アバナフィル
アバナフィル 物理性質
- 融点 :
- 150-152°C
- 比重(密度) :
- 1.372
- 貯蔵温度 :
- Sealed in dry,Store in freezer, under -20°C
- 溶解性:
- DMSO（微量）、メタノール（微量、加温）
- 外見 :
- 個体
- 酸解離定数(Pka):
- 11.84±0.46(Predicted)
- 色:
- ホワイトからオフホワイト
- InChIKey:
- WEAJZXNPAWBCOA-INIZCTEOSA-N
- SMILES:
- C1(N2CCC[C@H]2CO)=NC=C(C(NCC2=NC=CC=N2)=O)C(NCC2=CC=C(OC)C(Cl)=C2)=N1
- CAS データベース:
- 330784-47-9(CAS DataBase Reference)
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)
| 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 |
|
| 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。 |
|
| 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)
|
W01MAS118219 |
(S)-4-((3-Chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide |
330784-47-9 |
1g |
￥362900 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
SML2799 |
≥98% (HPLC)
Avanafil ≥98% (HPLC) |
330784-47-9 |
100MG |
￥5310 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
SML2799 |
≥98% (HPLC)
Avanafil ≥98% (HPLC) |
330784-47-9 |
500MG |
￥15900 |
2024-03-01 |
購入 |
アバナフィル 化学特性,用途語,生産方法
効能
勃起不全治療薬, ホスホジエステラーゼV阻害薬
説明
Avanafil (Zepeed) was approved by the Korean Health Ministry for the
treatment of erectile dysfunction (ED) in August 2011. Avanafil is a
highly selective type 5 phosphodiesterase (PDE5) inhibitor.
Avanafil is reported to be the most selective PDE5
inhibitor on the market. The onset of Tmax and half-life also varies among
the marketed PDE5 inhibitors. Sildenafil has a T
max at 1 h and a half-life of
3–5 h. Vardenafil is somewhat similar with a T
max of 0.6 h and a half-life of
4–6 h. Tadalafil has the longest half-life among the marketed drugs with a
half-life of 17 h. Avanafil has a fast onset of action reaching T
max in 0.6 h
with a half-life of 1.2 h. A synthesis of avanafil (TA-1790) is described
in the patent literature. The main elimination route of avanafil
is through the bile and feces. Avanafil was also found to be reabsorbed
through enterohepatic recirculation.
化学的特性
White Solid
使用
Avanafil is a highly selective PDE5 inhibitor with IC50 of 1 nM.
定義
ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-[(3-chloro-4-methoxybenzyl)amino]-2-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]pyrimidine-5-carboxylic acid with the amino group of pyrimidin-2-ylmethylamine
Used for treatment of erectile dysfunction.
臨床応用
Avanafil was originally discovered at Tanabe Seiyaku (now
Mitsubishi Tanabe). JW Pharmaceutical (previously Choongwae Pharma) and VIVUS have since developed and launched avanafil,
which is an oral PDE5 inhibitor for the treatment of erectile dysfunction
(ED). Although many marketed PDE5 inhibitors (e.g. sildenafil,
vardenafil and tadalafil) are available for the treatment of ED,
many patients are still unable to achieve the desired results and
experience undesired side-effects with these existing medications.
As such, second-generation PDE5 inhibitors with enhanced PDE5
selectivity, shorter systemic half-lives, and improved tolerability
are desired. Developed to meet these criteria, Avanafil exhibited
good oral bioavailability and PDE5 selectivity in both preclinical
studies and clinical trials. Avanafil had a short onset of action
(35 min) and short half-life (1.5 h).
アバナフィル 上流と下流の製品情報
原材料
準備製品
アバナフィル 生産企業
Global( 452)Suppliers
330784-47-9(アバナフィル)キーワード:
- 330784-47-9
- 4-[[(3-Chloro-4-Methoxyphenyl)Methyl]
aMino]-2-[(2S)-2-(hydroxyMethyl)-1-pyrrolidinyl]-N-(2-pyriMidinylMethyl)-5-pyriMidinecarboxaMide
- Avanafil 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide
- avanfil
- (S)-4-((3-Chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-yl
- avanafil:4-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)-1-pyrrolidinyl)-n-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide: (s)-2-(2-hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylami
- (S)-4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2pyrimidinylmethyl)-5-pyrimidinecarboxamide
- (S)-2-(2-Hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5-[(2-pyrimidinylmethyl)carbamoyl]pyrimidine
- 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide
- Avanafil
- Avanafil (usan/inn)
- D03217
- Avanafil PDE5 inhibitor
- pharmaceutical raw material suppliers Avanafil 330784-47-9 high quality lower Prices
- Natural Sex Steroid Hormones Avanafil Hormone Powder C23H26ClN7O3 CAS 330784-47-9
- Avanafil-d3
- 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide
- Avanafil(TA-1790)
- 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide
- [13C5, 15N]-Avanafil
- 4-[(3-Chloro-4-methoxybenzyl)amino]
- O cut the non
- AVANAFE
- Avanafil white powder
- Avanafil USP/EP/BP
- Avanafil , Stendra
- Avanafil, Standa
- (S)-4-chloro-6-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide
- 4-[(3-Chloro-4-methoxybenzyl)amino] Avanafil
- Avanafil-d4
- (S)-4-chloro-6-((3-chloro-4-methoxybenzyl)amino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl)pyrimidine-6-carboxamide
- アバナフィル
- 4-[(3-クロロ-4-メトキシベンジル)アミノ]-2-[(2S)-2-(ヒドロキシメチル)ピロリジン-1-イル]-N-(ピリミジン-2-イルメチル)ピリミジン-5-カルボキサミド
- 4-{[(3-クロロ-4-メトキシフェニル)メチル]アミノ}-2-[(2S)-2-(ヒドロキシメチル)ピロリジン-1-イル]-N-[(ピリミジン-2-イル)メチル]ピリミジン-5-カルボキサミド
- N-(ピリミジン-2-イルメチル)-2-[(2S)-2-(ヒドロキシメチル)ピロリジノ]-4-(3-クロロ-4-メトキシベンジルアミノ)ピリミジン-5-カルボアミド
- 4-[(3-クロロ-4-メトキシベンジル)アミノ]-2-[(2S)-2-(ヒドロキシメチル)ピロリジノ]-N-(2-ピリミジニルメチル)ピリミジン-5-カルボアミド