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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%
Manidipine (formerly CV-4093; CV 4093; CV4093), a calcium channel blocker (CCB) of the dihydropyridine class, is an approved drug that has been used clinically as an antihypertensive agent. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cell. Manidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists.
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The median Tmax is 1.5 h. Administration with food produces an 1.3-1.6-fold increase in Cmax but no change in Tmax. Manidipine does not accumulate significantly with multiple doses. Manidipine is eliminated through extensive metabolism. 63% is eliminated in the feces and 31% in the urine as metabolites. Metabolism / Metabolites Manidipine is extensively metabolized by CYP enzymes to pyridine derivatives and diphenylmethane derivatives which make up 4-7% and 22-24% of the dose excreted in the urine. Biological Half-Life The half life of elimination has been observed to be dose dependent. Doses of 5, 10, and 20 mg produced half lives of 3.94, 5.02, and 7.95 h respectively. |
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| Toxicity/Toxicokinetics |
Protein Binding
Manidipine is 99% bound to human plasma proteins. |
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| References |
Proc Natl Acad Sci U S A.1992;89(9):4071-5;Cancer Res.1992;52(5):1369-71.
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| Additional Infomation |
Manidipine is a diarylmethane.
Manidipine (INN) is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. It is selective for vasculature and does not produce effects on the heart at clinically relevant dosages. Drug Indication For the treatment of hypertension. Mechanism of Action Contraction of vascular smooth muscle is stimulated by Gq coupled receptors which produce calcium release from the sarcoplasmic reticulum. This is followed by opening of voltage dependent calcium channels and an influx of calcium into the cell ultimately producing contraction. Manidipine binds to and dissociates slowly from L- and T-type voltage dependent calcium channels on smooth muscle cells, blocking the entrance of extracellular calcium into the cell and preventing this contraction. This produces vasodilation which decreases blood pressure. Manidipine produces renal vasodilation and an increase in natriuresis. This likely contributes to the antihypertensive effect by reducing blood volume. Manidipine is selective for the vasculature and does not produce significant effects on the heart or central nervous system at clinically relevant dosages. Pharmacodynamics Manidipine produces vasodilation resulting in lower blood pressure. |
| Molecular Formula |
C35H38N4O6
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| Molecular Weight |
610.7
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| Exact Mass |
610.279
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| CAS # |
89226-50-6
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| Related CAS # |
Manidipine dihydrochloride;89226-75-5;Manidipine-d4;1189656-59-4
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| PubChem CID |
4008
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
722.0±60.0 °C at 760 mmHg
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| Melting Point |
125-128ºC
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| Flash Point |
390.4±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.601
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| LogP |
5.46
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
45
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C(C2C=C([N+](=O)[O-])C=CC=2)C(C(OCCN2CCN(C(C3C=CC=CC=3)C3C=CC=CC=3)CC2)=O)=C(C)NC=1C)OC
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| InChi Key |
JINNGBXKBDUGQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H38N4O6.2ClH/c1-24-30(34(40)44-3)32(28-15-10-16-29(23-28)39(42)43)31(25(2)36-24)35(41)45-22-21-37-17-19-38(20-18-37)33(26-11-6-4-7-12-26)27-13-8-5-9-14-27;;/h4-16,23,32-33,36H,17-22H2,1-3H3;2*1H
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| Chemical Name |
3-(2-(4-benzhydrylpiperazin-1-yl)ethyl) 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate dihydrochloride
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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 |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 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 |
| NCT03106597 | Terminated | Drug: Manidipine 20mg Drug: Amlodipine 10mg |
Hypertension | Korea University Guro Hospital | August 20, 2015 | Phase 4 |
| NCT00627952 | Completed | Drug: amlodipine 10 mg Drug: manidipine 20 mg |
Hypertension | University of Erlangen-Nürnberg Medical School |
November 2007 | Phase 3 |
| NCT00157586 | Completed | Drug: Delapril, Delapril-Manidipine Fixed combination |
Type 2 Diabetes | Mario Negri Institute for Pharmacological Research |
February 2002 | Phase 3 |
| NCT00741585 | Completed | Drug: Any antihypertensive medication alone or in combination |
Essential Hypertension | University of Vigo | September 1, 2008 | Phase 4 |
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