Cilnidipine CAS 132203-70-4
Introduction：Basic information about Cilnidipine CAS 132203-70-4, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Cilnidipine Basic informationDescription References
| Product Name: | Cilnidipine |
| Synonyms: | ATELEC;(+/-)-(e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate;O3-(2-Methoxyethyl) O5-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;Frc 8653,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic Acid 2-Methoxyethyl (2E)-3-Phenyl-2-propenyl Ester2-Methoxyethyl (2E)-3-Phenyl-2-propenyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate;ilnidipine |
| CAS: | 132203-70-4 |
| MF: | C27H28N2O7 |
| MW: | 492.52 |
| EINECS: | 634-350-6 |
| Product Categories: | Dihydropyridine Class Chemicals;Intermediates & Fine Chemicals;Pharmaceuticals;Calcium channel;API;FRC 8653;Dihydropyridine;APIs;Active Pharmaceutical Ingredients;132203-70-4 |
| Mol File: | 132203-70-4.mol |
Cilnidipine Chemical Properties
| Melting point | 97-99°C |
| Boiling point | 652.6±55.0 °C(Predicted) |
| density | 1.240±0.06 g/cm3(Predicted) |
| storage temp. | Keep in dark place,Sealed in dry,Room Temperature |
| solubility | H2O: ≤2mg/mL |
| pka | 2.61±0.70(Predicted) |
| form | powder |
| color | light yellow |
| Water Solubility | H2O: ≤2mg/mL DMSO: ≥20mg/mL |
| Merck | 14,2275 |
| InChI | 1S/C27H28N2O7/c1-18-23(26(30)35-14-8-11-20-9-5-4-6-10-20)25(21-12-7-13-22(17-21)29(32)33)24(19(2)28-18)27(31)36-16-15-34-3/h4-13,17,25,28H,14-16H2,1-3H3/b11-8+ |
| InChIKey | KJEBULYHNRNJTE-DHZHZOJOSA-N |
| SMILES | C1(C)NC(C)=C(C(OC/C=C/C2=CC=CC=C2)=O)C(C2=CC=CC([N+]([O-])=O)=C2)C=1C(OCCOC)=O |
| CAS DataBase Reference | 132203-70-4(CAS DataBase Reference) |
Safety Information
| Hazard Codes | Xi |
| Risk Statements | 41 |
| Safety Statements | 26-39 |
| WGK Germany | 3 |
| RTECS | US7975550 |
| HS Code | 29333990 |
| Storage Class | 11 - Combustible Solids |
| Hazard Classifications | Eye Dam. 1 |
| Toxicity | LD50 in male, female mice, rats (mg/kg): 5000, 5000, 5000, 4412 orally; 5000 all species s.c.; 1845, 2353, 441, 426 i.p. (Wada) |
| Description | Clinidipine is a kind of calcium channel blocker. It is a kind of novel calcium antagonist with the blocking effect on both L-type and N-type calcium channels. It is mainly used for the treatment of hypertension. Based on its effect on both N-type and L-type calcium channel, it can dilate both arterioles and venules, further reducing the pressure in the capillary bed. In addition, cilinidipine can attenuate the platelet activation associated with catecholamines. |
| References | https://www.drugbank.ca/drugs/DB09232 https://en.wikipedia.org/wiki/Cilnidipine |
| Description | Cilnidipine is a dihydropyridine calcium channel blocker that blocks L- and N-type high-voltage-activated calcium currents in rat hippocampal CA1 pyramidal neurons when used at a concentration of 10 μM. Cilnidipine (3 mg/kg) reduces the pressor response to acute cold stress, as well as mean blood pressure, in spontaneously hypertensive rats. It dose-dependently reduces mean blood pressure and cerebral vascular resistance without affecting cerebral blood flow in anesthetized rats at doses ranging from 3-100 μg/kg. Cilnidipine (100 μg/kg, i.p.) reduces cerebral infarction area in a rat model of focal brain ischemia. |
| Description | Cilnidipine is a dihydropyridine calcium antagonist introduced for thetreatment of essential and severe hypertension and hypertension associated withrenopathy. Cilnidipine has been demonstrated to exert a potent vasodilating effect by blocking calcium influx via dihydropyridine-sensitive, voltage-dependent calciumchannels. Compared to nifedipine and nicardipine, cilnidipine is superior, especially forlong-term treatment, due to its characteristics of slow onset and long duration with lesscardiodepressant activity. Cilnidipine is reportedly well tolerated with low toxicity.It may also be useful in ischemic heart disease. |
| Chemical Properties | Yellow Crystalline Solid |
| Originator | Fujirebio (Japan) |
| Uses | A dihydropyridine calcium channel blocker. |
| Uses | antihypertensive;dihydropyridine calcium channel blocker |
| Uses | Cilnidipine has been used:
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| Definition | ChEBI: A diesterified 1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium channel blocker, it is used as an antihypertensive. |
| Brand name | Cinalong;Siscard;Atelec |
| Biological Activity | Dual L- and N-type calcium channel blocker that displays antihypertensive, sympatholytic and neuroprotective activity. Lowers mean blood pressure and reduces the size of cerebral infarction in the rat model of focal brain ischemia. |
| Biochem/physiol Actions | Cilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC. |
| storage | +4°C |
| References | [1] YOSHINAKA MURAI . Preferential inhibition of L- and N-type calcium channels in the rat hippocampal neurons by cilnidipine[J]. Brain Research, 2000, 854 1: Pages 6-10. DOI: 10.1016/s0006-8993(99)02295-7 [2] MASAHIRO HOSONO . Inhibitory Effect of Cilnidipine on Pressor Response to Acute Cold Stress in Spontaneously Hypertensive Rats[J]. Japanese journal of pharmacology, 1995, 69 2: Pages 119-125. DOI: 10.1254/jjp.69.119 [3] AKIRA TAKAHARA. Neuroprotective effects of a dual L/N-type Ca(2+) channel blocker cilnidipine in the rat focal brain ischemia model.[J]. Biological & pharmaceutical bulletin, 2004, 27 9: 1388-1391. DOI: 10.1248/bpb.27.1388 |
Cilnidipine Preparation Products And Raw materials
| Raw materials | Methyl 3-aminocrotonate-->2-Methoxyethyl 2-[(3-nitrophenyl)methylene]acetoacetate |
