371825
GPCR-Helix 8 Signaling Inhibitor, JF5
The GPCR-Helix 8 Signaling Inhibitor, JF5 controls the biological activity of GPCR-Helix 8. This small molecule/inhibitor is primarily used for Biochemicals applications.
Synonym(s):
GPCR-Helix 8 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, GPCR-H8 Signaling Inhibitor, JF5
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About This Item
Empirical Formula (Hill Notation):
C17H22N2 · xHI
Molecular Weight:
254.37
UNSPSC Code:
12352200
Assay:
≥92% (HPLC)
Form:
powder
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
assay
≥92% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
off-white
solubility
DMSO: 50 mg/mL
shipped in
wet ice
storage temp.
2-8°C
General description
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 Gαq, but not Gα12. A non-orthosteric antagonist of PAR1 (IC50 = 4 µM) 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 ~1 mg/kg). Also acts as a potent, non-competitive blocker of α2A-adrenergic receptors (IC50 = 2.5 µM as shown by a decrease in 3H-yohimbine binding).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Dowal, L., et al. 2011. Proc. Natl. Acad. Sci. USA108, 2951.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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