481687-01-8

481687-01-8 structure

Name: JF-5
Chemical Name: MFCD23380199
CAS Number: 481687-01-8
Molecular Formula: C₁₇H₂₂N₂
Molecular Weight: 290.831
Create Date: 2020-01-11 18:36:03
Modify Date: 2024-01-17 17:44:35
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.

Name	MFCD23380199
Synonyms	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)

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)