| 规格 | 价格 | 库存 | 数量 |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 靶点 |
Etofibrate targets peroxisome proliferator-activated receptor α (PPARα) [1]
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| 体外研究 (In Vitro) |
依托贝特治疗可提高大鼠肝脏中细胞质甘油-3-磷酸脱氢酶活性和总肉碱浓度，同时降低三酰甘油和胆固醇浓度。依托贝特可降低大鼠肝微粒体中胆固醇、三酰甘油、游离脂肪酸 (FFA) 和甘油的血浆水平，以及总胆固醇和未酯化胆固醇的浓度。 Etofibrate 增加大鼠肝细胞质甘油-3-P 脱氢酶的活性，而降低微粒体 HMG-CoA 还原酶和胆固醇 7 α-羟化酶的活性，并且不影响酰基辅酶 A：胆固醇酰基转移酶 (ACAT)。依托贝特通过影响脂肪组织中脂解产物的释放及其内在肝脏代谢来降低肝脏中脂解产物的利用率。当喂养大鼠的附睾脂肪垫片在基础条件下进行孵育时，依托贝特会刺激脂肪酸再酯化的速率。
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| 体内研究 (In Vivo) |
烟酸和氯贝酸的乙二醇 1,2 二酯称为依托贝特。在人类和动物中，依托贝特已被证明是一种高效的降血脂药物。经过 10 天的依托贝特治疗后，大鼠的体重与对照组相当，但其肝脏重量显着增加，而三酰甘油和血浆胆固醇水平却下降。当肠肝循环中断时，给予依托贝特会导致动物的胆汁流量增加。这种效果在前两个小时内最为明显，在 30 分钟和 90 分钟后，与对照组的差异具有统计显着性。依托贝特治疗组和对照组的大鼠在累积胆汁分泌量与时间的关系中表现出高度显着的线性相关性，依托贝特组的斜率远高于对照组[1]。
在正常血脂 Wistar 大鼠（200–250 g）中，腹腔注射 Etofibrate（100 mg/kg 和 200 mg/kg）显著增加胆汁生成。给药后 2 小时，胆汁流速较溶媒对照组分别提高约 22%（100 mg/kg）和 35%（200 mg/kg）。该效应持续长达 4 小时，4 小时时胆汁流速仍较对照组分别高出约 18%（100 mg/kg）和 28%（200 mg/kg）[1] - Etofibrate（200 mg/kg，腹腔注射）改变胆汁成分：给药后 2 小时，胆汁中胆固醇含量降低约 30%，总胆汁酸浓度增加约 25%，磷脂水平与溶媒对照组相比无显著变化 [1] |
| 动物实验 |
Male Sprague Dawley rats weighing 200 to 220 g, fed ad libitum a standard laboratory diet and subjected to a 12 hr on-off light cycle and 22 to 24°C are used. Food is removed from the cages at the onset of the light cycle (7.00 a.m.) and 3 hr later, Etofibrate is administered by stomach tube without anesthesia at a dose of 300 mg/kg body weight/day to one group of animals whereas another, control, group is treated with the medium. After treatments, rats are again allowed free access to food. On the 10th day, the animals are treated as above, but 2 hr after receiving the Etofibrate or the medium the rats are anesthetized with an intraperitoneal injection (0.30 mL/100 g body weight). Animals are maintained at 37°C in a thermostatically controlled cabinet
Male Sprague Dawley rats Normolipidemic rat bile production assay: Male Wistar rats (200–250 g) were fasted for 12 hours but allowed free access to water. Rats were anesthetized with an appropriate anesthetic, and the common bile duct was cannulated with a polyethylene tube to collect bile. After a 30-minute stabilization period (basal bile collection), Etofibrate was dissolved in a suitable solvent (e.g., dimethyl sulfoxide diluted with saline) and administered intraperitoneally at doses of 100 mg/kg or 200 mg/kg. Vehicle control rats received the same volume of solvent. Bile was collected at 1-hour intervals for 4 hours, and bile volume was measured gravimetrically. Bile samples were analyzed for cholesterol, total bile acids, and phospholipid concentrations using standard biochemical assays [1] |
| 毒性/毒理 (Toxicokinetics/TK) |
In vivo toxicity: Intraperitoneal administration of Etofibrate (100–200 mg/kg) in normolipidemic rats did not cause obvious toxic symptoms (e.g., lethargy, respiratory distress, abnormal behavior) during the 4-hour observation period. No significant changes in body weight or gross organ appearance were observed at the end of the experiment [1]
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| 参考文献 |
[1]. Bocos C, et al. Effect of etofibrate on bile production in the normolipidemic rat. Gen Pharmacol. 1995 May;26(3):537-42
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| 其他信息 |
Etofibrate is a monocarboxylic acid.
Etofibrate is a fibrate produced by the combination of clofibrate ester linked to niacin. These components separate in the body slowly allowing for pharmacokinetics similar to controlled-release formulations. Etofibrate is an orally-available combination of clofibrate and niacin linked together by an ester bond. In the body clofibrate and niacin separate, acting as a controlled-release formulation. Etofibrate is a fibrate class hypolipidemic agent that acts primarily through activation of PPARα [1] - Its effect on bile production in normolipidemic rats suggests a role in modulating hepatobiliary lipid metabolism, potentially via increased bile acid synthesis and secretion, and reduced biliary cholesterol excretion [1] - The dose-dependent increase in bile flow indicates that Etofibrate enhances hepatocellular bile secretion, which may contribute to its cholesterol-lowering effect by promoting fecal cholesterol excretion via bile [1] |
| 分子式 |
C18H18CLNO5
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|---|---|---|
| 分子量 |
363.79
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| 精确质量 |
363.087
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| CAS号 |
31637-97-5
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| 相关CAS号 |
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| PubChem CID |
65777
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| 外观&性状 |
White to off-white solid powder
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| 密度 |
1.3±0.1 g/cm3
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| 沸点 |
486.8±35.0 °C at 760 mmHg
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| 熔点 |
42-44ºC
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| 闪点 |
248.2±25.9 °C
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| 蒸汽压 |
0.0±1.2 mmHg at 25°C
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| 折射率 |
1.555
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| LogP |
3.15
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| tPSA |
74.72
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| 氢键供体(HBD)数目 |
0
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| 氢键受体(HBA)数目 |
6
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| 可旋转键数目(RBC) |
9
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| 重原子数目 |
25
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| 分子复杂度/Complexity |
449
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| 定义原子立体中心数目 |
0
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| SMILES |
O=C(C1=CC=CN=C1)OCCOC(C(C)(OC2=CC=C(Cl)C=C2)C)=O
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| InChi Key |
XXRVYAFBUDSLJX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18ClNO5/c1-18(2,25-15-7-5-14(19)6-8-15)17(22)24-11-10-23-16(21)13-4-3-9-20-12-13/h3-9,12H,10-11H2,1-2H3
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| 化学名 |
2-[2-(4-Chlorophenoxy)-2-methylpropanoyl]oxyethyl pyridine-3-carboxylate
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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)
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| 溶解度 (体外实验) |
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| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (6.87 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。 *生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (6.87 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。 *20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (6.87 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 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 | 2.7488 mL | 13.7442 mL | 27.4884 mL | |
| 5 mM | 0.5498 mL | 2.7488 mL | 5.4977 mL | |
| 10 mM | 0.2749 mL | 1.3744 mL | 2.7488 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) 。
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