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[CAS NO. 594839-88-0] Tafamidis

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Catalog:	HY-14852
Brand:	MCE
CAS:	594839-88-0

Overview

MDL	-
Molecular Weight	308.12
Molecular Formula	C14H7Cl2NO3
SMILES	O=C(C1=CC=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1)O

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 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 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
NCT02217813	Pfizer	Healthy Volunteers	October 2014	Phase 1
NCT03662191	Pfizer	Healthy Volunteers	September 28, 2018	Phase 1
NCT05560555	Pfizer	Hereditary Transthyretin Amyloidosis (ATTRv)\|Polyneuropathy	September 30, 2022
NCT00925002	Pfizer	ATTR-PN	August 5, 2009	Phase 3
NCT05139680	Pfizer	Hereditary Transthyretin Amyloidosis (ATTRv) Cardiomyopathy (CM), Mixed Phenotype	December 1, 2022
NCT01994889	Pfizer	Transthyretin (TTR) Amyloid Cardiomyopathy	December 9, 2013	Phase 3
NCT00630864	Pfizer	Transthyretin-associated Amyloidosis With Polyneuropathy	June 2008	Phase 2
NCT01369836	Pfizer	Healthy	July 2011	Phase 1
NCT02534740	Pfizer	Healthy	September 2015	Phase 1
NCT01435655	Pfizer	Transthyretin Familial Amyloid Polyneuropathy	November 2011	Phase 3
NCT02406560	Pfizer	Healthy Volunteers	April 2015	Phase 1
NCT00935012	Pfizer	ATTR-CM\|TTR-CM	September 30, 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
NCT05498701	Pfizer	Healthy	September 29, 2022	Phase 1
NCT01655511	Pfizer	TTR Cardiomyopathy	July 2012	Phase 1
NCT01358565	Pfizer	Mild Hepatic Dysfunction\|Moderate Hepatic Dysfunction	November 2010	Phase 1
NCT00791492	Pfizer	Familial Amyloid Polyneuropathy\|ATTR-PN	July 2008	Phase 2\|Phase 3
NCT05482308	Pfizer	Healthy	August 29, 2022	Phase 1
NCT00409175	Pfizer	Familial Amyloid Polyneuropathy	January 2007	Phase 2\|Phase 3
NCT02791230	Pfizer	Transthyretin (TTR) Amyloid Cardiomyopathy	June 13, 2016	Phase 3
NCT03266705	Pfizer	Healthy	September 20, 2017	Phase 1
NCT04253353	Pfizer	Healthy Volunteers	February 6, 2020	Phase 1
NCT02189330	Pfizer	Healthy Volunteers	May 2014	Phase 1
NCT03280173	Pfizer	Healthy	September 29, 2017	Phase 1
NCT02697864	Pfizer	Healthy	April 2016	Phase 1
NCT04814186	Pfizer	Transthyretin Amyloid Cardiomyopathy	July 22, 2021	Phase 4
NCT00694161	Pfizer	Cardiomyopathy	August 2008	Phase 2
NCT02746926	Pfizer	Healthy	April 29, 2016	Phase 1
NCT04963985	Peking University Third Hospital	Transthyretin Amyloidosis	June 1, 2021	Phase 4
NCT04828993	Pfizer	Transthyretin Amyloid Polyneuropathy (ATTR-PN)	April 28, 2021	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 37.5 mg/mL ( 121.71 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2455 mL	16.2274 mL	32.4549 mL
5 mM	0.6491 mL	3.2455 mL	6.4910 mL
10 mM	0.3245 mL	1.6227 mL	3.2455 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: 2.5 mg/mL (8.11 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: 2.5 mg/mL (8.11 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

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

References

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

Synonyms

6-Benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)-

2-(3,5-Dichlorophenyl)-6-benzoxazolecarboxylic acid

Fx 1006

Tafamidis

Vyndamax

2-(3,5-Dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid

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