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Nicardipine hydrochloride

Product Name
Nicardipine hydrochloride
CAS No.
54527-84-3
Chemical Name
Nicardipine hydrochloride
Synonyms
YC-93;dafil;dagan;loxen;lincil;Vasonas;Dacarel;Barizin;Aprovan;NICODEL
CBNumber
CB1244267
Molecular Formula
C26H30ClN3O6
Formula Weight
515.99
MOL File
54527-84-3.mol
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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)
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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)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
N7510
Product name
Nicardipine hydrochloride
Purity
powder, ≥98%
Packaging
1g
Price
$132
Updated
2024/03/01
Sigma-Aldrich
Product number
PHR2531
Product name
Nicardipine hydrochloride
Purity
Pharmaceutical Secondary Standard; Certified Reference Material
Packaging
500MG
Price
$267
Updated
2024/03/01
Sigma-Aldrich
Product number
1463224
Product name
Nicardipine hydrochloride
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200mg
Price
$436
Updated
2024/03/01
Sigma-Aldrich
Product number
Y0001924
Product name
Nicardipine hydrochloride
Purity
European Pharmacopoeia (EP) Reference Standard
Packaging
Y0001924
Price
$148
Updated
2023/06/20
Sigma-Aldrich
Product number
Y0001917
Product name
Nicardipine for system suitability
Purity
European Pharmacopoeia (EP) Reference Standard
Packaging
Y0001917
Price
$201
Updated
2023/06/20
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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

anesthetic (topical)

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

Dihydropyridine calcium channel blocker. Antianginal; antihypertensive

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

Raw materials

Preparation Products

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Nicardipine hydrochloride Suppliers

Americas 1 Belgium 1 Canada 4 China 205 Europe 2 France 2 Germany 9 India 23 Italy 2 Japan 5 South Korea 3 Spain 2 Switzerland 4 United Kingdom 12 United States 50 USA 1 Global 326
TCI Europe
Tel
320-37350700
Fax
+32 (0)37350701
Email
sales@tcieurope.eu
Country
Europe
ProdList
23671
Advantage
75
kemikalieimport
Tel
--
Fax
--
Email
Sales@kemikalieimport.dk
Country
Europe
ProdList
6685
Advantage
47
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View Lastest Price from Nicardipine hydrochloride manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Nicardipine Hydrochloride 54527-84-3
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-10-11
Hebei Weibang Biotechnology Co., Ltd
Product
Nicardipine hydrochloride 54527-84-3
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
500000kg
Release date
2024-10-28
Hebei Yanxi Chemical Co., Ltd.
Product
Nicardipine hydrochloride 54527-84-3
Price
US $50.00-16.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20 tons
Release date
2023-09-13

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  • NICARDIPINE HYDROCHLORIDE
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  • 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-3,5-PYRIDINE-DICARBOXYLIC ACID 3-METHYL ESTER 5-[2-(METHYL-(BENZYL)AMINO)ETHYL] ESTER HYDROCHLORIDE
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  • 54527-84-3
  • 5427-84-3
  • C26H29N3O6HCl
  • C26H30ClN3O6
  • C25H28ClN3O6
  • C26H29N3O6ClH
  • Inhibitors and Activators
  • Ion Channels