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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Ramipril (HOE-498; Altace; Carasel; Ramace; Zabien; Tritace; Ramace; Triatec; Tritace; Vesdil) is a potent angiotensin-converting enzyme (ACE) inhibitor with anti-hypertensive effects. It inhibits ACE with an IC50 of 5 nM and has been approved for hypertension treatment. Ramipril is a produg that has to be activated by hydrolysis to the active metabolite Ramiprilat. Studies indicate that Ramipril is a more potent inhibitor in comparison to Zofenopril (sc-208496). Acute coronary syndrome investigations demonstrate that Ramipril increases IL-10, and decreases the levels of MCP-1 and IL-18.
| ln Vitro |
Angiotensin-converting enzyme (ACE) inhibitor ramipril (HOE-498) has an IC50 of 5 nM[1]. However, in endothelial cells expressing an S1270A ACE mutant or in ACE-deficient cells, ramipril (HOE-498) is unable to activate JNK or boost the nuclear accumulation of c-Jun. Instead, it increases the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells. Long-term Ramipril use raises ACE expression in mouse lung in vivo and primary cultures of human endothelial cells, a phenomenon that can be avoided by pretreating with the JNK inhibitor SP600125[2].
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| ln Vivo |
In contrast to the apoptosis effect in vitro, chronic in vivo administration of Ramipril (HOE-498) to rats at a dosage that has similar hypotensive effects in vitro HUVECs considerably lowers the rate of LPS-induced apoptosis relative to the other ACE inhibitors[3 [4].
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| References |
[1]. Raasch, W., et al., Combined blockade of AT1-receptors and ACE synergistically potentiates antihypertensive effects in SHR. J Hypertens, 2004. 22(3): p. 611-8.
[2]. Stevens, B.R., M.I. Phillips, and A. Fernandez, Ramipril inhibition of rabbit (Oryctolagus cuniculus) small intestinal brush border membrane angiotensin converting enzyme. Comp Biochem Physiol C, 1988. 91(2): p. 493-7. [3]. Kohlstedt, K., et al., Angiotensin-converting enzyme is involved in outside-in signaling in endothelial cells. Circ Res, 2004. 94(1): p. 60-7. [4]. Ceconi, C., et al., Differences in the effect of angiotensin-converting enzyme inhibitors on the rate of endothelial cell apoptosis: in vitro and in vivo studies. Cardiovasc Drugs Ther, 2007. 21(6): p. 423-9. |
| Molecular Formula |
C23H32N2O5
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| Molecular Weight |
416.51
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| CAS # |
87333-19-5
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| Related CAS # |
Ramipril-d5;1132661-86-9;Ramipril-d3;2673269-81-1
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| SMILES |
O=C([C@@H]1C[C@@](CCC2)([H])[C@@]2([H])N1C([C@@H](N[C@H](C(OCC)=O)CCC3=CC=CC=C3)C)=O)O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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: ≥ 3.25 mg/mL (7.80 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 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 3.25 mg/mL (7.80 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 32.5 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: ≥ 3.25 mg/mL (7.80 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: 30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL Solubility in Formulation 5: 20 mg/mL (48.02 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 | 2.4009 mL | 12.0045 mL | 24.0090 mL | |
| 5 mM | 0.4802 mL | 2.4009 mL | 4.8018 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4009 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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