2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
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2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid 속성
- 끓는 점
- 486.7±40.0 °C(Predicted)
- 밀도
- 1.530
- 저장 조건
- -20°
- 용해도
- DMSO에 용해됩니다(최대 20mg/ml).
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- 3.49±0.30(Predicted)
- 색상
- 회백색
- 안정성
- 최대 3개월 동안 -20°의 DMSO에 보관
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid C화학적 특성, 용도, 생산
개요
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (Kd1 = 3 nM; Kd2 = 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 (EC50s = 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.용도
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).정의
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.Synthesis
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%.
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid 준비 용품 및 원자재
원자재
준비 용품
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid 공급 업체
글로벌( 139)공급 업체
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| Changzhou Guiding Bio-Tech. Co.,Ltd. | +86-519-519-86686860 +8618795626222 |
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| Hebei Mojin Biotechnology Co., Ltd | +8613288715578 |
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| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
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| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
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| CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
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| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 |
info@chemia-pharm.com | CHINA | 311 | 58 |
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| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 |
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