[CAS NO. 951395-08-7] Tafamidismeglumine

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [951395-08-7]

Catalog

HY-14852A

Brand

MCE

CAS

951395-08-7

DESCRIPTION [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

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]J Med Chem. 2021 Sep 21.

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

In Vitro:

DMSO : 12.5 mg/mL ( 24.83 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (insoluble)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.25 mg/mL (2.48 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (2.48 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.25 mg/mL (2.48 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Bulawa CE, et al. Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9629-34.

Synonyms

D-Glucitol, 1-deoxy-1-(methylamino)-, 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate (1:1)

Fx 1006A

Tafamidis meglumine

Vyndaqel