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Merck

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
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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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

Quality Level

100

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)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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