タファミジス
タファミジス 物理性質
- 沸点 :
- 486.7±40.0 °C(Predicted)
- 比重(密度) :
- 1.530
- 貯蔵温度 :
- -20°
- 溶解性:
- DMSO に可溶 (最大 20 mg/ml)。
- 酸解離定数(Pka):
- 3.49±0.30(Predicted)
- 外見 :
- 個体
- 色:
- オフホワイト
- 安定性：:
- -20°C の DMSO 溶液で最大 3 か月間保存できます。
- InChI:
- InChI=1S/C14H7Cl2NO3/c15-9-3-8(4-10(16)6-9)13-17-11-2-1-7(14(18)19)5-12(11)20-13/h1-6H,(H,18,19)
- InChIKey:
- TXEIIPDJKFWEEC-UHFFFAOYSA-N
- SMILES:
- O1C2=CC(C(O)=O)=CC=C2N=C1C1=CC(Cl)=CC(Cl)=C1
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)
タファミジス 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
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更新時間 |
購入 |
タファミジス 化学特性,用途語,生産方法
効能
アミロイド形成抑制薬
説明
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (K
d1 = 3 nM; K
d2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC
50s = 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions
in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits
ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.
使用
Tafamidis can be used as a benzoxole derivative that is a transthyretin (TTR) amyloid fibril inhibitors. It is a new drug candidate in the treatment of TTR amyloidosis (caused my misfolding of proteins).
定義
ChEBI: A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazole-6-carboxylic acid in which the hydrogen at position 2 is replaced by a 3,5-dichlorophenyl group. Used (as its meglumine salt) for the amelioration of transthyretin-related hereditary amyloid
sis.
合成
The synthesis of 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid is as follows:
methyl 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylate (17.9 mmol) was dissolved in a mixture of THF:MeOH:H2O (3:1:1, 50 mL) and treated with LiOH (71.6 mmol) at room temperature for 6h. The mixture was acidified to pH 2 with 1 N HCl and extracted with EA. The combined organic layers were dried over MgSO4, filtered and concentrated to give the product as a white solid 5.0 g, yield 91%.
タファミジス 上流と下流の製品情報
原材料
準備製品
タファミジス 生産企業
Global( 177)Suppliers
594839-88-0(タファミジス)キーワード:
- 594839-88-0
- Tafamidis (Fx1006A)
- Tafamidis free acid
- PF-06291826(Tafamidis)
- TafaMidis
- Fx 1006
- 6-Benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)-
- Tafamidis(Fx 1006)
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- Fx 1006A
- Fx1006A
- Fx-1006A
- FX-1006A;FX1006A;FX 1006A
- Tafamidis free acid, 2-(3,5-dichlorophenyl)-6-benzoxazole carboxylic acid
- 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid
- afamidis (Fx1006A)
- 2-(3,5-Dichlorophenyl)benzoxazole-6-carboxylic Acid
- Tafamidis API
- 2-(3,5-Dichlorophenyl)-1,3-Benzoxazole-6-carboxylic acid
- Chlorfenazolac
- Tafamidis, 10 mM in DMSO
- D3-Tafamidis
- タファミジス
- タファミディス
- ビンダケル
- 2-(3,5-ジクロロフェニル)ベンゾオキサゾール-6-カルボン酸
- 2-(3,5-ジクロロフェニル)-1,3-ベンゾオキサゾール-6-カルボン酸