| 规格 | 价格 | 库存 | 数量 |
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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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| 体外研究 (In Vitro) |
盐酸莫西普利对血小板功能影响很小，且无抗炎作用[2]。莫西普利拉是盐酸莫西普利的水解产物，其 IC50 分别为 2.6 和 4.9 nM，可抑制兔肺和豚鼠血清中的 ACE[2]。盐酸莫昔普利 (0.01 nM-0.1 mM) 的 IC50 分别为 2.7 mM 和 0.165 mM，对血浆 ACE 和兔肺分离的 ACE 具有强大的功效[3]。盐酸莫昔普利（0-100 μM，24 小时）以剂量依赖性方式显着降低受损神经元的百分比[4]。盐酸莫昔普利（0-100 μM，24 小时）可显着降低 Fe2+/3+ 引起的神经毒性[4]。凋亡神经元的比例不受盐酸莫昔普利剂量的显着影响[4]。
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| 体内研究 (In Vivo) |
盐酸莫昔普利不能穿过血脑屏障[1]。盐酸莫昔普利（分别为 3 mg/kg、30 mg/kg 和 10 mg/kg；口服；每日一次；5 天）对肾性高血压大鼠、自发性高血压大鼠和肾周高血压犬的影响呈剂量依赖性，并且抗高血压[3]。在 NMRI 小鼠中，盐酸莫昔普利（0.3 mg/kg，腹腔注射）可显着减少小鼠大脑表面的梗塞面积[4]。在 Long-Evans 大鼠中，盐酸莫昔普利（0.1 mg/kg，腹腔注射）可显着减少皮质梗塞体积[4]。
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| 动物实验 |
Animal/Disease Models: Spontaneously hypertensive rats[3]
Doses: 30 mg/kg Route of Administration: po (oral gavage); one time/day; 5 days Experimental Results: Caused a progressive lowering of mean blood pressure from pretreatment values of 180 +/- 7 mmHg to a trough on day 4 of 127 +/- 4 mmHg. Dose-dependently diminished arterial blood pressure, and inhibited plasma and tissue ACE activity. Animal/Disease Models: Renal hypertensive rats[3] Doses: 0.03-10 mg/kg Route of Administration: po (oral gavage); one time/day; 5 days Experimental Results: Caused a dose-dependent decrease in blood pressure with a threshold dose of 0.3 mg/kg. Lowered mean blood pressure by about 70 mmHg of 3 mg/kg. Animal/Disease Models: Perinephritic hypertensive dogs[3] Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day; 5 days Experimental Results: Caused a drop of mean blood pressure by 25 mmHg from pre-treatment control , which persisted for 24 h, by a rapid onset and a long duration of action. Animal/Disease Models: NMRI mice (male, Permanent focal ischemia)[4] Doses: 0, 0.03, 0.3, and 3 mg/kg Administration |
| 参考文献 |
[1]. Chrysant, S.G. and G.S. Chrysant, Pharmacological and clinical profile of moexipril: a concise review. J Clin Pharmacol, 2004. 44(8): p. 827-36.
[2]. Friehe H, et al. Pharmacological and toxicological studies of the new angiotensin converting enzyme inhibitor moexipril hydrochloride. Arzneimittelforschung. 1997 Feb. 47(2):132-44. [3]. Edling, O., et al., Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril. J Pharmacol Exp Ther, 1995. 275(2): p. 854-63. [4]. Ravati A, et al. Enalapril and moexipril protect from free radical-induced neuronal damage in vitro and reduce ischemic brain injury in mice and rats. Eur J Pharmacol. 1999 May 28;373(1):21-33. |
| 分子式 |
C₂₇H₃₅CLN₂O₇
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|---|---|
| 分子量 |
535.03
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| CAS号 |
82586-52-5
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| 相关CAS号 |
Moexipril;103775-10-6;Moexipril-d5;1356929-49-1;Moexipril-d5 hydrochloride
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| SMILES |
O=C(C1N(C([C@@H](N[C@H](C(OCC)=O)CCC2=CC=CC=C2)C)=O)CC3=C(C=C(OC)C(OC)=C3)C1)O.[H]Cl
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| InChi Key |
JXRAXHBVZQZSIC-QGCARJLFSA-N
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| InChi Code |
InChI=1S/C27H34N2O7.ClH/c1-5-36-27(33)21(12-11-18-9-7-6-8-10-18)28-17(2)25(30)29-16-20-15-24(35-4)23(34-3)14-19(20)13-22(29)26(31)32;/h6-10,14-15,17,21-22,28H,5,11-13,16H2,1-4H3,(H,31,32);1H/t17-,21-,22?;/m0./s1
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| 化学名 |
2-(((S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)-L-alanyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid hydrochloride
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| 别名 |
SPM-925; SPM 925; SPM925; CI-925; CI 925; CI925;RS 10085; RS-10085; RS10085; Moexipril.
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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 |
| 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) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.89 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 20.8 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: ≥ 2.08 mg/mL (3.89 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 20.8 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: ≥ 2.08 mg/mL (3.89 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: 50 mg/mL (93.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 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 | 1.8691 mL | 9.3453 mL | 18.6905 mL | |
| 5 mM | 0.3738 mL | 1.8691 mL | 3.7381 mL | |
| 10 mM | 0.1869 mL | 0.9345 mL | 1.8691 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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