252889-88-6
252889-88-6 structure
- Name: RWJ-56110
- Chemical Name: N-[(2S)-4-Amino-1-(benzylamino)-1-oxo-2-butanyl]-Nα-{[1-(2,6-dichlorobenzyl)-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]carbamoyl}-3,4-difluoro-L-phenylalaninamide dihydrochloride
- CAS Number: 252889-88-6
- Molecular Formula: C41H43Cl2F2N7O3
- Molecular Weight: 863.650
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-07-01 01:50:31
- Modify Date: 2024-01-07 13:58:59
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RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2].
| Name | N-[(2S)-4-Amino-1-(benzylamino)-1-oxo-2-butanyl]-Nα-{[1-(2,6-dichlorobenzyl)-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]carbamoyl}-3,4-difluoro-L-phenylalaninamide dihydrochloride |
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| Synonyms |
Benzenepropanamide, N-[(1S)-3-amino-1-[[(phenylmethyl)amino]carbonyl]propyl]-α-[[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]amino]carbonyl]amino]-3,4-difluoro-, (α S)-, hydrochloride (1:2)
N-[(2S)-4-Amino-1-(benzylamino)-1-oxo-2-butanyl]-Nα-{[1-(2,6-dichlorobenzyl)-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]carbamoyl}-3,4-difluoro-L-phenylalaninamide dihydrochloride |
| Description | RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2]. |
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| Related Catalog | |
| In Vitro | Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors. RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 (HY-108566)[1]. RWJ-56110 is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 shows blockade of thrombin’s action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1]. RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2]. RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2]. RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1/2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1/2[2]. RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2/M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Time: Pretreatment for 15 min Result: Resuted in MAPK activation in Endothelial cells. Cell Cycle Analysis[2] Cell Line: Endothelial cells Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Time: Pretreatment for 15 min Result: Reduced cell number in S phase. |
| References |
| Molecular Formula | C41H43Cl2F2N7O3 |
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| Molecular Weight | 863.650 |
| Exact Mass | 861.230591 |