Benidipine
Based on 2 publication(s) in Google Scholar
Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.81%
- CAS No.: 105979-17-7
- Formule: C28H31N3O6
- Masse moléculaire:505.56
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Benidipine
MoreVoir tous les produits spécifiques à Isoform Calcium Channel
More
Activité biologique
Description
In Vivo
Benidipine (5 mg/kg; i.v.; every other day for 6 weeks) increases the activity of endothelial cell-type nitric oxide synthase (eNOS) and improves coronary circulation in hypertensive rats[3].
Benidipine (1, 3, 10 mg/kg; p.o.; once daily for 1 week) significant cardioprotective effects against ischemia-reperfusion injury[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sham MI (myocardial ischaemia)/R (ischmia reperfused injury) rabbits and MI/R rabbits[2]
-
Dosage:3, 5, 10 µg/kg
-
Administration:I.v.
-
Result:Caused a significant decreased in HR ( heart rate), MABP (mean arterial blood pressure), PRI (pressure-rateindex) at 10 µg/kg, decreased apoptotic positive cells to7.4% at 3 µg/kg and not significantly different from that seen in the group treated with higher dose.
-
Animal Model:Renovascular hypertensive rats (RHR)[3]
-
Dosage:5 mg/kg (dissolved in peanut oil)
-
Administration:I.v.; every other day for 6 weeks
-
Result:Significantly decreased the blood pressure and coronary vascular resistance index, but increased nitrite production and eNOS mRNA expression and significantly increased the coronary flow at rest, the capillary density.
-
Animal Model:Rats (heart model (Langendorff perfusion))[4]
-
Dosage:1, 3, 10 mg/kg
-
Administration:P.o.; once daily for 1 week
-
Result:Significantly 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%; p<0.05) at 3 mg/kg.
Chemical Information
-
CAS No. 105979-17-7
-
Appearance Solid
-
Masse moléculaire 505.56
-
Formule C28H31N3O6
-
Color Off-white to light yellow
-
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
-
Synonyms
KW-3049 free base
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Cell Metab
Hepatocyte-to-intestinal stem cell remote communication regulates blood glucose homeostasis. [Abstract]2026 Jul 7;38(7):1367-1384.e9. PMID: 42309059 -
Solvant et solubilité
In Vitro:
DMSO : 200 mg/mL (395.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
In Vivo:
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: ≥ 5 mg/mL (9.89 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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
-
Fiche technique (278 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
-
Instruction de manipulation (2659 KB)
Références
[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]
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. 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 | 1.9780 mL | 9.8900 mL | 19.7800 mL | 49.4501 mL |
| 5 mM | 0.3956 mL | 1.9780 mL | 3.9560 mL | 9.8900 mL | |
| 10 mM | 0.1978 mL | 0.9890 mL | 1.9780 mL | 4.9450 mL | |
| 15 mM | 0.1319 mL | 0.6593 mL | 1.3187 mL | 3.2967 mL | |
| 20 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4725 mL | |
| 25 mM | 0.0791 mL | 0.3956 mL | 0.7912 mL | 1.9780 mL | |
| 30 mM | 0.0659 mL | 0.3297 mL | 0.6593 mL | 1.6483 mL | |
| 40 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2363 mL | |
| 50 mM | 0.0396 mL | 0.1978 mL | 0.3956 mL | 0.9890 mL | |
| 60 mM | 0.0330 mL | 0.1648 mL | 0.3297 mL | 0.8242 mL | |
| 80 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.6181 mL | |
| 100 mM | 0.0198 mL | 0.0989 mL | 0.1978 mL | 0.4945 mL |
Benidipine Related Classifications
HY-B1448A Related Classifications
Powered by Bioz