A PAR2 antagonist
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I-191

Item No. 37553

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[8-(1,1-dimethylethyl)-6-(4-fluorophenyl)imidazo[1,2-b]pyridazin-2-yl]carbonyl]-3,3-dimethyl-2-piperazinone
CAS Number
1690172-25-8
Molecular Formula
C23H26FN5O2
Formula Weight
423.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
λmax
245, 283 nm
SMILES
O=C(N1CCNC(C1(C)C)=O)C2=CN3N=C(C4=CC=C(F)C=C4)C=C(C(C)(C)C)C3=N2
InChi Code
InChI=1S/C23H26FN5O2/c1-22(2,3)16-12-17(14-6-8-15(24)9-7-14)27-29-13-18(26-19(16)29)20(30)28-11-10-25-21(31)23(28,4)5/h6-9,12-13H,10-11H2,1-5H3,(H,25,31)
InChi Key
DTASTQAQBOZSRR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

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    100 mg

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    Cayman Chemical
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    Product Description

    I-191 is an antagonist of proteinase-activated receptor 2 (PAR2; IC50 = 72.4 nM in HT-29 cells expressing the human receptor).1 It inhibits trypsin-induced calcium release in HT-29 cells (IC50 = 200 nM for the human receptor). I-191 (0.1, 1, and 10 µM) reduces the migration of HT-29 cells in a scratch assay. It decreases the expression of mRNA encoding chemokine (C-X-C motif) ligand 8 (CXCL8) in, and secreted IL-8 levels from, HT-29 cells induced by the PAR2 agonist 2f-LIGRL-NH2 when used at a concentration of 1 and 10 µM. Ex vivo, I-191 (10 µM) inhibits tissue factor-induced clotting using isolated human whole blood.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jiang, Y., Yau, M.K., Lim, J., et al. A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling functions in human cancer cells. J. Pharmacol. Exp. Ther. 364(2), 246-257 (2018).

    2. Iyer, A., Humphries, T.L.R., Owens, E.P., et al. PAR2 activation on human kidney tubular epithelial cells induces tissue factor synthesis, that enhances blood clotting. Front. Physiol. 12, 615428 (2021).