SCH 79797 dihydrochloridePotent, selective non-peptide PAR1 antagonist CAS# 1216720-69-2 |
- Plerixafor (AMD3100)
Catalog No.:BCC1158
CAS No.:110078-46-1
- Reparixin
Catalog No.:BCC1885
CAS No.:266359-83-5
- Reparixin L-lysine salt
Catalog No.:BCC1886
CAS No.:266359-93-7
- AMD-070
Catalog No.:BCC1357
CAS No.:558447-26-0
- AMD-070 hydrochloride
Catalog No.:BCC1358
CAS No.:880549-30-4
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1216720-69-2 | SDF | Download SDF |
PubChem ID | 45073452 | Appearance | Powder |
Formula | C23H27Cl2N5 | M.Wt | 444.41 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 25 mM in ethanol and to 50 mM in DMSO | ||
Chemical Name | 3-N-cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamine;dihydrochloride | ||
SMILES | CC(C)C1=CC=C(C=C1)CN2C=CC3=C2C=CC4=C3C(=NC(=N4)NC5CC5)N.Cl.Cl | ||
Standard InChIKey | NNJTXSQXGHYXAJ-UHFFFAOYSA-N | ||
Standard InChI | 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 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Potent, selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). Inhibits haTRAP-induced- but not γ-thrombin-, ADP- or collagen-induced human platelet aggregation. Also selectively blocks PAR1 agonist- or thrombin-induced increases in cytosolic Ca2+ in vascular smooth muscle cells. |
SCH 79797 dihydrochloride Dilution Calculator
SCH 79797 dihydrochloride Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.2502 mL | 11.2509 mL | 22.5017 mL | 45.0035 mL | 56.2544 mL |
5 mM | 0.45 mL | 2.2502 mL | 4.5003 mL | 9.0007 mL | 11.2509 mL |
10 mM | 0.225 mL | 1.1251 mL | 2.2502 mL | 4.5003 mL | 5.6254 mL |
50 mM | 0.045 mL | 0.225 mL | 0.45 mL | 0.9001 mL | 1.1251 mL |
100 mM | 0.0225 mL | 0.1125 mL | 0.225 mL | 0.45 mL | 0.5625 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- Trap 101
Catalog No.:BCC7390
CAS No.:1216621-00-9
- 2-Cyclopropyl-4-(4-fluorophenyl)quinoline-3-carboxaldehyde
Catalog No.:BCC8573
CAS No.:121660-37-5
- 2-Cyclopropyl-4-(4-fluorophenyl)-quinolyl-3-methanol
Catalog No.:BCC8574
CAS No.:121660-11-5
- ZK 93423 hydrochloride
Catalog No.:BCC7227
CAS No.:1216574-52-5
- BX 513 hydrochloride
Catalog No.:BCC5940
CAS No.:1216540-18-9
- Kaempferol-3-O-(2',6'-di-O-trans-p-coumaroyl)-beta-D-glucopyranoside
Catalog No.:BCN1603
CAS No.:121651-61-4
- SB 258585 hydrochloride
Catalog No.:BCC7216
CAS No.:1216468-02-8
- YM 298198 hydrochloride
Catalog No.:BCC7366
CAS No.:1216398-09-2
- 6-Demethoxycleomiscosin A
Catalog No.:BCN7299
CAS No.:121587-20-0
- 6-Demethoxy-9'-deoxycleomiscosin A
Catalog No.:BCN7298
CAS No.:121587-18-6
- Valspodar
Catalog No.:BCC2027
CAS No.:121584-18-7
- DMCM hydrochloride
Catalog No.:BCC7560
CAS No.:1215833-62-7
- BYK 191023 dihydrochloride
Catalog No.:BCC7506
CAS No.:1216722-25-6
- GSK 4112
Catalog No.:BCC7741
CAS No.:1216744-19-2
- ZK 93426 hydrochloride
Catalog No.:BCC7229
CAS No.:1216792-30-1
- CGP 20712 dihydrochloride
Catalog No.:BCC6893
CAS No.:1216905-73-5
- Sarafotoxin S6c
Catalog No.:BCC5721
CAS No.:121695-87-2
- Moluccanin
Catalog No.:BCN6107
CAS No.:121700-26-3
- Moluccanin diacetate
Catalog No.:BCN6108
CAS No.:121700-27-4
- PTC209 HBr
Catalog No.:BCC5640
CAS No.:1217022-63-3
- BU 239 hydrochloride
Catalog No.:BCC5668
CAS No.:1217041-98-9
- GYKI 47261 dihydrochloride
Catalog No.:BCC7566
CAS No.:1217049-32-5
- 6-O-p-Methoxycinnamoylcatalpol
Catalog No.:BCN6109
CAS No.:121710-02-9
- CP 31398 dihydrochloride
Catalog No.:BCC2406
CAS No.:1217195-61-3
A role for proteinase-activated receptor 2 and PKC-epsilon in thrombin-mediated induction of decay-accelerating factor on human endothelial cells.[Pubmed:16079188]
Am J Physiol Cell Physiol. 2005 Dec;289(6):C1437-47.
Thrombin, an important mediator of thrombosis and inflammation, may also enhance vascular cytoprotection. Thus thrombin induces expression of the complement-inhibitory protein decay-accelerating factor (DAF) in human umbilical vein endothelial cells (HUVECs), thus increasing protection against complement-mediated injury. Using PKC isozyme-specific peptide antagonists and adenoviral constructs, we have shown in the present study that PKC-epsilon is the primary isozyme involved in DAF induction by thrombin. Experiments with proteinase-activated receptor-1 (PAR1) and PAR2 activating peptides (APs) showed that DAF expression induced by PAR1-AP was PKC-alpha-dependent; in contrast, PAR2-AP induction of DAF required activation of PKC-epsilon. PAR1-AP and PAR2-AP in combination exerted an additive effect on DAF protein expression, which was equivalent to that observed with thrombin alone. These data implied a specific role for PAR2 in DAF induction, which was supported by the observation that upregulation of endothelial cell (EC) PAR2-enhanced DAF induction by thrombin. ERK1/2, p38, and JNK MAPK were also involved in thrombin-induced DAF upregulation, with evidence of interdependence between ERK1/2 and JNK. A role for transactivation of PAR2 by PAR1 was suggested by partial inhibition of thrombin-induced DAF expression by the PAR1 signaling antagonists BMS-200261 and SCH79797, whereas inhibition of thrombin-induced cleavage of PAR1 by specific MAbs or hirudin completely abrogated the response. Together, these data imply that the predominant pathway for thrombin-induced DAF expression involves transactivation of PAR2 by PAR1 and signaling via PKC-epsilon/MAPK. This may represent an important, novel pathway for endothelial cytoprotection during inflammation and angiogenesis and suggests that PAR2 may play a central role in some thrombin-induced responses.
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.[Pubmed:11020444]
Biochem Pharmacol. 2000 Nov 15;60(10):1425-34.
A growing body of evidence suggests an important contribution of the cellular actions of thrombin to thrombosis and restenosis following angioplasty. Recently we reported on SCH 79797 (N3-cyclopropyl-7- inverted question mark[4-(1-methylethyl)phenyl]methyl inverted question mark-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine) and its analogs as new potent, nonpeptide thrombin receptor antagonists. This study further characterizes the biochemical and pharmacological actions of pyrroloquinazoline inhibitors of protease activated receptor-1 (PAR-1) in human platelets and coronary artery smooth muscle cells (hCASMC). SCH 79797 and its N-methyl analog (SCH 203099) inhibited binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP, Ala-Phe(p-F)-Arg-ChA-HArg-[(3)H]Tyr-NH(2)) to PAR-1 with IC(50) values of 70 and 45 nM, respectively. SCH 79797 inhibited [(3)H]haTRAP binding in a competitive manner. SCH 79797 and SCH 203099 inhibited alpha-thrombin- and haTRAP-induced aggregation of human platelets, but did not inhibit human platelet aggregation induced by the tethered ligand agonist for protease-activated receptor-4 (PAR-4), gamma-thrombin, ADP, or collagen. SCH 203099 inhibited surface expression of P-selectin induced by haTRAP and thrombin, and it did not increase P-selectin expression or prevent thrombin cleavage of the receptor. Thrombin and TFLLRNPNDK-NH(2) (TK), a PAR-1-selective agonist, produced transient increases in cytosolic free Ca(2+) concentration ([Ca(2+)](i)) in hCASMC. This increase in [Ca(2+)](i) was inhibited effectively by SCH 79797. However, the Ca(2+) transients induced by SLIGKV-NH(2,) a PAR-2-selective agonist, were not inhibited by SCH 79797. Thrombin- and TK-stimulated [(3)H]thymidine incorporation also was inhibited completely by SCH 79797. The results of this study demonstrate that SCH 79797 and SCH 203099 are potent, selective antagonists of PAR-1 in human platelets and hCASMC. These data also suggest that the thrombin stimulation of Ca(2+) transients and mitogenesis in hCASMC is mediated primarily through activation of PAR-1.
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.[Pubmed:10450984]
Bioorg Med Chem Lett. 1999 Jul 19;9(14):2073-8.
A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively.