サニルブジン

サニルブジン 化学構造式
3056-17-5
CAS番号.
3056-17-5
化学名:
サニルブジン
别名:
2',3'-ジデヒドロ-3'-デオキシチミジン;ゼリット;1-(2,3-ジデオキシ-β-D-glycero-ペンタ-2-エノフラノシル)-5-メチルウラシル;1-[5β-(ヒドロキシメチル)-2,5-ジヒドロフラン-2β-イル]チミン;1-[2,5-ジヒドロ-5β-(ヒドロキシメチル)フラン-2β-イル]チミン;3'-デオキシ-2',3'-ジデヒドロチミジン;1-(2,3-ジデオキシ-β-D-glycero-2-ペンテノフラノシル)チミン;1-[(2R,5S)-5-(ヒドロキシメチル)-2,5-ジヒドロフラン-2-イル]チミン;1-[[(2R,5S)-2,5-ジヒドロ-5-(ヒドロキシメチル)フラン]-2-イル]チミン;サニルブジン;1-[[2,5-ジヒドロ-5β-(ヒドロキシメチル)フラン]-2β-イル]-5-メチルピリミジン-2,4(1H,3H)-ジオン;スタブジン;D-4T【ヌクレオシド】;2',3'-ジデヒドロ-2',3'-ジデオキシチミジン;2',3'-ジデオキシチミジエン;2',3'-アンヒドロチミジン;2′,3′-ジデヒドロ-3′-デオキシチミジン;サニルブジン (JAN);3′-デオキシ-2′,3′-ジデヒドロチミジン;2′,3′-ジデオキシチミジエン
英語名:
Stavudine
英語别名:
D4T;ZERIT;Stavir;Avostav;Virostav;STAVUDINE;BMY-27857;NSC 163661;Stauvidine;sanilvudine
CBNumber:
CB4450928
化学式:
C10H12N2O4
分子量:
224.21
MOL File:
3056-17-5.mol
MSDS File:
SDS

サニルブジン 物理性質

融点 :
159-160°C
比旋光度 :
D25 -39.4° (c = 0.701 in water); D20 -46.1° (c = 0.7 in water)
比重(密度) :
1.374±0.06 g/cm3(Predicted)
屈折率 :
-46 ° (C=0.69, H2O)
貯蔵温度 :
-20°C
溶解性:
水に溶けやすく、エタノール (96%) に溶けにくく、ジクロロメタンに溶けにくい。
酸解離定数(Pka):
9.47±0.10(Predicted)
色:
白い
水溶解度 :
21℃で5~10g/100mL
BCS Class:
1,3
安定性::
安定。可燃性。強力な酸化剤とは相容れない。
InChIKey:
XNKLLVCARDGLGL-JGVFFNPUSA-N
CAS データベース:
3056-17-5(CAS DataBase Reference)
EPAの化学物質情報:
Thymidine, 2',3'-didehydro-3'-deoxy- (3056-17-5)
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)
主な危険性  Xi
Rフレーズ  36/37/38
Sフレーズ  26-36
WGK Germany  2
RTECS 番号 XP2075000
HSコード  29349990
有毒物質データの 3056-17-5(Hazardous Substances Data)
毒性 LD50 oral in rat: 4gm/kg
絵表示(GHS) GHS hazard pictograms
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
H341 遺伝性疾患のおそれの疑い 生殖細胞変異原性 2 警告 P201,P202, P281, P308+P313, P405,P501
注意書き
P201 使用前に取扱説明書を入手すること。
P202 全ての安全注意を読み理解するまで取り扱わないこ と。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P308+P313 暴露または暴露の懸念がある場合:医師の診断/手当てを 受けること。
P405 施錠して保管すること。
P501 内容物/容器を...に廃棄すること。

サニルブジン 価格 もっと(26)

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) W01LKTS7603 スタブジン
Stavudine
3056-17-5 100mg ¥10200 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01LKTS7603 スタブジン
Stavudine
3056-17-5 1g ¥52800 2024-03-01 購入
東京化成工業 D3580 2',3'-ジデヒドロ-3'-デオキシチミジン >98.0%(HPLC)(T)
2',3'-Didehydro-3'-deoxythymidine >98.0%(HPLC)(T)
3056-17-5 1g ¥6600 2024-03-01 購入
東京化成工業 D3580 2',3'-ジデヒドロ-3'-デオキシチミジン >98.0%(HPLC)(T)
2',3'-Didehydro-3'-deoxythymidine >98.0%(HPLC)(T)
3056-17-5 5g ¥21000 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) PHR3447 2′,3′-ジデヒドロ-3′-デオキシチミジン certified reference material, pharmaceutical secondary standard
certified reference material, pharmaceutical secondary standard
3056-17-5 500MG ¥22800 2024-03-01 購入

サニルブジン MSDS


3'-Deoxy-2',3'-didehydrothymidine

サニルブジン 化学特性,用途語,生産方法

外観

白色~ほとんど白色粉末~結晶

効能

抗ウイルス薬, 逆転写酵素阻害薬

説明

Stavudine, a dideoxynucleoside analog of thymidine, has been introduced in the U.S.A. for the treatment of late-stage AIDS patients who are refractory to other AIDS treatments. Similar as other currently available agents for AIDS treatment such as zidovudine (AZT), didanosine, and zalcitabine, the anti-HIV activity of these 2'3'- dideoxynucleosides is ascribed to the inhibitory effect of their corresponding 5'- triphosphates against the HlVsncoded RNAdependent DNA polymerase (reverse transcriptase). While some of these drugs have rapid development of drug resistance, stavudine is active against AZT-resistant HIV strains. It has a favorable pharmacokinetic profile with more complete and less variable oral absorption than AZT and didanosine and has a bioavailability of 80-90%.

化学的特性

Colourless solid

使用

Stavudine (Zidovudine EP Impurity A) is used as an antiviral. A reverse transcriptase inhibitor.

適応症

Stavudine (d4T, Zerit) is a thymidine nucleoside analogue that is active against HIV-1 and HIV-2. It is approved for the therapy of HIV infection as part of a multidrug regimen and is also used for postexposure prophylaxis.

定義

ChEBI: A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase

抗菌性

Stavudine is active against HIV-1, HIV-2 and HTLV-1.

獲得抵抗性

Resistance to stavudine is identical to that seen for zidovudine. Mutations at positions 41, 67 and 70, and positions 210, 215 and 219 (the ‘thymidine analog mutations’) of the reverse transcriptase genes are associated with diminished antiretroviral efficacy.

一般的な説明

Stavudine, 2'3'-didehydro-2'-deoxythymidine (D4T, Zerit), isan unsaturated pyrimidine nucleoside that is related to thymidine.The drug inhibits the replication of HIV by a mechanismsimilar to that of its close congener, AZT.Stavudine is bioactivatedby cellular enzymes to a triphosphate.
Stavudine is available as capsules for oral administration.The drug is acid stable and well absorbed (about 90%) followingoral administration. Stavudine has a short half-life(1–2 hours) in plasma and is excreted largely unchanged(85%–90%) in the urine.As with ddC, the primary doselimitingeffect is peripheral neuropathy.
Stavudine isrecommended for the treatment of adults with advancedHIV infection who are intolerant of other approved therapiesor who have experienced clinical or immunological deteriorationwhile receiving these therapies.

空気と水の反応

Water soluble.

反応プロフィール

Stavudine is sensitive to heat. Incompatible with strong oxidizing agents .

危険性

Moderately toxic by ingestion.

火災危険

Literature sources indicate that Stavudine is combustible.

応用例(製薬)

An analog of thymidine formulated for oral administration.

薬物動態学

Oral absorption: 86%
Cmax 40 mg twice daily: 0.54 mg/L
Plasma half-life: 1.4 h
Volume of distribution: 0.66 L/kg
Plasma protein binding: <5%
Absorption and distribution
It is rapidly absorbed with or without food. CNS penetration is moderate. The estimated semen:plasma ratio is >1. It is secreted into breast milk.
Metabolism and excretion
The metabolic fate in humans has not been elucidated. Renal elimination accounts for approximately 40% of overall clearance at a rate almost twice that of endogenous creatinine, indicating glomerular filtration and active tubular secretion. Clearance decreases as creatinine clearance decreases and the dosage should be adjusted in patients with reduced renal function. Pharmacokinetics are not significantly altered in patients with hepatic impairment.

臨床応用

Treatment of HIV infection in adults and children

副作用

The adverse effects with which stavudine is most frequently associated are headache, diarrhea, skin rash, nausea, vomiting, insomnia, anorexia, myalgia, and weakness. Peripheral neuropathy consisting of numbness, tingling, or pain in the hands or feet is also common with higher doses of the drug. Significant elevation of hepatic enzymes may be seen in approximately 10 to 15% of patients. Lactic acidosis occurs more frequently with stavudine than with other NRTIs. Viral resistance to stavudine may develop, and cross-resistance to zidovudine and didanosine may occur.

予防処置

Stavudine possesses several clinically significant interactionswith other drugs. Although hydroxyurea enhancesthe antiviral activity of stavudine and didanosine,combination therapy that includes stavudine anddidanosine, with or without hydroxyurea, increases therisk of pancreatitis. Combinations of stavudine and didanosineshould not be given to pregnant women becauseof the increased risk of metabolic acidosis.Zidovudine inhibits the phosphorylation of stavudine;thus, this combination should be avoided.

サニルブジン 上流と下流の製品情報

原材料

準備製品


サニルブジン 生産企業

Global( 499)Suppliers
名前 電話番号 電子メール 国籍 製品カタログ 優位度
Hebei Mojin Biotechnology Co., Ltd
+8613288715578
sales@hbmojin.com China 12452 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21700 55
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD
+86 18953170293
sales@sdzschem.com China 2931 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58
Accela ChemBio Inc.
(+1)-858-699-3322
info@accelachem.com United States 19965 58
Hebei Guanlang Biotechnology Co., Ltd.
+86-19930503282
alice@crovellbio.com China 8823 58
Xiamen AmoyChem Co., Ltd
+86-592-6051114 +8618959220845
sales@amoychem.com China 6387 58
Hubei xin bonus chemical co. LTD
86-13657291602
linda@hubeijusheng.com CHINA 22968 58
Standardpharm Co. Ltd.
86-714-3992388
overseasales1@yongstandards.com United States 14336 58

サニルブジン  スペクトルデータ(IR1、MS)


3056-17-5(サニルブジン)キーワード:


  • 3056-17-5
  • STAVUDINE
  • 3'-deoxythymidin-2'-ene
  • 3'-DEOXY-2',3'-DIDEHYDROTHYMIDINE
  • ZERIT
  • STAVUDINE[2'',3''-DIDEHYDRO-3''-DEOXYTHYMIDINE]
  • NSC 163661
  • Stavir
  • Thymidine, 2'', 3''-didehydro-3''-deoxy-
  • 1-(5-(HYDROXYMETHYL)-2,5-DIHYDROFURAN-2-YL)-5-METHYLDIHYDROPYRIMIDINE-2,4(1H,3H)-DIONE
  • 1-(2,3-dideoxy-β-d-glycero-pent-2-enofuranosyl)thymine
  • STAVUDINE(PATENTEDNO-SUPPLY)
  • 2',3'-Didehydro-3'-deoxy-D-thymidine
  • 2'-Thymidinene, 3'-deoxy- (8CI)
  • D 4T (nucleoside)
  • sanilvudine
  • Thymidine, 2',3'-didehydro-3'-deoxy- (9CI)
  • Thymine, 1-(2,3-dideoxy-b-D-glycero-pent-2-enofuranosyl)- (7CI, 8CI)
  • Stavudine (250 mg)
  • Stauvidine Hydrochloride
  • 1-[(2R,3R,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,4-triazole-3-carboxamide and 1-[(2R,5S)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methyl-pyrimidine-2,4-dione
  • 1-(2,3-Dideoxy-β-D-glycero-2-pentenofuranosyl)thymine
  • 2',3'-Dideoxythymidiene
  • 2μ,3μ-Anhydrothymidine, d4T, Stavudine, 1-(2,3-Dideoxy-β-D-glycero-pent-2-enofuranosyl)thymine
  • Stavudine SysteM Suitability Mixture
  • 2'', 3''-DIDEHYDRO-3''-DEOXYTHMIDINE (D4T: STAVUDINE)
  • Stauvidine
  • 1-(2,3-Dideoxy-beta-D-glycero-2-pentenofuranosyl)thymine
  • 1-((2R,5S)-5-HYDROXYMETHYL-2,5-DIHYDRO-FURAN-2-YL)-5-METHYL-1H-PYRIMIDINE-2,4-DIONE
  • 1-[2,3-DIDEOXY-BETA-D-GLYCERO-PENT-2-ENOFURANOSYL]THYMINE
  • 2',3'-DIDEHYDRO-3'-DEOXYTHYMIDINE
  • 2',3'-ジデヒドロ-3'-デオキシチミジン
  • ゼリット
  • 1-(2,3-ジデオキシ-β-D-glycero-ペンタ-2-エノフラノシル)-5-メチルウラシル
  • 1-[5β-(ヒドロキシメチル)-2,5-ジヒドロフラン-2β-イル]チミン
  • 1-[2,5-ジヒドロ-5β-(ヒドロキシメチル)フラン-2β-イル]チミン
  • 3'-デオキシ-2',3'-ジデヒドロチミジン
  • 1-(2,3-ジデオキシ-β-D-glycero-2-ペンテノフラノシル)チミン
  • 1-[(2R,5S)-5-(ヒドロキシメチル)-2,5-ジヒドロフラン-2-イル]チミン
  • 1-[[(2R,5S)-2,5-ジヒドロ-5-(ヒドロキシメチル)フラン]-2-イル]チミン
  • サニルブジン
  • 1-[[2,5-ジヒドロ-5β-(ヒドロキシメチル)フラン]-2β-イル]-5-メチルピリミジン-2,4(1H,3H)-ジオン
  • スタブジン
  • D-4T【ヌクレオシド】
  • 2',3'-ジデヒドロ-2',3'-ジデオキシチミジン
  • 2',3'-ジデオキシチミジエン
  • 2',3'-アンヒドロチミジン
  • 2′,3′-ジデヒドロ-3′-デオキシチミジン
  • サニルブジン (JAN)
  • 3′-デオキシ-2′,3′-ジデヒドロチミジン
  • 2′,3′-ジデオキシチミジエン
  • 2′,3′-ジデヒドロ-2′,3′-ジデオキシチミジン
  • 1-[(2R,5S)-5-(ヒドロキシメチル)-2,5-ジヒドロフラン-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
  • ヌクレオシド,ヌクレオチド&関連試薬
  • ヌクレオシドと類似体
  • 生化学
  • 試験研究用抗ウィルス剤
  • 試験研究用抗菌剤
  • 薬理研究用試薬
  • 代謝拮抗物質
  • 酵素阻害剤
  • 抗エイズ薬
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