Nateglinide Manufacturer For Hypoglycemic Drugs CAS NO.105816-04-4

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nateglinide basic information
physical and chemical properties hypoglycemic agents uses
product name: nateglinide
synonyms: (-)-n-(trans-4-isopropylcyclohexanecarbonyl)-d-phenylalanine;ay4166;nateglinide(h);trans-d-phenylalanin;trans-n-((4-(1-methylethyl)cyclohexyl)carbonyl)-d-phenylalanine;3-phenyl-2-(4-propan-2-ylcyclohexyl)carbonylamino-propanoic acid;a-4166;starlix
cas: 105816-04-4
mf: c19h27no3
mw: 317.42
einecs:
product categories: active pharmaceutical ingredients;api;apis;health & beauty;amino acids & derivatives;intermediates & fine chemicals;pharmaceuticals;aromatics;starlix;antidiabetic
mol file: 105816-04-4.mol
nateglinide structure
nateglinide chemical properties
melting point 137-141°c
alpha d20 -9.4° (c = 1 in methanol)
storage temp. room temp
solubility dmso: >5mg/ml
color white to off-white
merck 14,6428
cas database reference 105816-04-4(cas database reference)
safety information
hazard codes xn
risk statements 22
safety statements 24/25-36
rtecs sq7318950
msds information
provider language
nateglinide english
nateglinide usage and synthesis
physical and chemical properties white or almost white crystalline powder, odorless, bitter taste. it is soluble in methanol, ethanol, chloroform, dissolved in acetone, ethyl ether, almost insoluble in water. valid form used in clinic is h-type, mp 137~141 ℃. [α] d-37.5 °, the maximum uv absorption wavelength in methanol is 252,257,263nm.
the above information is edited by the chemicalbook of tian ye.
hypoglycemic agents nateglinide and mitiglinide, repaglinide are three commonly used non-sulfonylurea oral hypoglycemic agents for insulin secretion,it is successfully developed for the first time by the japanese company ajomoto , its chemical structure belongs to carbamoylmethyl-benzoic acid (cmba), it belongs to d-phenylalanine derivatives, it is a new generation of antidiabetic drugs having amino acid structure ,it is an amino acid derivative prompting insulin secretion, it is also currently the only non-sulfonylureas insulinotropic agent having amino acid structure. the mechanism is mainly through binding the pancreatic β cell sulfonylurea receptor, blocking islet cell atp-sensitive potassium channels, leading to membrane depolarization, causing the calcium channe lopen to promote insulin secretion. this product is a new type of meal blood glucose regulator, which can effectively control the postprandial blood glucose levels, with rapid onset, short duration of action, low incidence of cardiovascular side effects and hypoglycemia and other characteristics.
oral bioavailability is 72%, after 15min it can produce insulin secretion effect, tmax is 0.5~0.9 h, 0.2 h insulin levels achieve peak ,after 1.5 h it is similar to placebo. the plasma protein binding rate is 99%. after reaching plasmapeak , plasma concentrations decline rapidly.t1/2 of oral administration of 120 mg and intravenous injection 60 mg of is 1.5 to 1.7 hours, and the plasma clearance is 7.4 hours. it is metabolized in the liver by isoenzyme cyp2c9 and cyp3a4 way. the main metabolites are products after isomeric oxidation,it can be hydroxyl, diastereomers, isopropyl isomer or unsaturated aliphatic isomers.the main metabolites in plasma and urine are metabolites after the hydroxylation of isopropyl methine family (me-thine carbon) . about 2/3 nateglinide is excreted from the fecal , and the rest is excreted in the urine. such excretion way is beneficial to elderly ⅱ diabetes mellitus with renal dysfunction. nateglinide eliminate t1/2 is 1.4 h, because nateglinide t1/2 is short, there is no report yet about the drug accumulation in the body . long-term use of nateglinide does not produce drug-induced hypoglycemia caused by drug accumulation .it is used for the treatment of diet therapy, exercise therapy and mild to moderate non-insulin dependent (ⅱ type) diabetes which taking α-glucosidase inhibitor can not control. the results show that: nateglinide can be used more physiologically for meal glucose control, there is less opportunity for contact with insulin and hypoglycemia which allows patients to flexibly plan scheduling mealtimes, which means there is medication while eating, not eating no medication.
uses it is used for the treatment of diabetes
chemical properties cyrstalline solid
uses antidiabetic katp channel blocker
uses an amino-acid derivative that stimulates insulin secretion. used as an antidiabetic
definition chebi: an n-acyl-d-phenylalanine resulting from the formal condensation of the amino group of d-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. an orally-ad inistered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.