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[CAS NO. 951395-08-7] Tafamidismeglumine
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14852A |
| Brand: | MCE |
| CAS: | 951395-08-7 |
Overview
| MDL | MFCD28502032 |
|---|---|
| Molecular Weight | 503.33 |
| Molecular Formula | C21H24Cl2N2O8 |
| SMILES | O=C(C1=CC=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1)O.O[C@@H]([C@@H]([C@@H](CO)O)O)[C@@H](O)CNC |
1 Publications Citing Use of MCE
Summary
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC 50 s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis [1] .
IC50 & Target
EC50: 2.7-3.2 μM (TTR) [1]
In Vitro
Tafamidis binds selectively and with negative cooperativity (K
d
s ∼2 nM and ∼200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR
[1]
.
Tafamidis (0-7.2 μM) dose-dependently inhibits WT-TTR amyloidogenesis after treatment for 72 hours at a pH of 4.4-4.5
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00935012 | Pfizer |
ATTR-CM|TTR-CM
|
September 30, 2009 | Phase 3 |
| NCT03266705 | Pfizer |
Healthy
|
September 20, 2017 | Phase 1 |
| NCT05560555 | Pfizer |
Hereditary Transthyretin Amyloidosis (ATTRv)|Polyneuropathy
|
September 30, 2022 | |
| NCT02406560 | Pfizer |
Healthy Volunteers
|
April 2015 | Phase 1 |
| NCT01435655 | Pfizer |
Transthyretin Familial Amyloid Polyneuropathy
|
November 2011 | Phase 3 |
| NCT02189330 | Pfizer |
Healthy Volunteers
|
May 2014 | Phase 1 |
| NCT00630864 | Pfizer |
Transthyretin-associated Amyloidosis With Polyneuropathy
|
June 2008 | Phase 2 |
| NCT02746926 | Pfizer |
Healthy
|
April 29, 2016 | Phase 1 |
| NCT01655511 | Pfizer |
TTR Cardiomyopathy
|
July 2012 | Phase 1 |
| NCT04828993 | Pfizer |
Transthyretin Amyloid Polyneuropathy (ATTR-PN)
|
April 28, 2021 | Phase 4 |
| NCT02217813 | Pfizer |
Healthy Volunteers
|
October 2014 | Phase 1 |
| NCT05482308 | Pfizer |
Healthy
|
August 29, 2022 | Phase 1 |
| NCT04253353 | Pfizer |
Healthy Volunteers
|
February 6, 2020 | Phase 1 |
| NCT04814186 | Pfizer |
Transthyretin Amyloid Cardiomyopathy
|
July 22, 2021 | Phase 4 |
| NCT02697864 | Pfizer |
Healthy
|
April 2016 | Phase 1 |
| NCT05139680 | Pfizer |
Hereditary Transthyretin Amyloidosis (ATTRv) Cardiomyopathy (CM), Mixed Phenotype
|
December 1, 2022 | |
| NCT00791492 | Pfizer |
Familial Amyloid Polyneuropathy|ATTR-PN
|
July 2008 | Phase 2|Phase 3 |
| NCT02534740 | Pfizer |
Healthy
|
September 2015 | Phase 1 |
| NCT05498701 | Pfizer |
Healthy
|
September 29, 2022 | Phase 1 |
| NCT00409175 | Pfizer |
Familial Amyloid Polyneuropathy
|
January 2007 | Phase 2|Phase 3 |
| NCT04963985 | Peking University Third Hospital |
Transthyretin Amyloidosis
|
June 1, 2021 | Phase 4 |
| NCT01994889 | Pfizer |
Transthyretin (TTR) Amyloid Cardiomyopathy
|
December 9, 2013 | Phase 3 |
| NCT01369836 | Pfizer |
Healthy
|
July 2011 | Phase 1 |
| NCT00925002 | Pfizer |
ATTR-PN
|
August 5, 2009 | Phase 3 |
| NCT05489523 | University of Texas Southwestern Medical Center |
Transthyretin Cardiac Amyloidosis
|
December 15, 2022 | Phase 4 |
| NCT04575116 | Pfizer |
Healthy
|
September 17, 2020 | Phase 1 |
| NCT03280173 | Pfizer |
Healthy
|
September 29, 2017 | Phase 1 |
| NCT01358565 | Pfizer |
Mild Hepatic Dysfunction|Moderate Hepatic Dysfunction
|
November 2010 | Phase 1 |
| NCT03662191 | Pfizer |
Healthy Volunteers
|
September 28, 2018 | Phase 1 |
| NCT00694161 | Pfizer |
Cardiomyopathy
|
August 2008 | Phase 2 |
| NCT02791230 | Pfizer |
Transthyretin (TTR) Amyloid Cardiomyopathy
|
June 13, 2016 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 12.5 mg/mL ( 24.83 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9868 mL | 9.9338 mL | 19.8677 mL |
| 5 mM | 0.3974 mL | 1.9868 mL | 3.9735 mL |
| 10 mM | 0.1987 mL | 0.9934 mL | 1.9868 mL |
Synonyms
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