ChemicalBook > CAS DataBase List > Tafamidis Meglumine

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
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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|
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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..…

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N-Bromosuccinimide Price

Biorbyt Ltd
Product number
orb573018
Product name
Tafamidis meglumine
Purity
>98%
Packaging
100mg
Price
$615.4
Updated
2021/12/16
Biorbyt Ltd
Product number
orb573018
Product name
Tafamidis meglumine
Purity
>98%
Packaging
250mg
Price
$1060.8
Updated
2021/12/16
Biorbyt Ltd
Product number
orb573018
Product name
Tafamidis meglumine
Purity
>98%
Packaging
1g
Price
$2097.8
Updated
2021/12/16
DC Chemicals
Product number
DC12377
Product name
Tafamidismeglumine
Purity
>98%
Packaging
100mg
Price
$400
Updated
2021/12/16
DC Chemicals
Product number
DC12377
Product name
Tafamidismeglumine
Purity
>98%
Packaging
1g
Price
$1400
Updated
2021/12/16
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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

Hebei Weibang Biotechnology Co., Ltd
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
Hebei Mojin Biotechnology Co., Ltd
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

951395-08-7, Tafamidis MeglumineRelated Search:


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