リファペンチン

リファペンチン 化学構造式
61379-65-5
CAS番号.
61379-65-5
化学名:
リファペンチン
别名:
3-[[(4-シクロペンチル-1-ピペラジニル)イミノ]メチル]リファマイシン;リファペンチン;3-[(4-シクロペンチルピペラジノ)イミノメチル]リファマイシン;(7S,11S,12R,13S,14R,15R,16R,17S,18S,19Z,21Z)-26-{[(4-シクロペンチルピペラジン-1-イル)イミノ]メチル}-2,15,17,27,29-ペンタヒドロキシ-11-メトキシ-3,7,12,14,16,18,22-ヘプタメチル-6,23-ジオキソ-8,30-ジオキサ-24-アザテトラシクロ[23.3.1.14,7.05,28]トリアコンタ-1,3,5(28),9,19,21,25(29),26-オクタエン-13-イル アセタート
英語名:
Rifapentine
英語别名:
ktc1;dl473;r-773;mdl473;Priftin;Prifitin;Rifapenti;Rifapentin;PIFAPENTINE;RIFAPENTINE
CBNumber:
CB6381080
化学式:
C47H64N4O12
分子量:
877.03
MOL File:
61379-65-5.mol
MSDS File:
SDS

リファペンチン 物理性質

融点 :
179-1800C
沸点 :
969.3±65.0 °C(Predicted)
比重(密度) :
1.35±0.1 g/cm3(Predicted)
貯蔵温度 :
Sealed in dry,Store in freezer, under -20°C
溶解性:
メタノール: 可溶2mg/mL、透明、赤~赤褐色
外見 :
酸解離定数(Pka):
4.81±0.70(Predicted)
色:
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
WGK Germany  3
RTECS 番号 JQ0902000
HSコード  2941.90.3000
毒性 LD50 in mice (mg/kg): >2000 orally; 750 i.p. (Cricchio); LD50 in mice (mg/kg): 3300 orally; 710 i.p. (Aroli)
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
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms 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 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
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 GHS hazard pictograms
注意書き
P261 粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける 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。

リファペンチン 価格 もっと(11)

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) W01TRCR508500 リファペンチン
Rifapentine
61379-65-5 10mg ¥28200 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TRCR508500 リファペンチン
Rifapentine
61379-65-5 25mg ¥35400 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TRCR508500 リファペンチン
Rifapentine
61379-65-5 5mg ¥20600 2023-06-01 購入
東京化成工業 R0198 リファペンチン >98.0%(HPLC)
Rifapentine >98.0%(HPLC)
61379-65-5 100mg ¥18500 2024-03-01 購入
東京化成工業 R0198 >98.0%(HPLC)
Rifapentine >98.0%(HPLC)
61379-65-5 500MG ¥64800 2024-03-01 購入

リファペンチン 化学特性,用途語,生産方法

外観

うすい黄色~褐色粉末~結晶

効能

抗生物質, RNAポリメラーゼ阻害薬

説明

Rifapentine is a broad spectrum antibiotic highly active against Gram-positive bacteria and Neisseria gonorrhoea. It is reported to be 10 times more active than the structurally related rifampicin against Mycobacrerim fuberculosis. Unlike rifampicin the bioavailability of rifapentine is significantly increased when administered after a meal.

化学的特性

Crystalline Solid

使用

Semi-synthetic rifamycin. Antibacterial (tuberculostatic)

適応症

Rifapentine is an analogue of rifampin that is active against M. tuberculosis and M. avium. Rifapentine’s mechanism of action, cross-resistance, hepatic induction of P450 enzymes, drug interactions, and toxic profile are similar to those of rifampin. It has been used in the treatment of tuberculosis caused by rifampinsusceptible strains.

抗菌性

Activity is similar to that of rifampicin, but it is more active against atypical mycobacteria, especially the M. avium complex (MIC <0.06–0.5 mg/L). It has good activity on staphylococci and streptococci (MIC 0.01–0.5 mg/L), L. monocytogenes and Brucella spp.; less against Enterococcus faecalis (MIC 1–4 mg/L). Bacteroides spp. are inhibited by 0.5–2 mg/L. Gram-negative cocci are susceptible and, although some Gram-negative bacilli are inhibited by 4–32 mg/L, most are resistant.

危険性

Moderately toxic by ingestion.

応用例(製薬)

An analog of rifampicin in which a cyclopentyl group is substituted for a methyl group on the piperazine ring. It is available for oral administration.

作用機序

Because relapse and the emergence of resistant strains of bacteria are associated with poor patient compliance, reduced dosing is expected to increase compliance. Initial clinical studies actually showed that the relapse rates in patients treated with rifapentine (10%) were higher than those in the patients treated with RIF (5%). It was found that poor compliance with the nonrifamycin antituberculin agents was responsible for the increased relapse.

薬物動態学

Oral absorption:c. 70%
Cmax600 mg oral :12 mg/L after 5 h
Plasma half-life:13 h
Volume of distribution:1.5 L/kg
Plasma protein binding:97%
absorption
The absolute oral bioavailability of rifapentine has not been determined. The relative bioavailability of capsules (with an oral solution as reference) is 70%. Food increases absorption: a 600 mg dose taken after a meal gives Cmax and AUC values 44% higher than under fasting conditions. The extended halflife provides therapeutic concentrations for at least 72 h after administration, allowing less frequent dosing.
Distribution
Animal data suggest that it is well distributed in the body, with tissue concentrations exceeding the plasma concentration, except in bone, testes and brain. The ratio of intracellular:extracellular concentration in macrophages was estimated as 24:1.
Metabolism
The main metabolite is an antimicrobially active 25-desacetyl derivative. Although it induces liver cytochromes it is not an inducer of its own metabolism, which is mediated by an esterase. The peak concentration of 25-desacetyl rifapentine is about one-third of that of the unchanged drug, and is attained after about 11 h.
excretion
The main route of elimination is through the bile. In healthy volunteers about 70% of a 600 mg dose of 14C rifapentine was recovered in the feces, and less than 17% in the urine. There is evidence of enterohepatic recycling in humans.

臨床応用

Tuberculosis (in combination with other antituberculosis drugs)

副作用

Signs of teratogenic effects and fetal toxicity have been observed when administered during pregnancy to rats and rabbits. Rifapentine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
The most common adverse effect observed in combinations with other antimycobacterial agents was hyperuricemia, most probably due to pyrazinamide. Effects likely to be due to rifapentine were neutropenia (3.7% of patients) and hepatitis (increased transaminases in 1.6% of patients).

リファペンチン 上流と下流の製品情報

原材料

準備製品


リファペンチン 生産企業

Global( 281)Suppliers
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career henan chemical co
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factory@coreychem.com China 29826 58

リファペンチン  スペクトルデータ(1HNMR、MS)


61379-65-5(リファペンチン)キーワード:


  • 61379-65-5
  • rifamycinaf/acpp
  • 3{[(4-cyclopentyl-1-piperazinyl)imino]methyl}rifamycin
  • Rifapentine(Priftin)
  • PIFAPENTINE
  • antibioticdl473it
  • dl473
  • ktc1
  • mdl473
  • r-773
  • 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)-rifamyci
  • 3-(4-cyclopentyl-1-piperazinyl)iminomethylrifamycinsv
  • RIFAPENTINE
  • Rifapention
  • 3 & 4-NONENES & 4-NONANOL
  • Cyclopentylrifampicin
  • Prifitin
  • Priftin
  • Rifapenti
  • 3-[[(4-Cy-dopentyl-1piperazinyl)imino]methyl]rifamycin
  • Rifapentin
  • Rifamycin, 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)
  • 3-[(4-Cyclopentylpiperazino)iminomethyl]rifamycin
  • Rifapentinum
  • Rifapentina
  • (2S,12Z,14E,16S,17S,18R,19R,20R,21S,22R,23S,24E)-3-(((4-Cyclopentyl-1-piperazinyl)imino)methyl)-21-(Acetyloxy)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)naphtho[2,1-b]furan-1,11(2H)-dione
  • Rifapentine USP/EP/BP
  • Rifapentine (DL 473)
  • Rifapentine, ≥98% (HPLC)
  • 3-[[(4-シクロペンチル-1-ピペラジニル)イミノ]メチル]リファマイシン
  • リファペンチン
  • 3-[(4-シクロペンチルピペラジノ)イミノメチル]リファマイシン
  • (7S,11S,12R,13S,14R,15R,16R,17S,18S,19Z,21Z)-26-{[(4-シクロペンチルピペラジン-1-イル)イミノ]メチル}-2,15,17,27,29-ペンタヒドロキシ-11-メトキシ-3,7,12,14,16,18,22-ヘプタメチル-6,23-ジオキソ-8,30-ジオキサ-24-アザテトラシクロ[23.3.1.14,7.05,28]トリアコンタ-1,3,5(28),9,19,21,25(29),26-オクタエン-13-イル アセタート
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