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HENAN SUNLAKE ENTERPRISE CORPORATIONSale Orlistat Cas.no : 96829-58-2 C29H53NO5 pharmaceutical intermediates Synthetic intermediate//file1.lookchem.com/300w/synthetic/2022-02-15-06/b941c813-d2c1-4480-87e8-af7813078910.png
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Sale Orlistat Cas.no : 96829-58-2 C29H53NO5 pharmaceutical intermediates Synthetic intermediate CAS NO.96829-58-2

Min.Order Quantity:
10 Kilogram
Purity:
99%
Port:
Any Chinese main ports
Payment Terms:
L/C,T/T,MoneyGram,Other

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  • ProName: Sale Orlistat Cas.no : 96829-58-2 C29H...
  • CasNo: 96829-58-2
  • Molecular Formula: C29H53NO5
  • Appearance: light yellow solid
  • Application: 96829-58-2 2>pharmaceutical intermedi...
  • DeliveryTime: Within 7 working days since received y...
  • PackAge: 25kgs plastic bag 25kgs kraft bag 25kg...
  • Port: Any Chinese main ports
  • ProductionCapacity: 100 Kilogram/Month
  • Purity: 99%
  • Storage: Room temperature with sealed well
  • Transportation: BY SEA /BY AIR /BY COURIER
  • LimitNum: 10 Kilogram
  • Heavy Metal: <20PPM
  • Synonyms: Flibanserin;Bimt 17;3-[2-[4-[4-(Triflu...
  • Purity: 99.2%
  • Application: pharmaceutical raw materials

Superiority

1, rich experience in produce----we have 26 years experiences in chemical products and 6years experiences in pharmaceutical intermediate products and apis.

2, competitive price ---we have the competitive price owing to low labor cost (located in hejin,shanxi) and low material cost(we need large quantity).

3, stable supply ability ---we have a stable supply ability owing to three workshops produce plan every month and stock plan for each products ;

4, shipment timely---the shipment never delayed and we can get reorder from new customer;

5, rich experience in sales-- we have rich experience working with large international company like moriroku and fujifilm and so on;

6, strong quality control system ---we have a very strong quality control system raw material control / process control/ finished product quality inspection.

7, stronger r&d ability--- there is two teams r&d, one in factory and another in france cnrs and icoa. we supply the technology support for analyze and synthesis and do new product according to customer's requirement.

8. accept third lab test---we accept audit directly and tested . no any risk commitment for customers.

9.various payment terms---we can accept various payment terms include lc, dp and so on.

10,our service---free sample and 24 hours on-line professional service and other requirements.

96829-58-2

Details

orlistat basic information
a new type of lipid - lowering drugs pharmacological effects indications adverse reactions drug interactions dosage and usage precautions
product name: orlistat
synonyms: (s)-2-formylamino-4-methyl-pentanoic acid (s)-1-[[(2s,3s)-3-hexyl-4-oxo-2-oxetanyl]methyl]-dodecyl ester;ro-18-0647;(-)-tetrahydrolipstatin;orlistat;n-formyl-l-leucine (1s)-1-[[(2s,3s)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester;xenical;(-)-tetrahydrolipstatin(equivalenttoorlistat);orlipastat
cas: 96829-58-2
mf: c29h53no5
mw: 495.73
einecs:
product categories: pharmaceutical raw materials;miscellaneous biochemicals;api;antiobesity agent;chiral reagents;intermediates & fine chemicals;pharmaceuticals;amino acids & derivatives;heterocycles;actos;other apis;lipid-lowering medicine reducing weight
mol file: 96829-58-2.mol
orlistat structure
orlistat chemical properties
mp <50 °c
storage temp. 2-8°c
solubility dmso: 19 mg/ml
form solid
color white
cas database reference 96829-58-2(cas database reference)
safety information
wgk germany 3
rtecs oh3167600
hazardous substances data 96829-58-2(hazardous substances data)
msds information
provider language
(-)-tetrahydrolipstatin english
sigmaaldrich english
orlistat usage and synthesis
a new type of lipid - lowering drugs orlistat is currently internationally recognized as a new type of weight loss lipid-lowering drugs with the marketed product being under the name of xenical. it was first listed in new zealand in 1998 with annual sale of $ 146 million at that time. in 2007, the sale reaches $ 538 million, orlistat occupy 80% of the market share of the global weight-loss market with the annual sale of only china hong kong year reaching 80 million us dollars.
orlistat is a long-acting and potent specific inhibitor of gastrointestinal tract lipase, appearing as white or white-like powder at room temperature and being insoluble in water, soluble in chloroform and easily soluble in ethanol. it can form covalent bonds with the active serine sites of the gastric lipase and the pancreatic lipase in the stomach and small intestine cavity, resulting in inactivation of the enzymes. fat in food can’t be broken down into free fatty acids and monoacylglycerols so that the fat can’t be absorbed and utilized, thereby having reduced the body's calorie intake to control the body weight.
the drug does not need to be absorbed through the body. at normal doses, the absorption of fat can be inhibited by 30%. there is little absorption after oral administration. it can be subject to metabolic inactivation in the intestine with the metabolic sites located in the gastrointestinal wall. the elimination half-life is about 14 to 19 hours. about 97% of the goods are excreted with the feces, of which 83% are in the prototype.
clinically orlistat can be applied to the treatment of obesity and hyperlipidemia. under normal circumstances, it can be subject to oral administration at a dose of 120 mg for three times per day. take it during the meal or 1 hour after a meal. after 2 weeks of administration, the body weight can begin to decline. it can be taken continuously for 6 to 12 months. if the dose is increased to above 400 mg daily, the effect will no longer be further enhanced.
the orlistat tablets produced by the zhejiang hisun pharmaceutical co.
figure 1 the orlistat tablets produced by the zhejiang hisun pharmaceutical co.
pharmacological effects orlistat belongs to lipase inhibitor class weight-loss drugs, which is the hydration derivatives of lipstatin, being able to reduce the absorption of food fats so that the weight will get lost. this product has a potent and selective inhibitory effect on gastric lipase and pancreatic lipase with no influence on other kinds of digestive enzymes (amylase, trypsin, and chymotrypsin) and phospholipase without affecting the absorption of carbohydrates, protein and phospholipids. the drug is not absorbed by the gastrointestinal tract with its inhibition on lipase being reversible.
orlistat can form covalent bonds with the active serine sites of the gastric lipase and the pancreatic lipase in the stomach and small intestine cavity, resulting in inactivation of the enzymes, inhibiting the triglyceride hydrolysis so that the monoglyceride and free fatty acid intake will decrease, thereby controlling the body weight. the pharmacological activity of orlistat is dose-dependent with a therapeutic dose of orlistat (120 mg / day, taken at mealtime) in combination with a low-calorie balanced diet being capable of reducing 30% of fat absorption in the diet. studies on normal-weight and obese volunteers have shown that orlistat is not substantially absorbed by the body and that the concentration of the drug in the plasma is very low. after oral administration of a single dose (maximal dose of 800 mg), the plasma concentration of orlistat within 8 hours is lower than 5 ng / ml.
generally under the treatment dose, the body has a low systemic absorption of the orlistat without accumulation during short-term treatment. in vitro experiments, orlistat has an as high as over 99% binding rate to the plasma protein (lipoprotein, albumin as the major binding protein). orlistat can rarely bind to red blood cells. studies in obese patients show that orlistat, which is seldom absorbed, has two major metabolites in plasma, m1 (hydrolyzate of the 4-lactone ring) and m3 (m1 attached with a n-formyl-l lysine lysis product) account for 42% of the total plasma concentration. m1 and m3 have extremely week inhibitory effect on lipase. the unabsorbed orlistat was mainly excreted from the feces, accounting for 97% of the dose taken, 83% of which were prototype drugs, and the cumulative renal excretion amount of orlistat and its metabolites was less than 2%. it needs 3 to 5 days for thorough excretion (feces and urine) of drugs. both m1 and m3 can be excreted through bile.
this product also has an effect of regulating blood lipids: being able to reduce serum triglyceride (tg) and the low density lipoprotein cholesterol (ldl-c) and increase the proportion of high-density lipoprotein and low-density lipoprotein in the serum of obesity patients.
indications this combination of this product with mild low-calorie diet is applicable to obese and overweight patients, including for the long-term treatment of patients who have been associated with obesity-related risk factors. this product has long-term effects of weight control (weight loss, weight maintenance and prevention of rebound). administration of orlistat can reduce the incidence of obesity-related risk factors and other obesity-related diseases, including hypercholesterolemia, type 2 diabetes, impaired glucose tolerance, hyperinsulinemia, hypertension, and can also reduce the fat content in the organ.
adverse reactions there have reports of rare increase in aminotransferase, elevated alkaline phosphatase, and severe hepatitis associated with orlistat administration, together with cases of liver failure of which some patients require a liver transplant or can lead directly to death. there are also cases that orlistat leads to rare allergic reactions. the main clinical manifestations include itching, rash, urticaria, angioedema, bronchospasm and allergic reactions while the emergence of large herpes is very rare. post-marketing monitoring also noted pancreatitis reported.
drug interactions it can reduce the absorption of the vitamin a, d and e. the application of this product can be supplemented at the same time. if you are taking vitamins a, d and e preparations (such as some of the compound vitamin class preparations), we should take the goods after taking 2 hours or at bedtime.
patients with type 2 diabetes may need to reduce the dose of oral hypoglycemic agents (such as sulfonylurea drugs).
combination with cyclosporine can cause decreased plasma concentration of latter one.
combination with amiodarone may lead to reduced absorption and reduce the efficacy of the latter.
dosage and usage this combination of xenical (orlistat) with mild low-calorie diet is applicable to obese and overweight patients, including for the long-term treatment of patients who have been associated with obesity-related risk factors. this product has long-term effects of weight control (weight loss, weight maintenance and prevention of rebound). administration of orlistat can reduce the incidence of obesity-related risk factors and other obesity-related diseases, including hypercholesterolemia and type ii diabetes
adults: the recommended dose is taking a 120 mg capsule during meal or within one hour after meal. if a meal is not into the food or no fat, you can omit a medication. long-term use of treatment (including weight control and risk factors for improvement) is sustainable.
the patient's diet should be nutritionally balanced with slightly low heat. there is about 30% of heat coming from fat. the food should be rich in fruits and vegetables. the intake of fats, carbohydrates and protein should be distributed in three meals a day. there is no evidence that over three times daily /120mg per time can enhance the efficacy. no dose adjustment is required for the elderly.
precautions because of the reports regarding rare acute hepatocellular necrosis or acute liver failure after the marketing of orlistat, some of which require a liver transplant or can directly cause death, the prescribing physician should instruct the patient that if any liver symptoms and signs of dysfunction (such as loss of appetite, itching, jaundice, dark urine, fecal color, upper right quadrant pain) occur, the patients should immediately discontinued orlistat and other suspicious drugs, and test liver function.
chemical properties off-white solid
usage an antiobesity agent. a pancreatic lipase inhibitor. antiobesity agent.
usage antidiabetic
usage orlistat is an antiobesity agent. orlistat is an pancreatic lipase inhibitor.
usage tetrahydrolipstatin (orlistat) is a semi-synthetic derivative of lipstatin, a metabolite isolated from streptomyces toxytricini. tetrahydrolipstatin acts as a potent, irreversible inhibitor of pancreatic lipase. in vivo, it blocks the absorption of triglycerides while allowing fatty acid absorption. tetrahydrolipstatin is widely used for the treatment of obesity.
biological activity hypolipemic pancreatic, gastric and carboxylester lipase inhibitor. exhibits no activity at phospholipase a 2 , liver esterase, trypsin and chymotrypsin. inhibits the thioesterase domain of fatty acid synthase, leading to cell cycle arrest at the g 1 /s boundary in vitro . prevents the absorption of approximately one third of fat from food and exhibits progastrokinetic, antiobesity and antihypercholesterolemic activity in vivo

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