Tafamidis Meglumine
- CAS No.
- 951395-08-7
- Chemical Name:
- Tafamidis Meglumine
- Synonyms
- PF06291826;PF-06291826;cas 594839-88-0;afamidis Meglumine;Tafamidis Meglumine;Tafamidis-meglumine API;Tafamidis meglumine (Fx1006, PF06291826);tafamidis meglumine,Inhibitor,Tafamidis,inhibit;TAFAMIDIS;CAS 594839-88-0;PF-06291826;PF06291826;6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole meglumine
- CBNumber:
- CB53159986
- Molecular Formula:
- C21H24Cl2N2O8
- Molecular Weight:
- 503.33
- MDL Number:
- MFCD28502032
- MOL File:
- 951395-08-7.mol
| Melting point | 195 - 198°C |
|---|---|
| storage temp. | -20°C Freezer, Under inert atmosphere |
| solubility | DMSO (Sparingly, Heated, Sonicated) |
| form | Solid |
| color | White to Off-White |
| FDA UNII | ZU7CF08A1A |
| NCI Drug Dictionary | tafamidis meglumine |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H360 |
| Precautionary statements | P201-P202-P281-P308+P313-P405-P501 |
Tafamidis Meglumine price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biorbyt Ltd | orb573018 | Tafamidis meglumine >98% | 951395-08-7 | 100mg | $615.4 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb573018 | Tafamidis meglumine >98% | 951395-08-7 | 250mg | $1060.8 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb573018 | Tafamidis meglumine >98% | 951395-08-7 | 1g | $2097.8 | 2021-12-16 | Buy |
| DC Chemicals | DC12377 | Tafamidismeglumine >98% | 951395-08-7 | 100mg | $400 | 2021-12-16 | Buy |
| DC Chemicals | DC12377 | Tafamidismeglumine >98% | 951395-08-7 | 1g | $1400 | 2021-12-16 | Buy |
Tafamidis Meglumine Chemical Properties,Uses,Production
Description
In November 2011, the European Commission approved tafamidis meglumine (Fx-1006A, PF-06291826) for the treatment of transthyretin familial amyloid polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy. Tafamidis stabilizes both the wild type and mutant forms of TTR tetramer and prevents tetramer dissociation by noncooperatively binding to the two thyroxine binding sites. Tafamidis is the first approved medicine for TTR-FAP. The Kd values for tafamidis for the two thyroxine binding sites on TTR, as determined by isothermal titration calorimetry, were 3 nM and 278 nM, respectively. In another in vitro study using wild type TTR, V30M mutant TTR, and V122I mutant TTR, it was shown that tafamidis inhibited fibril formation in a concentration-dependent manner reaching EC50 at a tafamidis:TTR stoichiometry of <1 (EC50 was in the range of 2.7–3.2 μM, corresponding to a tafamidis:TTR stoichiometry range of 0.75–0.9). Tafamidis has been synthesized by coupling 4-amino-3- hydroxybenzoic acid with 3,5-dichlorobenzoyl chloride followed by dehydration using p-toluenesulfonic acid.
Originator
Scripps Research Institute (United States)
Uses
Tafamidis Meglumine is used as a potential therapeutics for COVID-19 and related viral infections
Definition
ChEBI: Tafamidis meglumine is an organoammonium salt obtained by combining tafamidis with one molar equivalent of 1-deoxy-1-(methylamino)-D-glucitol. Used for the amelioration of transthyretin-related hereditary amyloidosis. It has a role as a central nervous system drug. It contains a tafamidis(1-).
brand name
Vyndaqel
Clinical Use
Tafamidis meglumine is a transthyretin amyloid inhibitor that was approved for the treatment of transthyretin amyloid polyneuropathy (ATTR-PN) and transthyretin familial amyloid polyneropathy (TTR-FAP). These diseases represent a rare autosomal neurodegenerative disorder characterized by autonomic, sensory and motor impairment which are typically fatal. Tafamidis was discovered at The Scripps Research Institute and developed by Pfizer.
Synthesis
Numerous synthetic routes have been reported including the use of direct CH activation to form the key biaryl bond. Although only reported on small scale, the most likely production route is detailed in the scheme.
Condensation of methyl 4-amino-3-hydroxybenzoic acid (154) with 3,5-dichlorobenzoyl chloride (155) in refluxing pyridine gave intermediate amide 156 which underwent cycylization upon treatment with p-TsOH in refluxing toluene producing benzoxazole 157. Saponification of the methyl ester with LiOH (aq.) afforded tafamidis. The free acid was treated with N-methyl-D-glutamine to provide tafamidis meglumine (XXIV) in 82% yield.
Tafamidis Meglumine Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hebei Mojin Biotechnology Co., Ltd | +8613288715578 | sales@hbmojin.com | China | 12469 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Guangzhou TongYi biochemistry technology Co.,LTD | +8613073028829 | mack@tongyon.com | China | 2996 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Hefei TNJ Chemical Industry Co.,Ltd. | 0551-65418684 +8618949823763 | sales@tnjchem.com | China | 25363 | 58 |
| Jiangxi Huihe Chemical Co., Ltd. | +86-19189228086 +8618858568638 | wuzhouding@huihecrop.com | China | 886 | 58 |
| Nanjing Doge Biomedical Technology Co., Ltd | +86-25-58227606 +86-15305155328 | sales@dogechemical.com | China | 4128 | 58 |
| Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503259 +86-19930503259 | cherry@crovellbio.com | China | 18449 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
View Lastest Price from Tafamidis Meglumine manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2023-10-12 | Tafamidis Meglumine
951395-08-7
|
US $0.00 / KG | 1KG | 99% | 50000KG/month | Hebei Mojin Biotechnology Co., Ltd | |
 |
2023-09-06 | Tafamidis Meglumine
951395-08-7
|
US $0.00-0.00 / KG | 1KG | 99% | 500000kg | Hebei Guanlang Biotechnology Co., Ltd. |
-
- Tafamidis Meglumine
951395-08-7
- US $0.00 / KG
- 99%
- Hebei Mojin Biotechnology Co., Ltd
-
- Tafamidis Meglumine
951395-08-7
- US $0.00-0.00 / KG
- 99%
- Hebei Guanlang Biotechnology Co., Ltd.