An antagonist of PAR1
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Product Type

Small Molecule Modulators
Receptor Pharmacology
Antagonists

Research Area

SCH 79797 (hydrochloride)

Item No. 14633

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine, monohydrochloride
CAS Number
1216720-69-2
Molecular Formula
C23H25N5 • 2HCl
Formula Weight
444.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 11 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/mlEthanol: 1 mg/ml
λmax
214, 246, 340 nm
SMILES
NC1=NC(NC2CC2)=NC3=CC=C(N(CC4=CC=C(C(C)C)C=C4)C=C5)C5=C31.Cl.Cl
InChi Code
InChI=1S/C23H25N5.2ClH/c1-14(2)16-5-3-15(4-6-16)13-28-12-11-18-20(28)10-9-19-21(18)22(24)27-23(26-19)25-17-7-8-17;;/h3-6,9-12,14,17H,7-8,13H2,1-2H3,(H3,24,25,26,27);2*1H
InChi Key
NNJTXSQXGHYXAJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1).1 It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively).2 SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation.2 It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ahn, H.S., Arik, L., Boykow, G., et al. Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists. Bioorg. Med. Chem. Lett. 9(14), 2073-2078 (1999).

    2. Ahn, H.S., Foster, C., Boykow, G., et al. Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem. Pharmacol. 60(10), 1425-1434 (2000).

    3. Lidington, E.A., Steinberg, R., Kinderlerer, A.R., et al. A role for proteinase-activated receptor 2 and PKC-ε in thrombin-mediated induction of decay-accelerating factor on human endothelial cells. Am. J. Physiol. Cell Physiol. 289(6), 1437-1447 (2005).