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3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester

3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester structure

CAS No:
167221-71-8
Formula:
C21H23Cl2NO6
Chemical Name:
3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester
Synonyms:
3,5-Pyridinedicarboxylic acid,4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-,3-methyl 5-[(1-oxobutoxy)methyl] ester;3,5-Pyridinedicarboxylic acid,4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-,methyl (1-oxobutoxy)methyl ester;Clevidipine;rac-Clevidipine;Clevelox;H 324/38;Cleviprex;166432-28-6
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

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Description

White to Off-White SolidClevidipine is an ultra-short-acting vasodilator of the dihydropyridine (DHP) class of CCB. It is indicated as an intravenous treatment for the acute management of hypertension when oral therapy is not feasible or not desirable. Clevidipine is the second intravenous CCB to be marketed behind nicardipine for this indication. Both agents are primarily used for urgent treatment of hypertension in cardiac surgical setting, intensive care units, and emergency department

Clevidipine is a dihydropyridine.|Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option.

3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester Basic Attributes

Molecular Weight：

456.32

Exact Mass：

456.32

EC Number：

1312995-182-4

DSSTox ID：

DTXSID6057661

ATC Code：

C08CA16|C - Cardiovascular system

HScode：

29339900

Characteristics

PSA：

90.9

XLogP3：

4.3

Appearance：

Powder

Density：

1.289

Melting Point：

128-130°C

Boiling Point：

539.7±50.0 °C(Predicted)

Flash Point：

280℃

Refractive Index：

1.543

Storage Conditions：

Refrigerator

Safety Information

safety instructions：

24/25

Precautionary statement(s)：

P201, P202, P281, P308+P313, P405, P501

Hazard Statements：

H361

GHS Classification：

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Toxicity

Protein Binding：

>99.5%

Drug Information

Drug Indication：

For the reduction of blood pressure when when oral antihypertensive therapy is not feasible or not desirable.|FDA Label|Treatment of hypertensive disease

Pharmacology：

Clevidipine belongs to a well-known class of drugs called dihydropyridine calcium channel antagonists. Clevidpine is the first third generation intravenous dihydropyridine calcium channel blocker. In vitro studies demonstrated that clevidipine acts by selectively relaxing the smooth muscle cells that line small arteries, resulting in arterial dilation, widening of the artery opening, and without reducing central venous pressure or reducing cardiac output.

MeSH：

A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)

Absorption：

urine 63-74%, feces 7-22%

Metabolism/Metabolites：

Clevidipine is rapidly hydrolyzed to inactive metabolites by esterases in arterial blood.

Biological Half-Life：

1 minute

Mechanism of Action：

Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.

MeSH Entry Terms：

butyroxymethyl methyl 4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester Use and Manufacturing

Uses

A calcium channel protein inhibitor and blocker

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:456.3
XLogP3:4.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:10
Exact Mass:455.0902428
Monoisotopic Mass:455.0902428
Topological Polar Surface Area:90.9
Heavy Atom Count:30
Complexity:748
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Guide of 3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester

Description
Basic Attributes
Characteristics
Safety Information
Toxicity
Drug Information
Use and Manufacturing
Computed Properties
Recommended Suppliers
Latest News
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3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl 5-[(1-oxobutoxy)methyl] ester

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