Art. -Nr.: HY-14852

Tafamidis

Name: Tafamidis
Brand: MedChemExpress
SKU: HY-14852
Price: 66.00 USD
Availability: InStock
Rating: 5 (2 reviews)

(Synonyms: Fx-1006A free acid)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Tafamidis (Fx-1006A (free acid)) is an orally active and selective transthyretin (TTR) stabilizer. Tafamidis binds to the thyroxine binding site with negative cooperativity, stabilizes the TTR tetramer, slows TTR tetramer dissociation and subunit exchange, and inhibits TTR fibril formation. Tafamidis can be used in research on nervous system-related diseases.

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Reinheit : 99.93%
CAS. Nr.: 594839-88-0
Formel: C₁₄H₇Cl₂NO₃
Molecular Weight:308.12

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tafamidis Chemical Structure

CAS. Nr.: 594839-88-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Tafamidis exhibits high permeability in Caco-2 monolayer cells, with a P_app (A-to-B) of 30.9 × 10^-6 cm/s and an efflux ratio of 1.04; it is stable in rat liver microsomes, with 94.0% remaining unchanged after 300 min and an in vitro intrinsic clearance of 51.0 mL/h/kg^[1].
Tafamidis is highly bound to rat plasma proteins, with a binding rate of 99.8% at 2 μg/mL and a blood-to-plasma partition ratio of 56.6%^[1].
Tafamidis binds recombinant wild-type TTR and human plasma TTR with high selectivity and high affinity, and effectively inhibits the dissociation of wild-type TTR and more than 35 TTR mutant heterotetramers, including Val30Met and Val122Ile; it stabilizes TTR tetramers by slowing subunit exchange of the TTR tetramer and inhibiting tetramer dissociation^[2].
Tafamidis inhibits WT, V30M, and V122I TTR fibril formation with an EC₅₀ of 2.7-3.2 μM^[3].
Tafamidis shows a dose-dependent kinetic stabilization effect on WT-TTR under 6.5 M urea conditions, reducing dissociation to 33% at a 1:1 molar ratio and to below 3% at 2:1^[3].
Tafamidis binds WT-TTR with negative cooperativity, yielding K_d1 = 2 nM and K_d2 = 154 nM as derived from subunit exchange modeling^[3].
Tafamidis binding to TTR exhibits negative cooperativity, and the dissociation constants of its two binding sites are determined by two methods: single-exponential fitting of binding and second-order binding polynomial fitting yield K_d1 = 2 nM and K_d2 = 154 nM; isothermal titration calorimetry measurements yield K_d1 = 3 nM and K_d2 = 278 nM^[3].
Tafamidis selectively binds TTR in human plasma; in human plasma systems, it resists 4.8 M urea denaturation and exerts a stabilizing effect on wild-type, V30M, and V122I TTR tetramers; moreover, in a urea-denaturing environment, it also stabilizes various TTR variants in human plasma, including V30M, Y69H, F64S, I84S, V122I, and L111M^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_last	AUC_inf	MRT	Clearance (CL)	V_ss	F
Rat^[1]	0.3 mg/kg	i.v.	0.0833 h	2.51 μg/mL	46.9 h	39.3 μg·h/mL	43.3 μg·h/mL	51.6 h	7.03 mL/h/kg	354 mL/kg	/
Rat^[1]	1 mg/kg	i.v.	0.0833 h	11.4 μg/mL	39.5 h	146 μg·h/mL	155 μg·h/mL	44.0 h	6.52 mL/h/kg	286 mL/kg	/
Rat^[1]	3 mg/kg	i.v.	0.0833 h	31.6 μg/mL	48.6 h	436 μg·h/mL	470 μg·h/mL	42.4 h	6.41 mL/h/kg	270 mL/kg	/
Rat^[1]	0.3 mg/kg	p.o.	1.63 h	1.65 μg/mL	61.9 h	40.3 μg·h/mL	47.7 μg·h/mL	71.8 h	/	/	103 %
Rat^[1]	1 mg/kg	p.o.	2.00 h	6.57 μg/mL	34.8 h	146 μg·h/mL	153 μg·h/mL	41.4 h	/	/	99.7 %
Rat^[1]	3 mg/kg	p.o.	0.583 h	22.6 μg/mL	35.4 h	455 μg·h/mL	474 μg·h/mL	36.5 h	/	/	104 %

Chemical Information

CAS. Nr. 594839-88-0
Appearance Solid
Molecular Weight 308.12
Formel C₁₄H₇Cl₂NO₃
Color White to off-white
SMILES

O=C(C1=CC=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1)O
Synonyms

Fx-1006A free acid
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

J Med Chem

Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. [Abstract]

2021 Oct 14;64(19):14344-14357. PMID: 34547896
Vascul Pharmacol

Antithrombotic properties of Tafamidis: An additional protective effect for transthyretin amyloid cardiomyopathy patients. [Abstract]

2024 Jul 17:107411. PMID: 39029855

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 37.5 mg/mL (121.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 1 mg/mL (3.25 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lee K R, et al. Pharmacokinetics of tafamidis, a transthyretin amyloidosis drug, in rats. Xenobiotica, 2018, 48(8):831-838.

[2]. Coelho T, et al. Mechanism of Action and Clinical Application of Tafamidis in Hereditary Transthyretin Amyloidosis. Neurology and therapy. 2016 Jun;5(1):1-25.

[3]. Bulawa C E, et al. Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. PNAS, 2012, 109(24):9629-9634.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	3.2455 mL	16.2274 mL	32.4549 mL	81.1372 mL
DMSO	5 mM	0.6491 mL	3.2455 mL	6.4910 mL	16.2274 mL
	10 mM	0.3245 mL	1.6227 mL	3.2455 mL	8.1137 mL
	15 mM	0.2164 mL	1.0818 mL	2.1637 mL	5.4091 mL
	20 mM	0.1623 mL	0.8114 mL	1.6227 mL	4.0569 mL
	25 mM	0.1298 mL	0.6491 mL	1.2982 mL	3.2455 mL
	30 mM	0.1082 mL	0.5409 mL	1.0818 mL	2.7046 mL
	40 mM	0.0811 mL	0.4057 mL	0.8114 mL	2.0284 mL
	50 mM	0.0649 mL	0.3245 mL	0.6491 mL	1.6227 mL
	60 mM	0.0541 mL	0.2705 mL	0.5409 mL	1.3523 mL
	80 mM	0.0406 mL	0.2028 mL	0.4057 mL	1.0142 mL
	100 mM	0.0325 mL	0.1623 mL	0.3245 mL	0.8114 mL

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Keywords

Tafamidis

2 Cited Publications

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Tafamidis

Publications Citing Use of MedChemExpress (MCE) Tafamidis