Imidapril
Based on 1 Customer Validation
Imidapril (TA-6366 free base) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions.
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- Pureté: 99.0%
- CAS No.: 89371-37-9
- Formule: C20H27N3O6
- Masse moléculaire:405.44
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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MMP-9 |
Imidapril (1×10-9-1×10-7 μM; 2 h pre-treatment followed by 1 h LPS stimulation) inhibits the activation of the MKK4-JNK-c-Jun signaling pathway in LPS-induced human primary monocytes, with no effect on the activation of p38, ERK, or NF-κB p65[1].
Imidapril (0.1 μM; pre-treatment for 2 h followed by stimulation with LPS or poly I:C for 24 h) significantly downregulates LPS-induced TNF-α production and poly I:C-induced IP-10 production in THP-1 cells[1].
Imidapril (10-7-10-4 M) dose-dependently inhibits the gelatinase activity of recombinant MMP-9 in a cell-free in vitro system[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Imidapril (3 mg/kg/day; i.p.; continuous; 1 month) suppresses cerebral aneurysm formation and medial thinning in rats via an ACE-independent, MMP-9-dependent mechanism, reducing mean aneurysm size to 32.9 mm and increasing mean medial thickness ratio to 0.73 without altering blood pressure[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 89371-37-9
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Appearance Solid
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Masse moléculaire 405.44
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Formule C20H27N3O6
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Color White to off-white
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SMILES
O=C(N(C1=O)[C@@H](CN1C)C(O)=O)[C@H](C)N[C@H](C(OCC)=O)CCC2=CC=CC=C2
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Synonyms
TA-6366 free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : ≥ 50 mg/mL (123.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Tsai MK, et al. Suppressive effects of imidapril on Th1- and Th2-related chemokines in monocytes. J Investig Med. 2011;59(7):1141-1146. [Content Brief]
[3]. Ishibashi R, et al. Imidapril inhibits cerebral aneurysm formation in an angiotensin-converting enzyme-independent and matrix metalloproteinase-9-dependent manner. Neurosurgery. 2012;70(3):722-730. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4665 mL | 12.3323 mL | 24.6646 mL | 61.6614 mL |
| 5 mM | 0.4933 mL | 2.4665 mL | 4.9329 mL | 12.3323 mL | |
| 10 mM | 0.2466 mL | 1.2332 mL | 2.4665 mL | 6.1661 mL | |
| 15 mM | 0.1644 mL | 0.8222 mL | 1.6443 mL | 4.1108 mL | |
| 20 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0831 mL | |
| 25 mM | 0.0987 mL | 0.4933 mL | 0.9866 mL | 2.4665 mL | |
| 30 mM | 0.0822 mL | 0.4111 mL | 0.8222 mL | 2.0554 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5415 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0277 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL |
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