Tafamidis Meglumine
- Product Name
- Tafamidis Meglumine
- CAS No.
- 951395-08-7
- Chemical Name
- Tafamidis Meglumine
- Synonyms
- PF06291826;PF-06291826;cas 594839-88-0;afamidis Meglumine;Tafamidis Meglumine;Meglumine clobenzolate;Tafamidis-meglumine API;He prescribed metoclopramide;Tafamidis meglumine (Fx1006, PF06291826);tafamidis meglumine,Inhibitor,Tafamidis,inhibit
- CBNumber
- CB53159986
- Molecular Formula
- C21H24Cl2N2O8
- Formula Weight
- 503.33
- MOL File
- 951395-08-7.mol
Tafamidis Meglumine Property
- 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
- InChIKey
- DQJDBUPLRMRBAB-KUAVVOKVNA-N
- SMILES
- [C@@H](O)([C@@H](O)CNC)[C@H](O)[C@H](O)CO.ClC1=CC(Cl)=CC(C2=NC3=CC=C(C(=O)O)C=C3O2)=C1 |&1:0,2,7,9,r|
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H360May damage fertility or the unborn child
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P281Use personal protective equipment as required.
P308+P313IF exposed or concerned: Get medical advice/attention.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- orb573018
- Product name
- Tafamidis meglumine
- Purity
- >98%
- Packaging
- 100mg
- Price
- $615.4
- Updated
- 2021/12/16
- Product number
- orb573018
- Product name
- Tafamidis meglumine
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1060.8
- Updated
- 2021/12/16
- Product number
- orb573018
- Product name
- Tafamidis meglumine
- Purity
- >98%
- Packaging
- 1g
- Price
- $2097.8
- Updated
- 2021/12/16
- Product number
- DC12377
- Product name
- Tafamidismeglumine
- Purity
- >98%
- Packaging
- 100mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- DC12377
- Product name
- Tafamidismeglumine
- Purity
- >98%
- Packaging
- 1g
- Price
- $1400
- Updated
- 2021/12/16
Tafamidis Meglumine Chemical Properties,Usage,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
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View Lastest Price from Tafamidis Meglumine manufacturers
- Product
- Tafamidis Meglumine 951395-08-7
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 500000kg
- Release date
- 2024-11-04
- Product
- Tafamidis Meglumine 951395-08-7
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 50000KG/month
- Release date
- 2023-10-12