| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
IC50: 0.44 uM (PAR-1) IC50: 0.16 μM (the aggregation of human platelets induced by SFLLRN-NH2) IC50: 0.34 μM (the aggregation of human platelets induced by thrombin)[1][2]
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| ln Vitro |
The N-terminal extracellular domain of the proteinase-activated receptors (PARs) family of G protein-coupled receptors is cleaved by proteases, revealing a novel amino terminus sequence that acts as a tethered ligand to activate the receptors. When it comes to collagen and the thromboxane mimetic U46619 (HY-108566), RWJ56110 is very selective, but it also inhibits the aggregation of human platelets caused by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM).[1]. At an IC50 value of 3.5 μM, RWJ-56110 dihydrochloride completely suppresses the proliferation of RASMCs caused by thrombin. When RWJ-56110 dihydrochloride is used in conjunction with RASMC calcium mobilization (IC50=0.12 μM), HMVEC (IC50=0.13 μM), and HASMC calcium mobilization (IC50=0.17 μM), thrombin's action is blocked[1]. RWJ56110 (0.1–10 μM; 24-96 hours) has a dose-dependent inhibitory effect on endothelial cell proliferation, with a half-maximum inhibitory concentration of roughly 10 μM[2]. In a test for thymidine incorporation, RWJ56110 (0.1–10 μM; 6 hours) prevents endothelial cells from synthesizing DNA. While RWJ56110 decreases cell DNA synthesis in a dose-dependent way in endothelial cells in a fast-growing state (50–60% confluence), the inhibitory effect of PAR-1 antagonists is significantly less prominent in quiescent (100% confluent) cells[2]. Erk1/2 activation mediated by thrombin is inhibited in a concentration-dependent manner by RWJ56110 (0.1-10 μM; pretreatment for 15 min). Nevertheless, FBS (final concentration of 4%), when used to stimulate endothelial cells, partially lowers the activated levels of Erk1/2[2]. The advancement of the endothelial cell cycle is inhibited by RWJ56110 (30 μM; 24 hours). It decreases the proportion of cells in the S phase, but has less of an impact on the proportions of G1 and G2/M cells[2]
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Endothelial cells Tested Concentrations: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Duration: Pretreatment for 15 min Experimental Results: Resulted in MAPK activation in Endothelial cells. Cell Cycle Analysis[2] Cell Types: Endothelial cells Tested Concentrations: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Duration: Pretreatment for 15 min Experimental Results: decreased cell number in S phase. |
| References |
[1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62.
[2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54. |
| Molecular Formula |
C41H45CL4F2N7O3
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|---|---|
| Molecular Weight |
863.65
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| CAS # |
2387505-58-8
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| Related CAS # |
RWJ-56110;252889-88-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C(C1C(=CC=CC=1Cl)Cl)N1C=C(CN2CCCC2)C2=CC=C(NC(=O)N[C@H](C(=O)N[C@@H](CCN)C(=O)NCC3C=CC=CC=3)CC3C=CC(F)=C(F)C=3)C=C12.Cl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 200 mg/mL (231.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (5.79 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 50.0 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: ≥ 5 mg/mL (5.79 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 50.0 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1579 mL | 5.7894 mL | 11.5788 mL | |
| 5 mM | 0.2316 mL | 1.1579 mL | 2.3158 mL | |
| 10 mM | 0.1158 mL | 0.5789 mL | 1.1579 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.
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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