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Submit ReviewRWJ 56110 is a selective protease-activated receptor-1 (PAR1) antagonist; displays no activity at PAR2, PAR3, or PAR4 subtypes. Blocks thrombin-induced platelet aggregation and activation of MAPK in HUVECs. Also inhibits angiogenesis in a chick embryo angiogenesis model in vivo.
分子量 | 863.65 |
公式 | C41H43Cl2F2N7O3.2HCl |
储存 | Store at -20°C |
纯度 | ≥96% (HPLC) |
CAS Number | 2387505-58-8 |
PubChem ID | 90488773 |
InChI Key | MGZSVSHDIOPSBO-ZEUUMAKDSA-N |
Smiles | ClC1=CC=CC(Cl)=C1CN3C2=CC(NC(N[C@@H](CC5=CC(F)=C(F)C=C5)C(N[C@@H](CCN)C(NCC6=CC=CC=C6)=O)=O)=O)=CC=C2C(CN4CCCC4)=C3.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 21.59 | 25 | |
DMSO | 86.36 | 100 |
以下数据基于产品分子量 863.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.16 mL | 5.79 mL | 11.58 mL |
5 mM | 0.23 mL | 1.16 mL | 2.32 mL |
10 mM | 0.12 mL | 0.58 mL | 1.16 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
参考文献是支持产品生物活性的出版物。
Maryanoff et al (2003) Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1). Curr.Med.Chem.Cardiovasc.Hematol.Agents 1 13 PMID: 15317288
Zania et al (2006) 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. 318 246 PMID: 16595737
Andrade-Gordon et al (1999) Design, synthesis and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc.Natl.Acad.Sci.USA 96 12257 PMID: 10535908
If you know of a relevant reference for RWJ 56110, please let us know.
关键词: RWJ 56110, RWJ 56110 supplier, selective, PAR1, antagonists, PAR, receptors, protease-activated, proteinase-activated, RWJ56110, 252889-88-6, Protease-Activated, Receptors, 2614, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RWJ 56110 的部分引用包括:
Eum et al (2014) Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases. Am J Physiol Gastrointest Liver Physiol 306 G992 PMID: 24742991
Juncker-Jensen et al (2013) Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res 73 4196 PMID: 23687338
Shi et al (2019) Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons. JCI Insight 5 PMID: 31310593
Wang (2017) Complement-activation fragment C4a mediates effector functions by binding as untethered agonist to protease-activated receptors 1 and 4. Proc Natl Acad Sci U S A 114 10948 PMID: 28973891
Xu et al (2015) Heat stress-induced disruption of endothelial barrier function is via PAR1 signaling and suppressed by Xuebijing injection. PLoS One 10 e0118057 PMID: 25693178
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