クレブジン
クレブジン 物理性質
- 融点 :
- 184-185°
- 比旋光度 :
- D25 -111.77° (c = 0.23 in methanol)
- 比重(密度) :
- 1.55±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- under inert gas (nitrogen or Argon) at 2-8°C
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 外見 :
- 個体
- 酸解離定数(Pka):
- 9.55±0.10(Predicted)
- 色:
- 白い
- CAS データベース:
- 163252-36-6
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 毒性 |
LD50 in mice, rats (mg/kg): >5000, >3000 orally (Painter) |
|
|
| 絵表示（GHS） |
|
| 注意喚起語 |
警告 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
|
P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
| H332 |
吸入すると有害 |
急性毒性、吸入 |
4 |
警告 |
|
P261, P271, P304+P340, P312 |
| H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
|
|
|
| 注意書き |
| P280 |
保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
| P310 |
ただちに医師に連絡すること。 |
|
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQB-1067 |
クレブジン
Clevudine |
163252-36-6 |
100mg |
￥41000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01COBQB-1067 |
クレブジン
Clevudine |
163252-36-6 |
250mg |
￥95000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TRCC574150 |
クレブジン
Clevudine |
163252-36-6 |
10mg |
￥23700 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TRCC574150 |
クレブジン
Clevudine |
163252-36-6 |
50mg |
￥29100 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TRCC574150 |
クレブジン
Clevudine |
163252-36-6 |
100mg |
￥44100 |
2024-03-01 |
購入 |
クレブジン 化学特性,用途語,生産方法
効能
抗ウイルス薬, 逆転写酵素阻害薬
説明
Clevudine is a fluorinated b-L-nucleoside analog launched for the
oral treatment of chronic HBV infection. It is the fifth nucleoside or nucleotide
analog to be marketed for this indication. The previous drugs from this class
include lamivudine, adefovir, entecavir, and telbivudine. In HBV-expressing
human hepatoma cell line 2.2.15, clevudine inhibits HBV DNA synthesis with
an EC
50 of 0.1 μM, and does not show cytotoxicity up to 200 μM. It is
phosphorylated by cellular kinases to the active triphosphate derivative,
which subsequently inhibits HBV DNA polymerase and HBV replication.
466 Shridhar Hegde and Michelle Schmidt
Clevudine-5′-triphosphate has an intracellular half-life of 16.5 h. Interestingly, it
is a non-competitive inhibitor of viral polymerase, and inhibits HBV replication
without being incorporated into the DNA. The pharmacokinetic profile of clevudine was linear with a plasma half-life of approximately 60 h. Clevudine was undetectable in plasma after 4 weeks following the cessation of dosing.The most common adverse events reported with clevudine treatment include infection, asthenia, dyspepsia, abdominal pain, headache, and diarrhea.
Clevudine is chemically derived from L-ribose by first incorporating acyl protective groups to produce 1-O-acetyl-2,3,5-tri-O-benzoyl-b-L-ribofuranose intermediate, which is then converted to 1,3,5-tri-O-benzoyl-a-L-ribofuranose in two steps by treating To Market, To Market 2007 467 with hydrogen chloride and subsequent hydrolysis and acyl migration. The remaining steps leading to clevudine include conversion of the C2-hydroxy group to C2-fluoro group with triethylamine trihydrofluoride, formation of the corresponding ribofuranosyl bromide intermediate with hydrogen bromide and acetic acid, condensation with silylated thymine, and removal of benzoyl protective groups with methanolic ammonia.
化学的特性
White Solid
使用
Antiviral drug, used for the treatment of Hepatitis B.
クレブジン 上流と下流の製品情報
原材料
準備製品
クレブジン 生産企業
Global( 170)Suppliers
163252-36-6(クレブジン)キーワード:
- 163252-36-6
- 1-[(2S,3R,4S,5S)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-methyl-pyrimidine-2,4-dione
- CLEVUDINE
- 1-(2'-DEOXY-2'-FLUORO-BETA-L-ARABINOFURANOSYL)-5-METHYLURACIL
- 1-[(2S,3R,4S,5S)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
- 2'-Fluoro-5-methylarabinosyluracil
- Levovir
- 1-(2''-DEOXY-2''-FLUORO--L-ARABINOFURANOSYL)-5-METHYLURACIL
- CLEVUDINE: 1-(2''-DEOXY-2''-FLUORO-BETA-L-ARABINOFURANOSYL)-5-METHYLURACIL
- CLEVUDINE: 1-(2''-DEOXY-2''-FLUORO-SS-L-ARABINOFURANOSYL)-5-METHYLURACIL
- CLEVUDINE, 1-(2'-DEOXY-2'-FLUORO-β-L-ARABINOFURANOSYL)-5-METHYLURACIL
- 1-[(2S,3R,4S,5S)-3-fluoro-4-hydroxy-5-methylol-tetrahydrofuran-2-yl]-5-methyl-pyrimidine-2,4-quinone
- 1-(2-Deoxy-2-fluoro-β-L-arabinofuranosyl)-5-Methyl-2,4(1H,3H)-pyriMidinedione
- L-FMAU
- Clevudine(Levovir)
- 1-((2S,3R,4S,5S)-3-Fluoro-4-hydroxy-5-(hydroxyMethyl)tetrahydrofuran-2-yl)-5-MethylpyriMidine-2,4(1H,3H)-dione
- 1-((2S,3R,4S,5S)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4
- 1-((2S,3R,4S,5S)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-
- 2'-F-2'-ara-dT
- 2,4(1H,3H)-Pyrimidinedione, 1-(2-deoxy-2-fluoro-β-L-arabinofuranosyl)-5-methyl-
- Clevudine USP/EP/BP
- 1-[(2S,3R,4S,5S)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)-2-tetrahydrofuryl]-5-methylpyrimidine-2,4(1H,3H)-dione
- Clevudine
CAS
- Clevudine, 10 mM in DMSO
- クレブジン
- 1-(2-デオキシ-2-フルオロ-β-L-アラビノフラノシル)-5-メチルウラシル
- 1-(2-フルオロ-2-デオキシ-β-L-アラビノフラノシル)チミン
- L-FMAU
- 1-[(2S,3R,4S,5S)-3-フルオロ-4-ヒドロキシ-5-(ヒドロキシメチル)オキソラン-2-イル]-5-メチル-1,2,3,4-テトラヒドロピリミジン-2,4-ジオン