RWJ-56110 dihydrochloride - CAS:2387505-58-8

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RWJ-56110 dihydrochloride

目录号 : KM4579 CAS No. : 2387505-58-8

Data Sheet 产品使用指南

RWJ-56110 dihydrochloride 是一种有效的、选择性的、拟肽抑制剂，抑制 PAR-1 激活和内化 (结合 IC₅₀=0.44 uM)，对 PAR-2, PAR-3 和 PAR-4 无影响。RWJ-56110 dihydrochloride 抑制由 SFLLRN-NH2 (IC₅₀=0.16 μM) 和凝血酶 (IC₅₀=0.34 μM) 诱导的血小板聚集，相对于 U46619 具有相当的选择性。RWJ-56110 dihydrochloride 在体内阻断血管生成和新血管的形成。RWJ-56110 dihydrochloride 诱导细胞凋亡 (apoptosis)。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

RWJ-56110 dihydrochloride 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 dihydrochloride 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 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

体外研究

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 .
RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC₅₀ value of 3.5 μM. RWJ-56110 dihydrochloride 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).
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.
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.
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.
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.

Western Blot Analysis

Cell Line:	Endothelial cells
Concentration:	0 μM; 3 μM; 1 μM; 3 μM; 10 μM
Incubation Time:	Pretreatment for 15 min
Result:	Resulted in MAPK activation in Endothelial cells.

Cell Cycle Analysis

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.

分子量

863.65

CAS号

2387505-58-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : 200 mg/mL (231.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 5 mg/mL (5.79 mM); Clear solution

此⽅案可获得 ≥ 5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

以 1 mL ⼯作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μ L Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility:≥ 5 mg/mL (5.79 mM); Clear solution

此⽅案可获得 ≥ 5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

以 1 mL ⼯作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility:≥ 5 mg/mL (5.79 mM); Clear solution

此⽅案可获得 ≥ 5 mg/mL (5.79 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。

以 1 mL ⼯作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。