阿拉地平

Description

Aranidipine · CAS 86780-90-7 · C19H20N2O7. UNII 4Y7UR6X2PO. Melting Point: 149-150ºC.

Identification

CAS Registry Number	86780-90-7
PubChem CID	2225
Molecular formula	C19H20N2O7
IUPAC name	3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
UNII (FDA)	4Y7UR6X2PO

Computed Descriptors

Molecular Weight	388.4
XLogP3	2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	7
Exact Mass	388.12705098
Monoisotopic Mass	388.12705098
Topological Polar Surface Area	128
Heavy Atom Count	28
Formal Charge	0

Physical & Chemical Properties

Melting Point	149-150ºC

Physical description & handling notes

• Insoluble

Documented Uses

• Aranidipine has been used for many years to treat angina pectoris and hypertension.
• After administration, aranidipine is rapidly absorbed from the gastrointestinal tract. After absorption, the AUC and Cmax increased linearly in a dose-dependent manner, the Cmax was attained in approximate 3.8-4.8 hours for aranidipine and 4.8-6 hours for the metabolite M-1. The bioavailability of aranidipine in rat, dog, and monkey was about 48%, 41% and 3% respectively.
• Unchanged aranidipine is found in plasma but not in the urine after 1 hour of administration. Just a small amount of drug was found in the bile. These results indicate that the excretion profile of aranidipine is mainly driven by metabolism and not by excretion. When including the metabolites, 52-56% of the original dose is disposed in the urine, 34-45% in feces and 3-4% in expired air. The excretion in the bile was 59% of the administered dose and 63% of this portion is reabsorbed.
• The binding ratio of plasma proteins of aranidipine varies from 84-95%. This ratio of the drug is similar to the unchanged form and for the M-1 metabolite. Most of the binding happens towards serum albumin and a lower amount corresponds to the alpha1-acid glycoprotein.
• Eight metabolites of aranidipine were found after oral administration. These metabolites were brought by a reduction of the ketone group, oxidation of dihydropyridine ring and de-esterification at the C-3 position.
• The elimination half-life of aranidipine and the M-1 metabolite are 1.1-1.2 hour and 2.7-3.5 hour respectively.

Synonyms

aranidipine; 86780-90-7; Sapresta; Mpc-1304; MPC1304; DTXSID9048649; Aranidipino; 4Y7UR6X2PO; 3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; 3-METHYL 5-(2-OXOPROPYL) 2,6-DIMETHYL-4-(2-NITROPHENYL)-1,4-DIHYDROPYRIDINE-3,5-DICARBOXYLATE; DTXCID6028575; aranidipinum; RefChem:559905; methyl 2-oxopropyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid; Aranidipine [INN]; (+-)-Acetonyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate

Frequently Asked Questions

What are the CAS number and molecular formula of Aranidipine?

CAS 86780-90-7; molecular formula C19H20N2O7; molecular weight — g/mol.

What other names is Aranidipine known by?

aranidipine, 86780-90-7, Sapresta, Mpc-1304, MPC1304, DTXSID9048649.

What are the key physical properties of Aranidipine?

Melting Point: 149-150ºC.

Facts on this page are taken from PubChem (US National Library of Medicine) and Wikidata. Grade-specific data — assay, moisture, particle size, packaging, shelf life — is issued per batch on the COA and is not published here.