| Size | Price | Stock | Qty |
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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%
Benidipine HCl (formerly SC-278724, KW-3049 HCl; trade names Sular; Coniel) is the hydrochloride salt form of benidipine which is a DHP/dihydropyridine calcium channel blocker/CCB with anti-hypertensive activity. It has been approved for the treatment high blood pressure and angina pectoris. It also inhibits aldosterone-induced MCR activation. In addition, benidipine Hydrochloride has been reported to reduce oxidative stress. Benidipine is sold in the United States under the proprietary name Sular.
| ln Vitro |
Benidipine hydrochloride (0.01–1 μM, 7 days) increases phosphorylated Akt, which stimulates endothelial cell secretion [5]. In the G0/G1 and G1/S phases, benidipine hydrochloride (0.1–10 μM, 48 h) can considerably impede Western Blot analysis [5].
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| ln Vivo |
In rabbits, benidipine hydrochloride (3–10 μg/kg, intravenous administration) has strong anti-cellular effects that are unaffected by hemodynamics [2]. Hypertensive endothelial cell-type nitric oxide synthase (eNOS) activity is increased and coronary circulation is improved by benidipine hydrochloride (5 mg/kg, daily intravenous injection for 6 weeks) [3]. For one week, benidipine hydrochloride (1–10 mg/kg), taken orally, once a day, significantly reduces the risk of access reperfusion injury [4].
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| Cell Assay |
Western Blot Analysis[5]
Cell Types: mouse PBMC Tested Concentrations: 1 μM Incubation Duration: 7 days Experimental Results: Serine 473 The expression of phosphorylated Akt is increased. Cell proliferation analysis [6] Cell Types: Mesangial cells Tested Concentrations: 0.1-10 μM Incubation Duration: 48 h Experimental Results: Inhibition of cell cycle progression in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: MI/R rabbit model [2]
Doses: 3-10 μg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results:caused a significant decrease in HR (heart rate), MABP (mean arterial blood pressure) and PRI (pressure rate index) ), the concentration is 10 µg/kg. At 3 µg/kg, apoptosis-positive cells were diminished to 7.4%. Animal/Disease Models: Renovascular hypertension rat (RHR) model [3] Doses: 5 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: Reduce blood pressure and coronary vascular resistance index. Nitrite production and eNOS mRNA expression as well as resting coronary flow and capillary density were increased. Animal/Disease Models: Rat heart model [4] Doses: 1-10 mg/kg Route of Administration: Oral Experimental Results: Increased LVDP and post-ischemic recovery of 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%), 3 mg/kg. |
| References |
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| Molecular Formula |
C28H31N3O6.HCL
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|---|---|---|
| Molecular Weight |
542.02
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| Exact Mass |
541.197
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| CAS # |
91599-74-5
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| Related CAS # |
Benidipine;105979-17-7
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| PubChem CID |
656667
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
625.2±55.0 °C at 760 mmHg
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| Melting Point |
199-201ºC
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| Flash Point |
331.9±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
4.92
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
933
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=C([C@H](C(=C(N1)C)C(=O)O[C@@H]2CCCN(C2)CC3=CC=CC=C3)C4=CC(=CC=C4)[N+](=O)[O-])C(=O)OC.Cl
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| InChi Key |
KILKDKRQBYMKQX-MIPPOABVSA-N
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| InChi Code |
InChI=1S/C28H31N3O6.ClH/c1-18-24(27(32)36-3)26(21-11-7-12-22(15-21)31(34)35)25(19(2)29-18)28(33)37-23-13-8-14-30(17-23)16-20-9-5-4-6-10-20;/h4-7,9-12,15,23,26,29H,8,13-14,16-17H2,1-3H3;1H/t23-,26-;/m1./s1
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| Chemical Name |
5-O-[(3R)-1-benzylpiperidin-3-yl] 3-O-methyl (4R)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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: ≥ 2.08 mg/mL (3.84 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 (3.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8450 mL | 9.2248 mL | 18.4495 mL | |
| 5 mM | 0.3690 mL | 1.8450 mL | 3.6899 mL | |
| 10 mM | 0.1845 mL | 0.9225 mL | 1.8450 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00135551 | Completed | Drug: Angiotensin receptor blockers | Cardiovascular Disease | Seiji Umemoto, M.D., Ph.D. | May 2003 | Phase 4 |
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