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SKF89976A hydrochloride

Name: SKF89976A hydrochloride
Brand: TargetMol
SKU: T12930
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12930Cas No. 85375-15-1

Alias d,l-SKF89976A hydrochloride

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

SKF89976A hydrochloride

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Purity: 98.02%

Catalog No. T12930Alias d,l-SKF89976A hydrochlorideCas No. 85375-15-1

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$63	In Stock	In Stock
10 mg	$96	In Stock	In Stock
25 mg	$179	In Stock	In Stock
50 mg	$293	In Stock	In Stock
100 mg	$455	In Stock	In Stock
200 mg	$655	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.02%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.
Targets&IC50	GAT-3:202.8 μM , GAT-1:0.28 μM , GAT-1:137.34 μM
In vitro	SKF89976A exhibits weak antiallodynic properties and mildly inhibits the serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in Chinese hamster ovary (CHO) cells that stably express these transporters, as demonstrated in substrate uptake assays with IC50 values of 3514, 202.13, and 728.8, respectively. Additionally, SKF89976A functions as a GABA-transport blocker, effectively suppressing GABA-induced inward currents in the presence of GABA transport inhibitors tiagabine and SKF89976A at specified concentrations, while remaining unaffected by picrotoxin. Remarkably, SKF89976A, at a concentration of 100 μM, can reversibly block GABA transport into cells, thus eliminating GABA-elicited currents. It further acts as a non-transportable blocker of GAT-1, reducing baseline inward currents likely due to tonic GAT activation by background GABA. At a concentration of 100 μM, SKF89976A was able to reversibly reduce GAT currents by 67.9±4.4% in all studied cells (n=19), and a 20 μM intracellular perfusion of SKF89976-A progressively diminished and blocked GABA-induced GAT currents without affecting GABAAR-mediated currents.
In vivo	When administered i.v. (0.3 mg/kg), SKF89976A produces a weak antiallodynic response . The i.t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice[1].
Synonyms	d,l-SKF89976A hydrochloride

Chemical Properties

Molecular Weight	371.9
Formula	C₂₂H₂₆ClNO₂
Cas No.	85375-15-1
Smiles	Cl.OC(=O)C1CCCN(CCC=C(c2ccccc2)c2ccccc2)C1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 20 mg/mL (53.78 mM), Sonication is recommended.

DMSO: 100 mg/mL (268.89 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.76 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6889 mL	13.4445 mL	26.8889 mL	134.4447 mL
5 mM	0.5378 mL	2.6889 mL	5.3778 mL	26.8889 mL
10 mM	0.2689 mL	1.3444 mL	2.6889 mL	13.4445 mL
20 mM	0.1344 mL	0.6722 mL	1.3444 mL	6.7222 mL
50 mM	0.0538 mL	0.2689 mL	0.5378 mL	2.6889 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0269 mL	0.1344 mL	0.2689 mL	1.3444 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc