EXENATIDE ACETATE

PRODUCT IDENTIFICATION
CAS NO.

141732-76-5

 
EINECS NO.  
FORMULA C184H282N50O60S.C2H4O2
MOL WT. 4262.67

H.S. CODE

  

TOXICITY

 

SYNONYMS Exendin 4; Exenatide;
His-Gly-Gly-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala- Val-Arg-Leu-Phe-Ile- Glu- Trp- Leu- Lys-Asn-Gly-Gly-Pro-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2; 2-Glycine-3-L-glutamic acid- Exendin 3 (Heloderma horridum); Exendin 4 (Heloderma suspectum); L-Histidylglycyl-L-alpha-glutamylglycyl-L- threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl- L-leucyl-L-seryl-L-lysyl-L-glutaminyl- L-methionyl-L-alpha- glutamyl-L-alpha-glutamyl-L-alpha-glutamyl-L-alanyl-L-valyl- L-arginyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-alpha- glutamyl-L-tryptophyl-L-leucyl-L-lysyl-L- asparaginylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L- alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide; Other RN: 141732-76-5, 286014-72-0, 335149-21-8
SMILES

 

CLASSIFICATION

 Bioactive peptide, Antidiabetic, GLP-1 Receptor Agonist, Hypoglycemic Agent

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE white to off-white powder
MELTING POINT  
BOILING POINT

 

SPECIFIC GRAVITY

 

SOLUBILITY IN WATER Soluble (soluble in acetic acid)
pH  
VAPOR DENSITY

 

AUTOIGNITION

 

NFPA RATINGS

 Health: 2 Flammability: 0 Reactivity: 0

REFRACTIVE INDEX

 

FLASH POINT

 

STABILITY

Stable under ordinary conditions

GENERAL DESCRIPTION & APPLICATIONS

Incretin mimetics are a new class of pharmacological agents with multiple antihyperglycemic actions that mimic some effects of endogenous incretin hormones, including glucose-dependent enhancement of insulin secretion. Although these agents may exhibit glucoregulatory effects similar to those of GLP-1, their actions might not be mediated solely through the pancreatic GLP-1 receptor. Therefore, the class name "incretin mimetic" is intended to emphasize the glucoregulatory and metabolic effects of these agents, rather than their specific mechanisms of action. Several incretin mimetic GLP-1 analogues have been developed that are resistant to degradation by DPP-IV. Liraglutide (Novo Nordisk, Copenhagen, Denmark) and CJC-1131 (Conjuchem, Montreal, Canada) have undergone the most extensive testing to date of the GLP-1 analogues. Liraglutide is in phase 2 clinical trials. However, further clinical development of CJC-1131 has been put on hold in favor of CJC-1134, an exendin-4 conjugate, according to 30 September 2005 and 25 January 2006 press releases from Conjuchem and, therefore, will not be discussed further. Exenatide, which is not a GLP-1 analogue, is the first incretin mimetic approved for clinical use by the FDA. (http://www.medscape.com/)

Exenatide is the first of a new type of medication called incretin mimetics. The U.S. Food and Drug Administration (FDA) approved exenatide to treat people with type 2 diabetes who have not been able to control their blood sugar levels with oral medicines. It is given as a shot 2 times a day, before morning and evening meals. Incretin mimetics act like (mimic) the natural hormones in your body that lower blood sugar. These hormones are called incretins. Exenatide:

  • Allows your pancreas to release insulin. This drug lowers blood sugar levels only when they rise too high.
  • Prevents the pancreas from giving out glucagon. Glucagon is a hormone that causes the liver to release its stored sugar into the bloodstream.
  • Helps to slow the rate at which your stomach empties after eating. This may make you feel less hungry and more satisfied after a meal. (http://www.svcmc.org/)

Exenatide is an injectable drug that reduces the level of sugar (glucose) in the blood. It is used for treating type 2 diabetes. Exenatide belongs in a class of drugs called incretin mimetics because these drugs mimic the effects of incretins. Incretins, such as human-glucagon-like peptide-1 (GLP-1), are hormones that are produced and released into the blood by the intestine in response to food. GLP-1 increases the secretion of insulin from the pancreas, slows absorption of glucose from the gut, and reduces the action of glucagon. (Glucagon is a hormone that increases glucose production by the liver.) All three of these actions reduce levels of glucose in the blood. In addition, GLP-1 reduces appetite. Exenatide is a synthetic (man-made) hormone that resembles and acts like GLP-1. In studies, exenatide-treated patients achieved lower blood glucose levels and experienced weight loss. Exenatide was approved by the FDA in May, 2005. (http://www.medicinenet.com/)

SALES SPECIFICATION

APPEARANCE

 white to off-white powder

PURITY
98.0% min (HPLC)
AMINO ACID ±10% (theoretical Composition)
RELATED SUBSTANCE

2.0% max (total impurity)
PEPTIDE CONTENT
80.0% min (N determination)
ACETATE CONTENT

15.0% max
WATER CONTENT

6.0% max
BACTERIAL ENDOTOXINS 5EU/mg max
TRANSPORTATION
PACKING

 
HAZARD CLASS  
UN NO.  
SAFETY INFORMATION

Hazard Symbols: T, Risk Phrases: 45-60-22, Safety Phrases: 53-45