Talatisamine | CAS:20501-56-8 | Manufacturer ChemFaces

Talatisamine

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Description:

Talatisamine is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. Talatisamine (120 μM) and TEA (5mM) inhibits the enhanced I(K) caused by Aβ40 oligomers, attenuates cytotoxicity of Aβ oligomers by restoring cell viability and suppressing K(+) loss related apoptotic response.

Targets:

Bcl-2/Bax | Caspase | Beta Amyloid | Calcium Channel | Potassium Channel

In vitro:

Neurosci Lett. 2012 Jun 19;518(2):122-7.

The newly identified K+ channel blocker talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.[Pubmed: 22561032]

Loss of cytosolic K(+) through up-regulated delayed rectifier K(+) channels play an important role in beta-amyloid (Aβ) induced neurotoxicity. Potent K(+) channel blocker, particular specific for I(K) channels has been suggested as an attractive candidate for the treatment of Alzheimer's disease (AD). Talatisamine is a novel I(K) channel blocker discovered by virtual screening and electrophysiological characterization.
METHODS AND RESULTS:
In the present study, we examined the neuroprotective effect of Talatisamine against Aβ oligomers induced cytotoxicity in primarily cultured cortical neurons. The neurotoxicity related to K(+) loss caused by Aβ40 oligomers included enhanced I(K) density, increased cell membrane permeability, reduced cell viability, and impaired mitochondrial transmembrane potential. Decreased Bcl-2 and increased Bax level, activation of Caspase-3 and Caspase-9 were also observed after Aβ40 oligomers incubation. Talatisamine (120 μM) and TEA (5mM) inhibited the enhanced I(K) caused by Aβ40 oligomers, attenuated cytotoxicity of Aβ oligomers by restoring cell viability and suppressing K(+) loss related apoptotic response.
CONCLUSIONS:
Our results suggested that Talatisamine may become a leading compound as I(K) channel blocker for neuroprotection.

Talatisamine Description

Source:	The roots of Aconitum carmichaeli Debx.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Neuroscience. 2008 Aug 13;155(2):469-75.

Discovery of talatisamine as a novel specific blocker for the delayed rectifier K+ channels in rat hippocampal neurons.[Pubmed: 18601983]

Blocking specific K+ channels has been proposed as a promising strategy for the treatment of neurodegenerative diseases. Using a computational virtual screening approach and electrophysiological testing, we found four Aconitum alkaloids are potent blockers of the delayed rectifier K+ channel in rat hippocampal neurons.
METHODS AND RESULTS:
In the present study, we first tested the action of the four alkaloids on the voltage-gated K+, Na+ and Ca2+ currents in rat hippocampal neurons, and then identified that Talatisamine is a specific blocker for the delayed rectifier K+ channel. External application of Talatisamine reversibly inhibited the delayed rectifier K+ current (IK) with an IC50 value of 146.0+/-5.8 microM in a voltage-dependent manner, but exhibited very slight blocking effect on the voltage-gated Na+ and Ca2+ currents even at the high concentration of 1-3 mM. Moreover, Talatisamine exerted a significant hyperpolarizing shift of the steady-state activation, but did not influence the steady state inactivation of IK and its recovery from inactivation, suggesting that Talatisamine had no allosteric action on IK channel and was a pure blocker binding to the external pore entry of the channel.
CONCLUSIONS:
Our present study made the first discovery of potent and specific IK channel blocker from Aconitum alkaloids. It has been argued that suppressing K+ efflux by blocking IK channel may be favorable for Alzheimer's disease therapy. Talatisamine can therefore be considered as a leading compound worthy of further investigations.

Product Name	Talatisamine
Price:	$288 / 20mg
CAS No.:	20501-56-8
Catalog No.:	CFN98580
Molecular Formula:	C₂₄H₃₉NO₅
Molecular Weight:	421.57 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:	The roots of Aconitum carmichaeli Debx.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF Manual
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library Potassium Channel Inhibitor Library Caspase Inhibitor Library Calcium Channel Inhibitor Library Beta Amyloid Inhibitor Library Bcl-2/Bax Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.3721 mL	11.8604 mL	23.7209 mL	47.4417 mL	59.3021 mL
5 mM	0.4744 mL	2.3721 mL	4.7442 mL	9.4883 mL	11.8604 mL
10 mM	0.2372 mL	1.186 mL	2.3721 mL	4.7442 mL	5.9302 mL
50 mM	0.0474 mL	0.2372 mL	0.4744 mL	0.9488 mL	1.186 mL
100 mM	0.0237 mL	0.1186 mL	0.2372 mL	0.4744 mL	0.593 mL

CFN98583	13-Dehydroxyindaconintine	N/A	613.74	C₃₄H₄₇NO₉
CFN99501	Indaconitine	4491-19-4	629.82	C₃₄H₄₇NO₁₀
CFN96413	Yunaconitoline	259099-25-7	625.69	C₃₄H₄₃NO₁₀
CFN90373	Crassicauline A	79592-91-9	643.77	C₃₅H₄₉NO₁₀
CFN89452	Carmichaenine A	2065228-59-1	541.67	C₃₁H₄₃NO₇
CFN89453	Carmichaenine E	2065228-63-7	557.67	C₃₁H₄₃NO₈
CFN90689	Fuziline	80665-72-1	453.58	C₂₄H₃₉NO₇
CFN98580	Talatisamine	20501-56-8	421.57	C₂₄H₃₉NO₅
CFN96243	10-Hydroxyneoline	132362-42-6	453.6	C₂₄H₃₉NO₇
CFN96267	Neolinine	112515-37-4	423.6	C₂₃H₃₇NO₆