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Chemical Structure : JF-5
Catalog No.: PC-62040Not For Human Use, Lab Use Only.
JF5 (PAR1 inhibitor JF5) is an allosteric inhibitor of PAR1 that binds to helix 8 of the receptor.
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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.
JF5 also interacts with the α2A-adrenergic receptor.
JF5 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.
JF5 inhibited thrombus formation in vivo following vascular injury with IC50 of 1 mg/kg.
JF5 is a useful probe to evaluate the role of H8 in coupling of GPCRs to cognate Gα subunits.
| M.Wt | 290.835 | |
| Formula | C17H22N2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Dowal L, et al. Proc Natl Acad Sci U S A. 2011 Feb 15;108(7):2951-6.
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