Benidipine hydrochloride
Based on 1 publication(s) in Google Scholar
Benidipine hydrochloride is an orally active calcium channel antagonist. Benidipine hydrochloride can inhibit cell proliferation and apoptosis. Benidipine hydrochloride has antioxidant activity and can increase nitric oxide synthase activity and improve coronary circulation in hypertensive rats.
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- Purity: 99.80%
- CAS No.: 91599-74-5
- 화학식: C28H32ClN3O6
- 분자량:542.02
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Benidipine hydrochloride
MoreAll Calcium Channel Isoforms
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Biological Activity
Benidipine hydrochloride (0.01-1 μM, 7 days) promotes mouse endothelial cell differentiation by enhancing phosphorylated Akt[5].
Benidipine hydrochloride (0.1-10 μM) inhibits the proliferation of mesangial cells, at both the G0/G1 and G1/S phases[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine PBMCs
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Concentration:1 μM
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Incubation Time:7 days
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Result:Increased the expression of phosphorylated Akt on serine-473.
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Cell Line:Mesangial cells
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Concentration:0.1-10 μM
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Incubation Time:48 h
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Result:Inhibited the progression of the cell cycle in a dose-dependent manner.
Benidipine hydrochloride (5 mg/kg, i.v., every day for 6 weeks) increases the activity of endothelial cell-type nitric oxide synthase (eNOS) and improves coronary circulation in hypertensive rats[3].
Benidipine hydrochloride (1-10 mg/kg, p.o., once daily for 1 week) has significant cardioprotective effects against ischemia-reperfusion injury[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MI/R rabbits model[2]
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Dosage:3-10 μg/kg
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Administration:i.v.
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Result:Caused a significant decrease in HR ( heart rate), MABP (mean arterial blood pressure), and PRI (pressure-rate index) at 10 µg/kg. Decreased apoptotic positive cells to 7.4% at 3 µg/kg.
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Animal Model:Renovascular hypertensive rats (RHR) model[3]
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Dosage:5 mg/kg
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Administration:i.v.
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Result:Decreased the blood pressure and coronary vascular resistance index. Increased nitrite production and eNOS mRNA expression and the coronary flow at rest, the capillary density.
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Animal Model:Rat heart model[4]
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Dosage:1-10 mg/kg
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Administration:p.o.
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Result:Increased the post-ischemic recovery of LVDP and LV dP/dt max (LVDP: 87.5±10.1 vs 64.6±11.9%; LV dP/dt max: 97.8±10.4 vs 70.2±15.7%) at 3 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 91599-74-5
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Appearance Solid
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분자량 542.02
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화학식 C28H32ClN3O6
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C)NC(C)=C(C(O[C@H]2CN(CC3=CC=CC=C3)CCC2)=O)[C@@H]1C4=CC=CC([N+]([O-])=O)=C4)OC.[H]Cl
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Synonyms
KW-3049
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Metab
Hepatocyte-to-intestinal stem cell remote communication regulates blood glucose homeostasis. [Abstract]2026 Jul 7;38(7):1367-1384.e9. PMID: 42309059
용액&용해도
DMSO : 33.33 mg/mL (61.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (3.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.84 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Yao K, et al. Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker. J Pharmacol Sci. 2006 Apr;100(4):243-61. [Content Brief]
[2]. Gao F, et al. Anti-apoptotic effect of benidipine, a long-lasting vasodilating calcium antagonist, in ischaemic/reperfused myocardial cells. Br J Pharmacol. 2001 Feb;132(4):869-78. [Content Brief]
[3]. Kobayashi N, et al. Benidipine stimulates nitric oxide synthase and improves coronary circulation in hypertensive rats. Am J Hypertens. 1999 May;12(5):483-91. [Content Brief]
[4]. Masanori S, et al. Orally administered benidipine and manidipine prevent ischemia-reperfusion injury in the rat heart. Circ J. 2004 Mar;68(3):241-6. [Content Brief]
[5]. Ando H, et al. Benidipine, a dihydropyridine-Ca2+ channel blocker, increases the endothelial differentiation of endothelial progenitor cells in vitro. Hypertens Res. 2006 Dec;29(12):1047-54. [Content Brief]
[6]. Ono T, et al. Broad antiproliferative effects of benidipine on cultured human mesangial cells in cell cycle phases. Am J Nephrol. 2002 Sep-Dec;22(5-6):581-6. [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 (sealed storage, away from moisture). 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 | 1.8450 mL | 9.2248 mL | 18.4495 mL | 46.1238 mL |
| 5 mM | 0.3690 mL | 1.8450 mL | 3.6899 mL | 9.2248 mL | |
| 10 mM | 0.1845 mL | 0.9225 mL | 1.8450 mL | 4.6124 mL | |
| 15 mM | 0.1230 mL | 0.6150 mL | 1.2300 mL | 3.0749 mL | |
| 20 mM | 0.0922 mL | 0.4612 mL | 0.9225 mL | 2.3062 mL | |
| 25 mM | 0.0738 mL | 0.3690 mL | 0.7380 mL | 1.8450 mL | |
| 30 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5375 mL | |
| 40 mM | 0.0461 mL | 0.2306 mL | 0.4612 mL | 1.1531 mL | |
| 50 mM | 0.0369 mL | 0.1845 mL | 0.3690 mL | 0.9225 mL | |
| 60 mM | 0.0307 mL | 0.1537 mL | 0.3075 mL | 0.7687 mL |
Benidipine hydrochloride Related Classifications
HY-B1448 Related Classifications
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