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SCH-79797

Alias: SCH-79797 SCH 79797 SCH79797
Cat No.:V14527 Purity: ≥98%
SCH-79797 (SCH79797) is a novel, potent and selective PAR1 (protease activated receptor 1)antagonist with anIC50of 70 nM and aKiof 35 nM.
SCH-79797
SCH-79797 Chemical Structure CAS No.: 245520-69-8
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
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Other Forms of SCH-79797:

  • SCH79797 diHCl
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SCH-79797 (SCH79797) is a novel, potent and selective PAR1 (protease activated receptor 1) antagonist with an IC50 of 70 nM and a Ki of 35 nM. SCH-79797 limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH 79797 protects against ischemia/reperfusion-induced arrhythmias in the rat hearts. SCH 79797 and its N-methyl analogue (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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
SCH79797 competitively prevents the high-affinity binding of the thrombin receptor activating peptide ([3H]haTRAP). Alpha-thrombin and haTRAP-induced human platelet aggregation is inhibited by SCH79797, but not that of tethering ligand agonists of protease-activated receptor 4 (PAR-4), gamma-thrombin, ADP, or collagen. In hCASMCs, thrombin produces a brief rise in the concentration of cytosolic free Ca2+ ([Ca2+]i). The rise in [Ca2+]i is effectively inhibited by SCH79797. TK-stimulated [3H]thymidine incorporation is totally inhibited by SCH79797 [1] and thrombin. In a concentration-dependent way, SCH79797 impedes the development of several human and animal cell lines. For NIH 3T3, HEK 293, and A375 cells, the corresponding ED50 values for growth inhibition were 75 nM, 81 nM, and 116 nM. At low doses, SCH79797 suppresses serum-stimulated p44/p42 mitogen-activated protein kinase (MAPK) activation in NIH 3T3 cells, but at higher concentrations, it promotes apoptosis [2].
ln Vivo
In two models of myocardial ischemia/reperfusion (I/R) injury, intact rats' myocardial necrosis following cardiac I/R was decreased by SCH79797 (2.5-250 μg/kg; i.v.; male Sprague Dawley rats) when administered before to or during ischemia. The best dose for the dose-dependent response is 25 μg/kg [4].
Animal Protocol
Animal/Disease Models: Male Sprague Dawley rats (8 weeks old) with myocardial I/R injury [4]
Doses: 2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg and 250 μg/kg
Route of Administration: IV
Experimental Results: Myocardial necrosis after I/R was diminished in intact rat hearts before or during ischemia.
References

[1]. 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. 2000 Nov 15;60(10):1425-34.

[2]. Protease-activated receptor 1-selective antagonist SCH79797 inhibits cell proliferation and induces apoptosis by a protease-activated receptor 1-independent mechanism. Basic Clin Pharmacol Toxicol. 2007 Jul;101(1):63-9.

[3]. A novel therapeutic target in various lung diseases: airway proteases and protease-activated receptors. Pharmacol Ther. 2007 Jul;115(1):70-83.

[4]. SCH 79797, a selective PAR1 antagonist, limits myocardial ischemia/reperfusion injury in rat hearts. Basic Res Cardiol. 2007 Jul;102(4):350-8.

Additional Infomation
N3-cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamine is a member of quinazolines.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H25N5
Molecular Weight
371.488
Exact Mass
443.164
CAS #
245520-69-8
Related CAS #
SCH79797 dihydrochloride;1216720-69-2
PubChem CID
4259181
Appearance
Light yellow to brown solid powder
Boiling Point
678.3ºC at 760mmHg
Flash Point
364ºC
Vapour Pressure
1.23E-18mmHg at 25°C
LogP
7.17
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
5
Heavy Atom Count
28
Complexity
527
Defined Atom Stereocenter Count
0
InChi Key
AVXQPEKZIGPIJW-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H25N5/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)
Chemical Name
N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine
Synonyms
SCH-79797 SCH 79797 SCH79797
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~134.60 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6919 mL 13.4593 mL 26.9186 mL
5 mM 0.5384 mL 2.6919 mL 5.3837 mL
10 mM 0.2692 mL 1.3459 mL 2.6919 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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