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Sitagliptin; CAS 486460 -32-6

Colour
White
Transport Package
Bags
Specification
25KG
Trademark
Ruisite
Origin
China
Production Capacity
20000
Reference Price
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Product Description

Product Description

Sitagliptin; CAS 486460-32-6
Product Name:  Sitagliptin 
CAS No.:  486460-32-6
Molecular Formula: C16H15F6N5O
Molecular Weight: 407.3136
Property: White powder
Assay: 99%
Package: 25kg/drum

Application:

Sitagliptin is an oral antihyperglycemic of the dipeptidyl peptidase-4  inhibitor class. This enzyme-inhibiting drug is used either alone or in combination with other oral antihyperglycemic agents for treatment of diabetes mellitus type 2.The benefit of this medicine is its fewer side effects in the control of blood glucose values. While safety is its advantage, efficacy is often challenged as it is often recommended to be combined with other agents such as metformin.

 
 

 

Sitagliptin Chemical Properties
Melting point  114.1-115.7 °C
Boiling point  529.9±60.0 °C(Predicted)
density  1.61±0.1 g/cm3(Predicted)
pka 7.20±0.10(Predicted)
CAS DataBase Reference 486460-32-6(CAS DataBase Reference)
EPA Substance Registry System 1-Butanone, 3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-, (3R)- (486460-32-6)
Safety Information
Hazardous Substances Data 486460-32-6(Hazardous Substances Data)
MSDS Information
 
Sitagliptin Usage And Synthesis
Description Sitagliptin is an orally-bioavailable selective DPP4 inhibitor that was discovered through the optimization of a class of β-aminoacid-derived DPP4 inhibitors. It lowers DPP4 activity in a sustained manner following once daily administration, preserves the circulating levels of intact GIP and GLP1 following meals in both acute and chronic studies and reduces blood glucose levels without significant increases in hypoglycaemia.

Sitagliptin phosphate (STG) is used to treat DM type 2 because it improves glycemic control by increasing the levels of active incretin hormones, GLP-1 (peptide-1) and GIP (glucose-dependent ins ulinotropic peptide). The activation of these incretins in β-pancreatic cells causes increased levels of cyclic adenosine monophosphate (cAMP) and intracellular calcium, with subsequent glucose-dependent insu lin secretion (2). This hypoglycemic drug belongs to a new class called dipeptidyl peptidase IV inhibitors. STG was approved by the FDA in 2006.
Mechanism of action Sitagliptin prolongs the activity of proteins that increase the release of ins ulin after blood sugar rises, such as after a meal. Sitagliptin is a selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), which metabolizes the naturally occurring incretin hormones glucagon-like peptide-1(GLP-1) and glucose-dependent ins ulinotropic polypeptide (GIP) resulting in enhanced glucose-dependent ins ulin secretion from the pancreas and decreased hepatic glucose production. Since GLP-1 enhances in sulin secretion in the presence of raised blood glucose levels, inhibiting DPP-IV activity will increase and prolong the action of GLP-1 by reducing its rate of inactivation in plasma. Sitagliptin reduces hemoglobin A1c (HbA1c), fasting and postprandial glucose by glucose-dependent stimulation of insu lin secretion and inhibition of glucagon secretion. GLP-1 has other widespread effects including delaying gastric emptying, significantly reducing glucagons levels and possible central effects on the appetite.
Pharmacokinetics Bioavailability of sitagliptin is approximately 87%. Halflife is between 8-14 hours. It is 38% bound to plasma proteins. It undergoes limited metabolism via CYP3A4 and CYP2C8. Elimination is mainly through urine.
Indications Sitagliptin is approved by the FDA as an adjunct to diet and exercise to improve glycaemic control in patients with T2DM, either as a monotherapy, or in combination with metformin or a peroxisome proliferatoractivated receptor-γ agonist (for example, thiazolidinediones) when the single agent does not provide adequate glycaemic control.
Clinical Use In October 2006, the U.S. Food and Drug Administration (FDA) approved sitagliptin as monotherapy and as add-on therapy to either of two other types of oral diabetes medications, metformin or thiazolidinediones to improve blood glucose control in patients with type 2 diabetes when diet and exercise are not enough. In March, 2007 it was approved in European Union. Sitagliptin is currently approved in 42 countries. The recommended dose of sitagliptin is 100 mg once daily. It may be taken with or without food. In April, 2007 FDA approved the combination product of sitaglibtin and metformin for type 2 diabetes. In clinical trials of 1-year duration, sitagliptin improved glycaemic control by reducing both fasting and postprandial glucose concentrations, leading to clinically meaningful reductions in glycosylated haemo  globin levels. Monotherapy with sitagliptin 100mg daily decreases mean HbA1c by 0.6- 0.79% (mean difference from placebo). When used in combination with metformin or pioglitazone, the mean reduction is HbA1c is 0.7% and 0.9% respectively. Sitagliptin is considered to be weight neutral and lipid neutral.
Side effects In clinical trials, sitagliptin demonstrated an overall incidence of side effects comparable to placebo. The most common side effects in studies were upper respiratory tract infection, stuffy or running nose, sore throat, headache and diarrhea. The incidence of hypoglycemia with sitagliptin monotherapy was not significantly different than placebo. Pooled data from 2 monotherapy and 2 combination trials show that the incidence of hypoglycemia was 1.2% and 0.9% for sitagliptin 100mg and placebo respectively.
Drug interactions Sitagliptin plasma concentrations may be increased modestly (approximately 68%), with cyclosporine which is not expected to be clinically important. Dig oxin plasma levels may be increased slightly (approximately 18%), no dosage adjustment is recommended. Although sitagliptin is not as likely to cause hypoglycemia as some other oral diabetes medications, be careful while prescribing any other drug that can potentially lower blood sugar, such as: probenecid, nonsteroidal anti-inflammatory drugs (NSAIDs), aspirin or other salicylates, sulfa drugs, a monoamine oxidase inhibitor (MAOI) or beta-blockers.
Description Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is a first-in-class oral drug launched for the treatment of type 2 diabetes. It acts by slowing the inactivation of incretins, which are endogenous peptides involved in the physiologic regulation of glucose homeostasis. Incretin hormones, including glucagonlike peptide-1 (GLP-1) and glucose-dependent insu linotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. When blood glucose concentrations are normal or elevated,GLP-1 and GIP increase the synthesis and release of insu lin from pancreatic b cells via intracellular signaling pathways involving cAMP. GLP-1 also lowers glucagon secretion from pancreatic αcells, which leads to reduced hepatic glucose production.
Originator Merck (US)
Uses Labeled Sitagliptin , intended for use as an internal standard for the quantification of Sitagliptin by GC- or LC-mass spectrometry.
Definition ChEBI: A triazolopyrazine that exhibits hypoglycemic activity.
Brand name Ruisite

Packaging & Shipping

Sitagliptin; CAS 486460-32-6
Sitagliptin; CAS 486460-32-6

 

Company Profile

Hebei Ruisite Technology Co .,ltb  is a professional chemical company in China. Specializing deal and export various kinds of quality chemicals since 1997. The products Include industry chemical, Animal feed additive, Food additive, Agrochemical, Fertilizer, pharmaceu-ticals, water treatment and Minerals. Our management team has over 17 years of combined expertise meeting the needs of clients. We are proud our quality chemcials and service was approbated by the clients in the worldwide.
 
  Hebei Ruisite Technology Co .,ltb   is an ISO9001:2008 certificated organization. We alway pay attention to the quality control. For us, quality means satisfied clients. Only by constantly improving our internal and external procedures are we able to remain a reliable supplier of chemicals for our clients worldwide. Every step of the distribution chain is constantly checked and rechecked to guarantee the quality. Through continuous improvement in quality and service, we will provide our customers with products of optimum quality consistent with their requirements.
 
Besides the quality, we think the competitive price of goods is also important. Our comprehensive distribution network, buying power and efficient inventory management system allow us to offer our products at the best possible prices. Our principle is: Quality Chemicals With Competitive Prices - We Supply!
 
Up to now many of our chemicals have been done REACH final registration. It is convenient for the clients to use our chemicals in Europe market.
 
Your satisfaction is our most interested thing. Also your any suggestion will be highly welcome by us. Now enjoy your visiting and hope to hearing from you!
Sitagliptin; CAS 486460-32-6

FAQ

Q1: Can I get samples?
A: Yes, we can supply free sample, you pay for the freight charge only.
Q2: How to pay? 
A: PI will be sent firstly after our aligned products specification. Payment by Paypal , T/T, Western Union,LC, are ok.
Q3: How is your MOQ? 
A: Normally speaking, our MOQ is 1kg. But we can also accept less quantity such as 100g on the condition that sample charge is100% paid.
Q4: How can you guarantee the quality of your products ?
1. Our staff are all experienced in chemical products or related major background, they are well trained before quotation.
2. Free sample or pre-shipment sample are available for our new cooperation before you place commercial order. We are sure the same specification commercial products as sample to customers
3. Third Party Inspection like SGS can be arranged according to your requirement before shipping.
4. On-Spot QC in our APPROVED associated production bases with necessary certification like GMP, ISO etc.
Q5: Do you have any other chemicals?
A: Yes, We can provide kinds of additives and fungicides, such as PHMB, PCMX, PVP, DCMX, Glutaraldehyde, Chlorhexidine digluconate 20%, ZPT, CMIT/MIT 14%, Carbomer, BKC, etc ..... 
Q6: If you still have questions, contact with us ~

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