CANDESARTAN CILEXETIL

PRODUCT IDENTIFICATION

CAS NO. 139481-59-7 (Base)
145040-37-5 (cilexetil)

CANDESARTAN CILEXETIL

EINECS NO.  
FORMULA C33H34N6O6
MOL WT. 610.67

H.S. CODE

 

TOXICITY

 
SYNONYMS Blopress; Atacand;
(±)-2-Ethoxy-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1H-benzimidazole-7- carboxylic acid 1-(((cyclohexyloxy)carbonyl)oxy)ethyl ester; 7-Carboxy-1-(2-((cyclohexylcarbonyl)oxy)ethyl) -2-ethoxy-1-(2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)-1H- benzimidazolium hydroxide, inner salt; (±)-1-Hydroxyethyl 2-ethoxy-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-7-benzimidazolecarboxylate cyclohexyl carbonate; Amias; Ratacand;
DERIVATION

 

CLASSIFICATION

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE White to off-white crystalline powder
MELTING POINT 157 - 160 C
BOILING POINT  
SPECIFIC GRAVITY  
SOLUBILITY IN WATER Practically insoluble (soluble in methanol)
pH  
VAPOR DENSITY

 

AUTOIGNITION

 

NFPA RATINGS

 

REFRACTIVE INDEX

 
FLASH POINT

 

STABILITY Stable under ordinary conditions.

GENERAL DESCRIPTION & APPLICATIONS

Angiotensin is a polypeptide vasopressor hormone formed by the catalytic action of renin which is released mainly by the kidneys in response to low blood volume or low sodium content in the body. The juxtaglomerular cells release renin, when juxtaglomerular apparatus decreases in the kidneys. Renin (called angiotensinogenase, EC 3.4.23.15) is an enzyme of the hydrolase class that catalyzes cleavage of the leucine-leucine bond in angiotensinogen (a serum globulin) to generate angiotensin I (decapeptide hormone) in the liver. Among angiotensin I's various biological activity, it acts mainly as a precursor to angiotensin II (octapeptide hormone) which is a vasopressor and stimulator of aldosterone secretion by the adrenal cortex, and functions also as a neurotransmitter. A. II is formed by catalytic action of the hydrolase called peptidyl-dipeptidase A (EC 3.4.15.1) on C-terminal oligopeptide (A.I). In case of the cleavage of A. I to the activated A.II, it is called angiotensin-converting enzyme (ACE); in case of the cleavage and inactivation of kinins, it is called kininase II (also called dipeptidyl carboxypeptidase I). Angiotensin III (heptapeptide) is a  degradation product of A. II, having less vasopressor activity than the parent compound. The renin-angiotensin system plays an important role in the regulation of blood volume and blood pressure, stimulates antidiuretic hormone and aldosterone production, and the hypothalamus to activate the thirst reflex, but is crucial in the pathogenesis of hypertension patients due to blood vessels constrict, retention of fluid and raising blood pressure. ACE inhibitors prevent A.I from converting into A.II. and act to widen the blood vessels and make it easier for the heart to pump blood through the body. If high blood pressure continues for a long time, it  may damage the blood vessels of the brain, heart, and kidneys, resulting in heart attack, heart failure, or kidney failure. ACE inhibitors are used in ther treatment of hypertension, congestive heart failure, and to alleviate strain on hearts damaged as a result of a heart attack. They prevent from cardiovascular disorders, left ventricular dysfunction, and nephropathy in diabetes mellitus. They also helps control the amount of blood in your body. Angiotensin receptor blockers (ARBs) reduce hypertension by displacing A.II 2 from receptors on the surface of cells. There are  A.I receptor as well as A.II receptor. They are used when patients are intolerant of ACE inhibitor therapy. They have fewer side effects.

Angiotensin-Converting enzyme Inhibitors

  • Benazepril (CAS #: 86541-75-5)
  • Captopril (CAS #: 62571-86-2)
  • Enalapril (CAS #: 75847-73-3)
  • Fosinopril (CAS #: 98048-97-6)
  • Imidapril (CAS #: 89371-37-9)
  • Lisinopril (CAS #: 83915-83-7)
  • Moexipril (CAS #: 103775-10-6)
  • Quinapril (CAS #: 85441-61-8)
  • Perindopril (CAS #: 82834-16-0)
  • Ramipril (CAS #: 87333-19-5)
  • Trandolapril (CAS #: 87679-37-6)

Angiotension II Receptor Blockers

  • Candesartan (CAS #: 145040-37-5)
  • Eprosartan (CAS #: 133040-01-4)
  • Irbesartan (CAS #: 138402-11-6)
  • Losartan (CAS #: 114798-26-4)
  • Olmesartan (CAS #: 144689-24-7)
  • Telmisartan (CAS #: 144701-48-4)
  • Valsartan (CAS #: 137862-53-4)

Candesartan is a nonpeptide angiotensin II blocker used as an antihypertensive. Commercially cilexeti (cyclohexyl 1-hydroxyethyl carbonate) ester form is available. Candesartan cilexetil is the producg which is separated into the active candesartan and ester by reacting with a molecule of water. Candesartan cilexetil a white crystalline powder; melting point 157 - 160 C; insoluble in water, soluble in methanol; administered orally. Chemical designation is (±)-2-Ethoxy-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)- 4-yl)methyl)-1H-benzimidazole-7-carboxylic acid 1- (((cyclohexyloxy)carbonyl)oxy)ethyl ester. Candesartan is also used in a combination with thiazide diuretic (hydrochlorothiazide) to improve antihypertensive effect. Candesartan is marketed as the cyclohexyl 1-hydroxyethyl carbonate (cilexetil) ester,

SALES SPECIFICATION

APPEARANCE

White crystalline powder

IDENTIFICATION

Complies

ASSAY (HPLC)

99.0% min
MELTING POINT 157 - 160 C

LOSS ON DRYING

0.5% max

HEAVY METALS

10ppm max

SULFATED ASH 0.1% max
TRANSPORTATION
PACKING

10kgs in tin can

HAZARD CLASS  
UN NO.  
PRICE INFORMATION

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