Tafamidis Meglumine

Tafamidis Meglumine Structure
CAS No.
951395-08-7
Chemical Name:
Tafamidis Meglumine
Synonyms
PF06291826;PF-06291826;cas 594839-88-0;afamidis Meglumine;Tafamidis Meglumine;Tafamidis-meglumine API;He prescribed metoclopramide;Tafamidis meglumine (Fx1006, PF06291826);tafamidis meglumine,Inhibitor,Tafamidis,inhibit;TAFAMIDIS;CAS 594839-88-0;PF-06291826;PF06291826
CBNumber:
CB53159986
Molecular Formula:
C21H24Cl2N2O8
Molecular Weight:
503.33
MOL File:
951395-08-7.mol
Modify Date:
2024/8/28 16:27:42

Tafamidis Meglumine Properties

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|

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 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.

Uses

Tafamidis Meglumine is used as a potential therapeutics for COVID-19 and related viral infections

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.

Tafamidis Meglumine Preparation Products And Raw materials

Raw materials

Preparation Products

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951395-08-7(Tafamidis Meglumine)Related Search:

Tafamidis Meglumine 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole meglumine cas 594839-88-0 PF06291826 PF-06291826 TAFAMIDIS;CAS 594839-88-0;PF-06291826;PF06291826 Tafamidis meglumine (Fx1006, PF06291826) tafamidis meglumine,Inhibitor,Tafamidis,inhibit Tafamidis-meglumine API afamidis Meglumine He prescribed metoclopramide (2R,3R,4R,5S)-6-(Methylamino)hexane-1,2,3,4,5-pentaol 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylate 951395-08-7 C21H24Cl2N2O8 C7H17NO5C14H7Cl2NO3 API