited favorable PK properties and good safety profile. Animal Model: Balb/c mice (6-8 weeks; intranasally infected with 4 × 10^6 FFU of RSV) Dosage: 25, 50 and 100 mg/kg Administration: PO; b.i.d for 4 days Result: Exhibited a stronger activity and decreased the virus titers below the detection limit at 50 mg/kg, also reduced lung injury after RSV infection.
Form:Solid
IC50& Target:SARS-CoV-2, RSV
规格
规格或纯度
≥99%
英文名称
VV116
生化机理
VV116 (JT001) 是 Remdesivir ( HY-104077 ) 的氚化物，Remdesivir ( HY-104077 ) 是一种针对 SARS-CoV-2 和呼吸道合胞病毒（RSV）的高活性口服核苷类抗病毒药物。VV116 保留了 Remdesivir 对 COVID-19 的抗病毒活性，是目前世界上第一款可用于 SARS-CoV-2 和呼吸道合胞病毒（RSV）的口服核苷类抗病毒药物。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
[2H]C1=C2C(=NC=NN2C(=C1)[C@]3([C@@H]([C@@H]([C@H](O3)COC(=O)C(C)C)OC(=O)C(C)C)OC(=O)C(C)C)C#N)N.Br
Isomeric SMILES
[2H]C1=C2C(=NC=NN2C(=C1)[C@]3([C@@H]([C@@H]([C@H](O3)COC(=O)C(C)C)OC(=O)C(C)C)OC(=O)C(C)C)C#N)N.Br
PubChem CID
分子量
583.45
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 250 mg/mL (428.49 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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