ChemicalBook > CAS DataBase List > Nicardipine hydrochloride
Nicardipine hydrochloride
Nicardipine hydrochloride
- CAS No.54527-84-3
- Chemical Name:Nicardipine hydrochloride
- CBNumber:CB1244267
- Molecular Formula:C26H30ClN3O6
- Formula Weight:515.99
- MOL File:54527-84-3.mol
Nicardipine hydrochloride Property
- Melting point 176-1780C
- storage temp. 2-8°C
- solubility DMSO: ~1 mg/mL
- form powder
- color yellow
- Merck 14,6495
- Stability Stable for 1 year from date of purchase as supplied. Solutions in distilled water or ethanol may be stored at -20°C for up to 1 month.
- InChIKey AIKVCUNQWYTVTO-UHFFFAOYSA-N
- CAS DataBase Reference 54527-84-3(CAS DataBase Reference)
- FDA UNII K5BC5011K3
- UNSPSC Code 41116107
- NACRES NA.77
Safety
- Hazard Codes :T
- Risk Statements :23/24/25
- Safety Statements :36/37/39-45
- RIDADR :UN 2811 6.1/PG 3
- WGK Germany :3
- RTECS :US7972100
- HazardClass :6.1(b)
- PackingGroup :III
- HS Code :2933399090
- Toxicity :LD50 in male, female rats (mg/kg): 634, 557 orally; 18.1, 25.0 i.v.; in male, female mice: 634, 650 orally; 20.7, 19.9 i.v. (Odani, Sado)
-
NFPA 704:
0 4 0
-
Symbol(GHS)
- Signal wordDanger
- Hazard statements H301+H311+H331
- Precautionary statements P280-P301+P310+P330-P302+P352+P312-P304+P340+P311
Nicardipine hydrochloride Price
More Price(5)
- Brand: Sigma-Aldrich(India)
- Product number: N7510
- Product name : Nicardipine hydrochloride
- Purity: powder, ≥98%
- Packaging: 1G
- Price: ₹12632.78
- Updated: 2022/06/14
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- Brand: Sigma-Aldrich(India)
- Product number: PHR2531
- Product name : Nicardipine hydrochloride
- Purity: Pharmaceutical Secondary Standard; Certified Reference Material
- Packaging: 500MG
- Price: ₹22764.98
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: N7510
- Product name : Nicardipine hydrochloride
- Purity: powder, ≥98%
- Packaging: 5G
- Price: ₹49513.55
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: N7510
- Product name : Nicardipine hydrochloride
- Purity: powder, ≥98%
- Packaging: 10G
- Price: ₹79834.38
- Updated: 2022/06/14
- Buy: Buy
- Brand: TCI Chemicals (India)
- Product number: N0635
- Product name : Nicardipine Hydrochloride
- Purity:
- Packaging: 5G
- Price: ₹8900
- Updated: 2022/05/26
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Nicardipine hydrochloride Chemical Properties,Usage,Production
- Description Nicardipine is a dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity. It is reported to inhibit adenosine A1, A2A, and A3 receptors with Ki values of 19.6, 63.8, and 3.25 μM, respectively, and can inhibit cytochrome P450 3A4 catalytic activity with an IC50 value of 0.148 μM. Additionally, nicardipine has been shown to activate transient receptor potential A1 channels, producing an increase in Ca2+ (EC50 = 0.5 μM).
- Chemical Properties Yellow Solid
- Uses Dihydropyridine calcium channel blocker. Antianginal; antihypertensive
- Uses Nicardipine is a dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity. It is reported to inhibit adenosine A1, A2A, and A3 receptors with Ki values of 19.6, 63.8, and 3.25 μM, respectively, and can inhibit cytochrome P450 3A4 catalytic activity with an IC50 value of 0.148 μM. Additionally, nicardipine has been shown to activate transient receptor potential A1 channels, producing an increase in Ca2+ (EC50 = 0.5 μM).
- Uses anesthetic (topical)
- Definition ChEBI: Nicardipine hydrochloride is a dihydropyridine. It has a role as a geroprotector.
- brand name Cardene(PDL Biopharma); Cardene (Roche).
- General Description Nicardipine hydrochloride,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylicacid methyl 2-[methyl(phenylmethyl)amino]ethylester hydrochloride (Cardene), is a more potent vasodilator ofthe systemic, coronary, cerebral, and renal vasculature andhas been used in the treatment of mild, moderate, and severehypertension. The drug is also used in the management of stableangina.
- Biochem/physiol Actions Blocks L-type voltage-dependent calcium channels; antihypertensive.
-
Clinical Use
Calcium-channel blocker:
Prophylaxis and treatment of angina
Mild to moderate hypertension
Acute life-threatening hypertension and post operative hypertension (IV) - Safety Profile Poison by ingestion, intravenous, and intraperitoneal routes. Moderately toxic by subcutaneous route. Human systemic effects: decreased urine volume or anuria. Experimental reproductive effects. When heated to decomposition it emits toxic fumes of NOx an
-
Drug interactions
Potentially hazardous interactions with other drugs
Aminophylline: possibly increases aminophylline concentration.
Anaesthetics: enhanced hypotensive effect.
Antibacterials: metabolism possibly accelerated by rifampicin; metabolism possibly inhibited by clarithromycin, erythromycin and telithromycin.
Antidepressants: enhanced hypotensive effect with MAOIs.
Antiepileptics: effect reduced by carbamazepine, barbiturates, phenytoin and primidone.
Antifungals: metabolism possibly inhibited by itraconazole and ketoconazole; negative inotropic effect possibly increased with itraconazole.
Antihypertensives: enhanced hypotensive effect, increased risk of first dose hypotensive effect of post synaptic alpha-blockers.
Antivirals: concentration possibly increased by ritonavir; use telaprevir with caution.
Cardiac glycosides: digoxin concentration increased.
Ciclosporin: concentration of ciclosporin increased
Grapefruit juice: concentration increased - avoid.
Tacrolimus: may increase tacrolimus levels.
Theophylline: possibly increased theophylline concentration. - Metabolism Nicardipine is subject to saturable first-pass metabolism. It is extensively metabolised in the liver and excreted in the urine and faeces, mainly as inactive metabolites.
- References 1) Merck 14 6495 2) Hulubei et al. (2012), 4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter; Bioorg. Med. Chem., 20 6620
Nicardipine hydrochloride Preparation Products And Raw materials
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