| Size | Price | Stock | Qty |
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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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Purity: ≥98%
Moexipril HCl (RS-10085) is a potent and orally bioactive nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure. As a potent ACE inhibitor, Moexipril hydrochloride blocks the conversion of angiotensin I to angiotensin II. Moexipril in addition, has cardioprotective effects mediated through a combination of angiotensin II inhibition and bradykinin proliferation. The proliferation of bradykinin stimulates the production of prostaglandin E2 and nitric oxide.
| ln Vitro |
Moexipril hydrochloride has little effect on platelet function and no anti-inflammatory qualities[2]. With IC50s of 2.6 and 4.9 nM, respectively, moexiprilat, which is the product of moexipril hydrochloride's hydrolysis, inhibits ACE in both rabbit lung and guinea pig serum[2]. With IC50s of 2.7 mM and 0.165 mM, respectively, moexipril hydrochloride (0.01 nM-0.1 mM) demonstrates strong efficacy against both plasma ACE and isolated ACE from rabbit lung[3]. In a dose-dependent way, moexipril hydrochloride (0-100 μM, 24 h) dramatically decreased the percentage of injured neurons[4]. The neurotoxicity caused by Fe2+/3+ is considerably reduced by moexipril hydrochloride (0-100 μM, 24 h)[4]. The fraction of apoptotic neurons is not significantly affected by moexipril hydrochloride dosage[4].
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| ln Vivo |
The blood-brain barrier cannot be crossed by moexipril hydrochloride[1]. The effects of moexipril hydrochloride (3 mg/kg, 30 mg/kg, and 10 mg/kg, respectively; po; once daily; 5 days) on renal hypertensive rats, spontaneously hypertensive rats, and perinephritic hypertensive dogs are dose-dependent and antihypertensive[3]. In NMRI mice, the infarct area on the mouse brain surface is dramatically reduced by moexipril hydrochloride (0.3 mg/kg, ip)[4]. In Long-Evans rats, moexipril hydrochloride (0.1 mg/kg, ip) dramatically reduces the cortical infarct volume[4].
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| Animal Protocol |
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 |
| References |
[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. |
| Molecular Formula |
C₂₇H₃₅CLN₂O₇
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|---|---|
| Molecular Weight |
535.03
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| CAS # |
82586-52-5
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| Related CAS # |
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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| Chemical Name |
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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| Synonyms |
SPM-925; SPM 925; SPM925; CI-925; CI 925; CI925;RS 10085; RS-10085; RS10085; Moexipril.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
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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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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