Софосбувир
|
1190307-88-0
|
- CAS №
- 1190307-88-0
- Химическое название:
- Софосбувир
- английское имя:
- Sofosbuvir
- Синонимы:
- Suofeibuwei;(S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyriMidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-Methyltetrahydrofuran-2-yl)Methoxy)(phenoxy)phosphoryl)aMino)propanoate;Sophy Bouvet;propan-2-yl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate;propan-2-yl (2S)-2-[[[(2R,3R,4R,5S)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate;Isopropyl (2S)-2-{[(S)-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl)-4-fluoro-3-hydroxy-4-methyltetrahydro-2-furanyl]methoxy}(phenoxy)phosphoryl]amino}propanoate;GS-7977;PSI 7977;Sofosbubir;sofosbuvir
- CBNumber:
- CB02604350
- Формула:
- C22H29FN3O9P
- молекулярный вес:
- 529.45
- MOL File:
- 1190307-88-0.mol
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Софосбувир атрибут
| Температура плавления: |
122-124°C |
| плотность: |
1.41 |
| температура хранения: |
Hygroscopic, -20°C Freezer, Under inert atmosphere |
| растворимость: |
ДМСО (Мало растворим), метанол (Мало растворим) |
| форма: |
Твердый |
| пка: |
9.39±0.10(Predicted) |
| цвет: |
белый |
| ИнЧИКей: |
TTZHDVOVKQGIBA-YBSJRAAASA-N |
| SMILES: |
C(OC(C)C)(=O)[C@@H](N[P@@](OC[C@@H]1[C@@H](O)[C@](F)(C)[C@H](N2C(=O)NC(=O)C=C2)O1)(OC1=CC=CC=C1)=O)C |
| Справочник по базе данных CAS: |
1190307-88-0 |
| FDA UNII: |
WJ6CA3ZU8B |
| Словарь наркотиков NCI: |
sofosbuvir |
| Код УВД: |
J05AP08 |
безопасность
- Заявления о рисках и безопасности
- код информации об опасности(GHS)
| символ（GHS） |
 
|
| сигнальное слово |
Warning |
| Заявление об опасности |
| пароль |
Заявление об опасности |
Класс опасности |
категория |
сигнальное слово |
пиктограмма |
предупреждение |
| H373 |
Может поражать органы (Нервная система) в результате
многократного или продолжительного воздействия при
вдыхании. |
Специфическая органная токсичность, многократное воздействие |
Категория 2 |
Предупреждение |
|
P260, P314, P501 |
|
| Внимание |
| P260 |
Не вдыхать газ/ пары/ пыль/ аэрозоли/ дым/ туман. |
| P314 |
В случае плохого самочувствия обратиться к врачу. |
| P501 |
Удалить содержимое/ контейнер на утвержденных станциях
утилизации отходов. |
|
Софосбувир химические свойства, назначение, производство
Описание
Sofosbuvir is a drug used for the treatment of hepatitis C. It is recommended to be used in combination with other drugs (such as velpatasvir) for the first-line treatment for HCV genotypes 1, 2, 3, 4, 5, and 6. It takes effect through acting as a nucleotide analog inhibitor, being capable of specially inhibiting the HCV NS5B (non-structural protein 5B) RNA-dependent RNA polymerase.
Использование
PSI-7977 is a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate and is currently being investigated in phase 3 clinical trials for the t
reatment of hepatitis C. Studies have profiled PSI-7977 as a nucleotide inhibitor of hepatitis C virus, exerting selective inhibitory effects towards HCV NS5B polymerase.
Определение
ChEBI: A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.
Клиническое использование
In December 2013, sofosbuvir (also known as GS-7977 and PSI-7977) was approved in the United States for the treatment of hepatitis C virus (HCV) infection as a component of a combination antiviral treatment regimen. Sofosbuvir was discovered from an effort to enhance the activity of the parent nucleoside by bypassing rate-limiting monophosphorylation with a prodrug that would liberate the intactmonophosphate in the liver, where it would then be converted by cellular kinases to the active triphosphate species. In addition, the prodrug was designed to be amenable to oral delivery. In the initial synthesis of sofosbuvir, the iso-propyl ester of (L)-alanine was coupled with phenyl dichlorophosphate to provide a diastereomeric intermediate that was coupled with the uridine nucleoside. The diastereomeric mixture (GS-9851) was shown to produce high levels of triphosphate in vitro in primary hepatocytes and in the livers of rats, dogs, and monkeys after oral dosing. The individual diastereomers were obtained by chromatography or by crystallization. The diastereomer with the Sp configuration at the phosphorous center (sofosbuvir) was found to be >10-fold more potent in an HCV replicon assay than the corresponding Rp diastereomer (EC90s of 0.42 and 7.5 μM, respectively).
Софосбувир препаратная продукция и сырье
сырьё
препарат
Софосбувир поставщик
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