A cell-permeable quinolinimine compound that acts as a selective, potent blocker of G-protein coupled receptors (GPCR) that contain a constrained eighth helix (H8). The inhibition is selective and blocks G-protein signaling mediated via Gaq, but not Ga12. A non-orthosteric antagonist of PAR1 (IC50=4uM) that is shown to inhibit PAR1 and CCR-4 induced platelet aggregation without affecting PAR4 mediated aggregation. Shown to inhibit thrombus formation following vascular injury (IC50 ~1mg/kg). Also acts as a potent, non-competitive blocker of a2A-adrenergic receptors (IC50=2.5uM as shown by a decrease in 3H-yohimbine binding).
Formula:C17H22N2 · HI
Solubility:DMSO
Molecular Weight:382.3
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
![GPCR-Helix 8 Signaling Inhibitor, JF5 (GPCR-H8 Signaling Inhibitor, JF5, 4-Pentyl-2,3-dihydro-1H-cyclopenta[b]quinolin-9-imine, HI, 4-Pentyl-1,2,3,4-tetrahydro-9H-cyclopenta[b]quinolin-9-imine, HI) 10mg](https://aimg.as-1.co.jp/c/85/2073/14/85133520.jpg)