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
• Empirical Formula (Hill Notation): C₁₇H₂₂N₂ · xHI
• Molecular Weight: 254.37
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

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 G_αq, but not G_α12. 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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable