Home Tools

SKF89976A hydrochloride

Catalog No. T12930 CAS 85375-15-1

Synonyms: 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SKF89976A hydrochloride Chemical Structure

SKF89976A hydrochloride, CAS 85375-15-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 63.00
10 mg	In stock	$ 96.00
25 mg	In stock	$ 196.00
50 mg	In stock	$ 382.00
100 mg	In stock	$ 562.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

Bulk Inquiry

Select Batch

Purity: 98.72%

Biological Description

Chemical Properties

Storage & Solubility Information

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-1:137.34 μM , GAT-3:202.8 μM , GAT-1:0.28 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
Molecular Weight	371.9
Formula	C22H26ClNO2
CAS No.	85375-15-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

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

References and Literature

1. Jinzenji A, et al. Antiallodynic action of 1-(3-(9H-Carbazol-9-yl)-1-propyl)-4-(2-methyoxyphenyl)-4-piperidinol (NNC05-2090), a betaine/GABA transporter inhibitor. J Pharmacol Sci. 2014;125(2):217-26. 2. Kreitzer MA, et al. Glutamate modulation of GABA transport in retinal horizontal cells of the skate. J Physiol. 2003 Feb 1;546(Pt 3):717-31. 3. Barakat L, et al. GAT-1 and reversible GABA transport in Bergmann glia in slices. J Neurophysiol. 2002 Sep;88(3):1407-19.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Ion Channel Inhibitor Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

Tiagabine Topiramate Gabapentin (R)-baclofen DL-Menthol SCH 50911 hydrochloride AZD-6280 CGP 36742

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

SKF89976A hydrochloride 85375-15-1 Membrane transporter/Ion channel Neuroscience GABA Receptor Gamma-aminobutyric acid Receptor SKF89976A Hydrochloride γ-Aminobutyric acid Receptor d,l-SKF89976A d,l-SKF89976A Hydrochloride d,l-SKF89976A hydrochloride SKF89976A inhibit Inhibitor SKF-89976A hydrochloride inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.