Art. -Nr.: HY-N0663

Talatisamine

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Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca²⁺-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC₅₀=78 μM), and blocking delayed rectifier K⁺ channels (IC₅₀=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.

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Reinheit: 99.77%
CAS. Nr.: 20501-56-8
Formel: C₂₄H₃₉NO₅
Molecular Weight:421.57

Speicherung:

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Talatisamine Chemical Structure

CAS. Nr.: 20501-56-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Cyclophilin D

IKr

Alle Cyclophilin Isoform-spezifische Produkte anzeigen :

In Vitro

Talatisamine (10-200 μM) inhibits Ca²⁺-dependent mPTP opening in isolated rat liver mitochondria in a concentration-dependent manner, with an IC₅₀ of 78 μM^[1].
Talatisamine (10-200 μM) inhibits Ca²⁺-dependent mPTP opening in isolated rat heart mitochondria in a concentration-dependent manner in vitro, and its activity is weaker than that in rat liver mitochondria^[1].
Talatisamine (10-200 μM) exhibits enhanced concentration-dependent inhibition of Ca²⁺-dependent mPTP opening in isolated rat liver mitochondria in the presence of cyclosporin A (CsA)^[1].
Talatisamine (50-200 μM) inhibits Fe²⁺/ascorbic acid-induced MDA production in isolated rat liver mitochondria in vitro in a concentration-dependent manner^[1].
Talatisamine (10-100 μM) inhibits Fe²⁺/ascorbic acid-induced lipid peroxidation (LPO) in isolated rat liver mitochondria in a concentration-dependent manner in vitro, with the maximum inhibitory effect observed at 100 μM^[1].
Talatisamine exhibits no inhibitory effect on voltage-gated Na⁺ or Ca²⁺ currents at concentrations up to 3 mM^[2].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	T_1/2	T_max	CL	V_d	C_max	Bioavailability
Mice^[2]	1 mg/kg	i.v.	970.4 ng·h/mL	986.7 ng·h/mL	1.6 h	1.8 h	1.3 h	0.1 h	1.2 L/h/kg	2.1 L/kg	583.4 ng/mL	/
Mice^[2]	2 mg/kg	p.o.	1261.6 ng·h/mL	1419.6 ng·h/mL	2.1 h	3.2 h	2.5 h	0.8 h	1.5 L/h/kg	4.9 L/kg	614.8 ng/mL	65.0 %
Mice^[2]	4 mg/kg	p.o.	3023.6 ng·h/mL	3050.8 ng·h/mL	1.6 h	1.7 h	1.2 h	0.8 h	1.4 L/h/kg	2.4 L/kg	1716.6 ng/mL	77.9 %
Mice^[2]	8 mg/kg	p.o.	6149.6 ng·h/mL	6208.9 ng·h/mL	1.6 h	1.7 h	1.1 h	0.8 h	1.3 L/h/kg	2.0 L/kg	3045.6 ng/mL	79.2 %

In Vivo

Talatisamine (1 mg/kg; i.v.; single dose; 2-8 mg/kg; p.o.; single dose) exhibits rapid elimination in male ICR mice following intravenous or oral administration, with absolute oral bioavailability ranging from 65.0% to 79.2% across tested doses^[2].

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

Chemical Information

CAS. Nr. 20501-56-8
Appearance Solid
Molecular Weight 421.57
Formel C₂₄H₃₉NO₅
Color White to off-white
SMILES

CO[C@@H]1C(C(N(CC)C2)C3C4)([C@@](C[C@@]5([H])[C@@H]6O)([H])[C@@]6([H])[C@@]3(C[C@@H]5OC)O)[C@@]4([H])[C@@]2(COC)CC1
Structure Classification
- Alkaloids
- Pyrrole Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (118.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.3721 mL

11.8604 mL

23.7209 mL

5 mM

0.4744 mL

2.3721 mL

4.7442 mL

10 mM

0.2372 mL

1.1860 mL

2.3721 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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 (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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 (5.93 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 (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Muratova D K, et al. Effect of talatisamine and its derivate 14-O-benzoyltalatisamine on functional state of rat liver and heart mitochondria[J]. Biomedical and Pharmacology Journal, 2023, 16(4): 2333-2343.

[2]. Chen M, et al. Quantitative determination of talatisamine and its pharmacokinetics and bioavailability in mouse plasma by UPLC-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2019;1124:180-187. [Content Brief]

[3]. Huang S, et al. Metabolite profiling of talatisamine in heart tissue after oral administration and analysis of cardiac bioactivities[J]. Planta Medica, 2023, 89(06): 674-682.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3721 mL	11.8604 mL	23.7209 mL	59.3021 mL
	5 mM	0.4744 mL	2.3721 mL	4.7442 mL	11.8604 mL
	10 mM	0.2372 mL	1.1860 mL	2.3721 mL	5.9302 mL
	15 mM	0.1581 mL	0.7907 mL	1.5814 mL	3.9535 mL
	20 mM	0.1186 mL	0.5930 mL	1.1860 mL	2.9651 mL
	25 mM	0.0949 mL	0.4744 mL	0.9488 mL	2.3721 mL
	30 mM	0.0791 mL	0.3953 mL	0.7907 mL	1.9767 mL
	40 mM	0.0593 mL	0.2965 mL	0.5930 mL	1.4826 mL
	50 mM	0.0474 mL	0.2372 mL	0.4744 mL	1.1860 mL
	60 mM	0.0395 mL	0.1977 mL	0.3953 mL	0.9884 mL
	80 mM	0.0297 mL	0.1483 mL	0.2965 mL	0.7413 mL
	100 mM	0.0237 mL	0.1186 mL	0.2372 mL	0.5930 mL

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Alle Cyclophilin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Talatisamine Related Classifications

HY-N0663 Related Classifications