| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
|
||
| 1mg |
|
||
| 5mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
| 体外研究 (In Vitro) |
Apabetalone (RVX-208) 与乙酰化组蛋白肽与四种 BET 蛋白的串联 BD1 BD2 蛋白结构的结合竞争，表现出 0.5 至 1.8 µM 之间的 IC50。 Apabetalone 在体外促进肝细胞中 ApoA-I 的形成，从而导致高密度脂蛋白胆固醇 (HDL-C) 增加。 Apabetalone 主要与 BET（溴结构域和额外末端）家族的溴结构域结合，竞争与内源配体乙酰化赖氨酸结合的位置，这解释了其药理作用。通过表观遗传机制增加载脂蛋白 AI (ApoA-I) 的合成，表明 BET 抑制可能是治疗动脉粥样硬化的一种有前途的新方法。 Apabetalone 促进肝细胞中 ApoA-I 的表达[2]。
|
||
|---|---|---|---|
| 体内研究 (In Vivo) |
在动脉粥样硬化预防性治疗的研究设计中，小鼠接受西方饮食以及 150 毫克/公斤/剂量 bid 的药物治疗，持续 12 周。治疗一年后，处死小鼠。媒介物处理组和Apabetalone (RVX-208)处理组均显示出体重逐渐增加。采用西方饮食 12 周后，Apabetalone 治疗组的体重增加了 4 克（从 24 克增至 28 克），而载体治疗组则增加了 9 克（从 25 克增至 34 克）。在用 Apabetalone 治疗的小鼠中观察到的体重增加显着减少并不是由于采食量减少，这表明该化合物具有有利的特性。在用媒介物或apibetalone治疗六周和十二周后，进行血浆脂质测量。治疗六周后，与载体对照动物相比，用 apibetalone 治疗的小鼠的 HDL-C 水平显着升高（约 200%）。这种增加一直持续到为期 12 周的研究得出结论[3]。
|
||
| 动物实验 |
|
||
| 参考文献 |
[1]. Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9.
[2]. McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. [3]. Jahagirdar R, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236(1):91-100 |
| 分子式 |
C20H22N2O5
|
|
|---|---|---|
| 分子量 |
370.4
|
|
| CAS号 |
1044870-39-4
|
|
| 相关CAS号 |
|
|
| SMILES |
O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3
|
|
| InChi Key |
NETXMUIMUZJUTB-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)
|
|
| 化学名 |
2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
|
|
| 别名 |
RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.
|
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外) |
|
|||
|---|---|---|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 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 (6.75 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. Solubility in Formulation 6: ≥ 0.5 mg/mL (1.35 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 7: 0.5% CMC Na (1N HCl, PH 2.5-3.0):8 mg/mL Solubility in Formulation 8: 15.15 mg/mL (40.90 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6998 mL | 13.4989 mL | 26.9978 mL | |
| 5 mM | 0.5400 mL | 2.6998 mL | 5.3996 mL | |
| 10 mM | 0.2700 mL | 1.3499 mL | 2.6998 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03655704 | Completed | Drug: Apabetalone | Pulmonary Arterial Hypertension | Steeve Provencher | August 22, 2019 | Early Phase 1 |
| NCT04915300 | Not yet recruiting | Drug: Apabetalone Drug: Placebo |
Pulmonary Arterial Hypertension | Laval University | October 2023 | Phase 2 |
| NCT04894266 | Terminated | Drug: Apabetalone Other: Standard of care |
COVID-19 Infection | Resverlogix Corp | January 14, 2022 | Phase 2 Phase 3 |
| NCT03160430 | Not yet recruiting | Drug: apabetalone Drug: Placebos |
Kidney Failure, Chronic | Resverlogix Corp | November 22, 2024 | Phase 1 Phase 2 |
|
 |
Nrf2 activator-2
7-O-Methylaloesinol
BRD7-IN-2
I-BET432
InvivoChem的所有产品仅用于作科学研究，不面向患者销售
Copyright 2020 InvivoChem LLC | All Rights Reserved 粤ICP备20063088号-1
COA
粤公网安备 44011102003439号