Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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ln Vitro |
Weak antiallodynic effects are shown with SKF89976A. SKF89976A mildly inhibits the norepinephrine transporter (NET), dopamine transporter (DAT), and serotonin transporter (SERT) in Chinese hamster ovary (CHO) cells that are stable transducers of each transporter, as determined by a substrate uptake experiment. 3514, 202.13, and 728.8 are the IC50 values, respectively [1]. A GABA transmission blocker is SKF89976A. The inward current generated by GABA (1 mM) was not impacted by 100 μM picrotoxin, but it was totally suppressed by the GABA transport inhibitors tiagabine (10 μM) and SKF89976A (100 μM). It is known that 100 μM SKF 89976-A fully and reversibly blocks GABA-induced currents via blocking GABA transport into cells [2]. GAT-1 is blocked non-transferably by SKF89976A. Additionally, baseline inward currents that may result from background GABA activation of tonic GAT are inhibited by SKF89976-A. In every cell under investigation, SKF89976A (100 μM) reversibly decreased GAT current by 67.9±4.4% (n= 19). GABA-induced GAT currents were gradually decreased and inhibited by intracellular infusion of 20 μM SKF89976-A, whereas GABAAR-mediated currents (n=4) were not prevented [3].
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ln Vivo |
SKF89976A given intravenously (0.3 mg/kg) elicits a mild antiallodynic effect. In PSL model mice, injection of SKF89976A can improve the decrease of withdrawal threshold in a dose-dependent manner [1].
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References |
[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 |
Molecular Formula |
C22H25NO2.HCL
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Molecular Weight |
371.90034
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Elemental Analysis |
C, 71.05; H, 7.05; Cl, 9.53; N, 3.77; O, 8.60
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CAS # |
85375-15-1
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Related CAS # |
85375-15-1 ( free base);85375-85-5 (HCl);
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Appearance |
Solid powder
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SMILES |
O=C(C1CN(CC/C=C(C2=CC=CC=C2)/C3=CC=CC=C3)CCC1)O.[H]Cl
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Synonyms |
SKF89976A HCl; SKF 89976A; SKF-89976A; SKF89976A hydrochloride
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~268.89 mM)
H2O : ~20 mg/mL (~53.78 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (67.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6889 mL | 13.4445 mL | 26.8889 mL | |
5 mM | 0.5378 mL | 2.6889 mL | 5.3778 mL | |
10 mM | 0.2689 mL | 1.3444 mL | 2.6889 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.