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JF-5

Names

[ CAS No. ]:
481687-01-8

[ Name ]:
JF-5

[Synonym ]:
4-Pentyl-1,2,3,4-tetrahydro-9H-cyclopenta[b]quinolin-9-imine hydrochloride (1:1)
MFCD23380199
1,2,3,4-Tetrahydro-4-pentyl-9H-cyclopenta[b]quinolin-9-imine hydrochloride
JF5 hydrochloride
9H-Cyclopenta[b]quinolin-9-imine, 1,2,3,4-tetrahydro-4-pentyl-, hydrochloride (1:1)

Biological Activity

[Description]:

JF5 (PAR1 inhibitor JF5) is an allosteric inhibitor of PAR1 that binds to helix 8 of the receptor; inhibits PAR1 coupling to Gα subunits, but fails to inhibit signaling downstream of Gα12/13; also interacts with the α2A-adrenergic receptor; blocks granule secretion from platelets activated with the PAR1 agonist SFLLRN with IC50 of 4 uM, inhibits AYPGKF-mediated activation of murine platelets with IC50 of 10 uM; inhibited thrombus formation in vivo following vascular injury with IC50 of 1 mg/kg; a useful probe to evaluate the role of H8 in coupling of GPCRs to cognate Gα subunits.

[References]

References 1. Dowal L, et al. Proc Natl Acad Sci U S A. 2011 Feb 15;108(7):2951-6. View Related Products by Target Protease-activated Receptor (PAR)

Chemical & Physical Properties

[ Molecular Formula ]:
C17H22N2

[ Molecular Weight ]:
290.831

[ Exact Mass ]:
290.154968

Related Compounds

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