2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- CAS No.
- 594839-88-0
- Chemical Name:
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
- Synonyms
- TafaMidis;Fx-1006A;Fx 1006;Fx1006A;Fx 1006A;Tafamidis API;Tafamidis(Fx 1006);afamidis (Fx1006A);Tafamidis free acid;Tafamidis (Fx1006A)
- CBNumber:
- CB52484674
- Molecular Formula:
- C14H7Cl2NO3
- Molecular Weight:
- 308.12
- MDL Number:
- MFCD16621109
- MOL File:
- 594839-88-0.mol
- MSDS File:
- SDS
| Boiling point | 486.7±40.0 °C(Predicted) |
|---|---|
| Density | 1.530 |
| storage temp. | -20° |
| solubility | Soluble in DMSO (up to 20 mg/ml). |
| form | solid |
| pka | 3.49±0.30(Predicted) |
| color | Off-white |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| FDA UNII | 8FG9H9D31J |
| ATC code | N07XX08 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H335-H319-H315 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P | |||||||||
| NFPA 704 |
|
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid price More Price(15)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 13694 | Tafamidis ≥98% | 594839-88-0 | 5mg | $67 | 2024-03-01 | Buy |
| Cayman Chemical | 13694 | Tafamidis ≥98% | 594839-88-0 | 10 mg | $107 | 2024-03-01 | Buy |
| Cayman Chemical | 13694 | Tafamidis ≥98% | 594839-88-0 | 25 mg | $217 | 2024-03-01 | Buy |
| Cayman Chemical | 13694 | Tafamidis ≥98% | 594839-88-0 | 50 mg | $398 | 2024-03-01 | Buy |
| Biosynth Carbosynth | FD27988 | 2-(3,5-Dichlorophenyl)-6-benzoxazolecarboxylic acid | 594839-88-0 | 10mg | $540 | 2021-12-16 | Buy |
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Chemical Properties,Uses,Production
Description
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.
Uses
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).
Definition
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%.
References
1) Bulawa?et al.?(2012),?Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits amyloid cascade; Proc. Natl. Acad. Sci. USA,?109?9629 2) Scott (2014),?Tafamidis: a review of its use in familial amyloid polyneuropathy; Drugs,?74?1371 3) Zhao?et al.?(2019),?Tafamidis, a Noninvasive Therapy for Delaying Transthyretin Familial Amyloid Polyneuropathy: Systemic Review and Meta-analysis; J. Clin. Neurol.,?15?108 4) Lorenzini and Elliott (2019),?Tafamidis for the treatment of transthyretin amyloidosis; Future Cardiol.,?15?53
2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Changzhou Guiding Bio-Tech. Co.,Ltd. | +86-519-519-86686860 +8618795626222 | ning@guiding-bio.com | China | 299 | 58 |
| Hebei Mojin Biotechnology Co., Ltd | +8613288715578 | sales@hbmojin.com | China | 12456 | 58 |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 7845 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9702 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
View Lastest Price from 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-03-23 | 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
|
US $32.00-1.50 / kg | 1kg | 99% | g-kg-tons, free sample is available | Henan Fengda Chemical Co., Ltd | |
 |
2023-10-14 | 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
|
US $0.00 / KG | 1KG | 99% | 50000KG/month | Hebei Mojin Biotechnology Co., Ltd | |
 |
2023-09-06 | 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
|
US $0.00-0.00 / KG | 1KG | 99% | 500000kg | Hebei Guanlang Biotechnology Co., Ltd. |
-
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
- US $32.00-1.50 / kg
- 99%
- Henan Fengda Chemical Co., Ltd
-
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
- US $0.00 / KG
- 99%
- Hebei Mojin Biotechnology Co., Ltd
-
- 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid
594839-88-0
- US $0.00-0.00 / KG
- 99%
- Hebei Guanlang Biotechnology Co., Ltd.