Cart
sales@molnova.com
Home - Products - Membrane Transporter/Ion Channel - GAT - SKF-89976A hydrochloride

SKF-89976A hydrochloride

CAS No. 85375-15-1

SKF-89976A hydrochloride( SKF89976A hydrochloride )

Catalog No. M16199 CAS No. 85375-15-1

A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 57 Get Quote
10MG 86 Get Quote
25MG 176 Get Quote
50MG 344 Get Quote
100MG 506 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote
Get Quotation Bulk Inquiry Add to Cart

Biological Information

  • Product Name
    SKF-89976A hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1.
  • Description
    A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1; shows little to no activity for rGAT-2, hGAT-3 and hBGT-1 (IC50>500 uM); blocks GABA uptake and uncoupled transmitter-gated current with Ki of 7 uM and 0.03 uM, respectively.
  • In Vitro
    SKF89976A has a weak antiallodynic action. SKF89976A weakly inhibits serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in chinese hamster ovary (CHO) cells stably expressing each transporter using a substrate uptake assay, with IC50 values of 3514 , 202.13, and 728.8, respectively. SKF89976A is a GABA-transport blocker. GABA (1 mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10 μM) and SKF89976A (100 μM), but is unaffected by 100 μM picrotoxin. 100 μM SKF 89976-A is known to block the transport of GABA into cells, completely eliminated the GABA-elicited current in a reversible fashion. SKF89976A is a nontransportable blockers of GAT-1. SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA. SKF89976A (100 μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n=19). Intracellular perfusion of 20 μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n=4).
  • In Vivo
    SKF89976A produces a weak antiallodynic response when administered i.v. (0.3 mg/kg). The i.t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice.
  • Synonyms
    SKF89976A hydrochloride
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    GAT
  • Recptor
    GAT
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    85375-15-1
  • Formula Weight
    371.9003
  • Molecular Formula
    C22H26ClNO2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 34 mg/mL
  • SMILES
    O=C(C1CN(CC/C=C(C2=CC=CC=C2)/C3=CC=CC=C3)CCC1)O
  • Chemical Name
    3-Piperidinecarboxylic acid, 1-(4,4-diphenyl-3-buten-1-yl)-, hydrochloride (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ali FE, et al. J Med Chem. 1985 May;28(5):653-60. 2. Stringer JL, et al. Epilepsy Res. 2002 Dec;52(2):129-37. 3. Krause S, et al. Mol Pharmacol. 2005 Dec;68(6):1728-35.
Calculator

Molecular Weight Calculator

Dilution Calculator

Molarity Calculator

molnova catalog
related products

  • AZD6280

    AZD6280 is a potent, α2/3 functionally selective, partial GABAA receptor modulator with pKi of 7.7.

  • Carisoprodol

    Carisoprodol is a centrally acting skeletal muscle relaxant of the carbamate class and produces all the effects associated with barbiturate receptor ligands.

  • Alprazolam

    Alprazolam (D-65MT;U 31889) is a triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities.

Sign In Join Free