| Identification | Back Directory | [Name]
7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2) | [CAS]
1216720-69-2 | [Synonyms]
SCH 79797 (hydrochloride)
7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2) | [Molecular Formula]
C23H25N5 | [MDL Number]
MFCD04039788 | [MOL File]
1216720-69-2.mol | [Molecular Weight]
371.478 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at 2-8°C, protect from light | [solubility ]
Soluble to 25 mM in ethanol and to 50 mM in DMSO | [form ]
Powder | [color ]
White to yellow |
| Hazard Information | Back Directory | [Description]
SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1). 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). SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation. It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells. | [Uses]
N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine Dihydrochloride is a selective PAR1 antagonist which was shown to limit myocardial ischemia/reperfusion injury in rat hearts. | [in vivo]
SCH79797 (2.5-250 μg/kg; intravenous injection; male Sprague Dawley rats) treatment immediately before or during ischemia reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury. This response is dose-dependent with the optimal dose being 25 μg/kg[4]. | Animal Model: | Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury[4] | | Dosage: | 2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg, and 250 μg/kg | | Administration: | Intravenous injection | | Result: | Immediately before or during ischemia reduced myocardial necrosis following I/R in the intact rat heart.
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| [IC 50]
PAR1 | [storage]
Desiccate at RT | [References]
[1] HO-SAM AHN. Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists[J]. Bioorganic & Medicinal Chemistry Letters, 1999, 9 14: Pages 2073-2078. DOI: 10.1016/s0960-894x(99)00339-x
[2] HO-SAM AHN . 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[J]. Biochemical pharmacology, 2000, 60 10: Pages 1425-1434. DOI: 10.1016/s0006-2952(00)00460-3
[3] ELAINE A LIDINGTON. A role for proteinase-activated receptor 2 and PKC-epsilon in thrombin-mediated induction of decay-accelerating factor on human endothelial cells.[J]. American journal of physiology. Cell physiology, 2005, 289 6: C1437-47. DOI: 10.1152/ajpcell.00502.2004 |
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BOC Sciences
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https://www.bocsci.com |
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