China Professional Factory Supply 99% White Solid Orlistat CAS No.:96829-58-2

Essential information

Molecular formula: C22H30CaFN3O6S

Molecular weight: 523.63

Physical property

Melting point: 122°C

Storage condition: 2-8°C

Specific rotation：D24 +14.8° (c = 1.012 in 50% methanol)

Optical activity: [α]/D +12 to +18°, c = 1 in methanol: water (1:1)

λmax: 243nm(Phosphate buffer sol.)(lit.)

Solubility: DMSO: 25 mg/mL (49.94 mM; Ultrasound required)H2O: 1 mg/mL (2.00 mM; Requires ultrasound)

EINECS: 627-028-1

Chemical property

white crystalline powder, almost insoluble in water, easily soluble in chloroform, easily soluble in methanol and ethanol, easy to pyrolysis, melting point of 40℃ ~ 42℃. The molecule is a diastereoisomer with four chiral centers. At the wavelength of 529nm, the ethanol solution has negative optical activity.

Mechanism of action

Orlistat is a long-acting, potent and specific gastrointestinal lipase inhibitor, which inactivates the above two enzymes by forming covalent bonds with lipase active serine sites in the stomach and small intestine. The inactivated enzymes cannot break down fat in food into free fat Chemicalbook acid and glycerol that can be absorbed by the body, thus reducing fat intake. Play a role in weight loss. In addition, it has been found that orlistat inhibits intestinal absorption of cholesterol by inhibiting niemann-pickC1-like1 (NPC1L1).

Pharmacological action  

Orlistat belongs to the lipase inhibitor class of weight loss drugs, it is a hydrated derivative of lipstatin, can reduce the absorption of food fat, resulting in weight loss. This product has a strong and selective inhibition of gastric lipase and pancreatic lipase, and has no effect on other digestive enzymes (amylase, trypsin, chymotrypsin) and phospholipase, and does not affect the absorption of carbohydrates, proteins and phospholipids. The drug is not absorbed by the gastrointestinal tract, and the inhibition of lipase is reversible. Orlistat inactivates the enzyme mainly in the gastrointestinal tract by covalently binding with serine residues at the active site of gastric lipase and pancreatic lipase, inhibits the hydrolysis of triacylglycerol, and reduces the intake of monoglycerol and free fatty acids, thereby controlling body weight. The pharmacological activity of orlistat is dose-dependent, and a therapeutic dose of orlistat (120mg/d, tid, taken with meals) combined with a slightly low-calorie balanced diet can reduce dietary fat absorption by 30%. Studies in normal weight and obese volunteers have shown that orlistat is basically not absorbed by the body, the plasma concentration of the drug is very low, and the plasma concentration of orchemicalbook lilistat is <5ng/ml within 8h after oral administration of a single dose (maximum dose 800mg). Generally, systemic absorption of orlistat by the body is minimal at therapeutic doses, and there is no accumulation after short-term treatment. In vitro experiments, the binding rate of orlistat to plasma proteins is as high as 99% (lipoprotein and albumin are the main binding proteins), and orlistat rarely binds to red blood cells. Studies in obese patients have shown that the rarely absorbed orlistat has two main metabolites in plasma, M1(4-lactone ring hydrolysate) and M3(M1 attached to an n-formylleucine cleavage product), which account for 42% of the total plasma concentration. The inhibition of M1 and M3 on lipase was very weak. Unabsorbed orlistat is excreted mainly in the stool, accounting for about 97% of the dose taken, of which 83% is the original drug, the cumulative renal excretion of orlistat and its metabolites is less than 2%, and the complete excretion of the drug (stool and urine) takes 3 to 5 days. Both M1 and M3 can be excreted through bile. This product also has the effect of regulating blood lipids: it can reduce triglycerides (TG), low-density lipoprotein cholesterol LDL-C and increase the ratio of high-density lipoprotein to low-density lipoprotein in the serum of obese patients.

Purpose

Orlistat is a general-purpose lipase inhibitor that acts on the PL of human duodenal fluid with IC50 of 122 ng/ml.

Packaging Details: 25 kg/bag or as your requirement.
Port: Tianjin/ Qingdao/ Shanghai, etc.
We can ship the samples by air.
Lead Time: Within 2-3days after receiving the advance payment or original L/C.

XI'AN YI HANG CHEMICAL CO.,LTD was founded in 2002, located in xian City, shannxi, China. We are the high-tech chemical enterprise which specialized in researching, manufacturing and trading for chemical raw materials ,our products widely used in paints, textile, rubber, leather, plastic and so on.

With many years development and operation,we have become the group company for chemical production,we have the owned factory for produce stable quality products with high performance, and the advanced lab to ensure the best quality of each batch products.

We have our strictly quality control in our production, and we have passed ISO9001:2015 Quality Management System Certification and ISO14001 Environment Management System Certification.

Our main products includes Titanium Dioxide, Lithopone, Iron Oxide series, Chrome Oxide Green, Zinc Oxide, Carbon Black, STPP, SHMP, Oxalic Acid, DOP, SLES, and so on.

Q1: Are you manufacturer or trading company?

A1:Manufacturer.

Q2: Can I get some sample?
A2: Yes, usually 10-25g sample for free.

Q3: Is there a discount?
A3: Of course, welcome to contact us. Price would be different based on different quantity. For bulk
quantity, we will have discount for you.

Q4: How long for production and delivery?
A4: Most products we have in stock, sent time:Within 1-3 business days after received payment. Customized products further discussed.

Q5: Do you accept ODM or OEM service?
A5: Yes,we accept ODM and OEM services, ranges: Soft gel, Capsule, Tablet, Sachet, Granule,Private Label service, etc. Please contact us to design your own brand product.

Q6: How to deliver the goods?
A6: ≤50kg ship by FedEx or DHL etc, ≥50kg ship by Air, ≥100kg can be shipped by Sea. If you have special request on delivery, please contact us.

Q7: How to start orders or make payments?
A7:There are two ways for you to confirm order:
1. Proforma invoice with our company bank details will be sent to you once the order confirmed by Email. Pls arrange payment by  TT. Goods will be sent after received payment within 1-3 business days.
2. Trade assurance order will be drafted for you through ALIBABA. Pls confirm and pay through Alibaba. Goods will be sent after  received payment within 1-3 business days.