显示标签为“Inhibitors”的博文。显示所有博文
显示标签为“Inhibitors”的博文。显示所有博文

2016年10月12日星期三

Linagliptin




Linagliptin (BI-1356, trade names Tradjenta (US), Trajenta (worldwide)) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.

Linagliptin (once-daily) was approved by the U.S. Food and Drug Administration (FDA) on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.

Medical uses

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.
Mechanism of action

TRADJENTA belongs to a class of drugs called DPP-4 inhibitors. DPP-4 inhibitors work by increasing hormones that stimulate your pancreas to produce more insulin and stimulate your liver to produce less glucose.In other words, TRADJENTA, along with diet and exercise, can help your body produce more insulin and less sugar. Managing your sugar can mean a lower A1C – and that's an important goal for anyone with type 2 diabetes.

products details:

1.Product name: Linagliptin
2.CAS No.:668270-12-0
3.Purity: 99% min
4.Storage information: Store in Cool and dry .place, keep away from strong light, high temperature
5.Usage:Pharmaceutical raw materials
6.Transportation:by air express delivery(DHL,FedEx,EMS ect.) or sea shipping (FOB,CIF,CFR,CNF ect.)
7.Sample:sample can be supplied if you inquiry 
8.Price: we will give you the best price !

Specification:
Product Name
Linagliptin       CAS 668270-12-0
Batch No.
150120
Quantity
25kgs
Test date
2015.01.20
Report date
2015.01.27
Expire date
2017.01.20
Standard
In-house
Result of Analysis
Items
Specifications
Results
Appearance
White or off-white crystalline
powder
Conforms
HPLC
The retention time of the major peaking the chromatogram of the sample corresponds to that exhibited by the working standard
Conforms
Loss on drying
No more than 1.0%
0.40%
Residue on Ignition
No more than 0.1%
0.02%
Heavy Metals
No more than 20ppm
<10ppm
Related substances
Total impurities no more than 1.0%
0.50%
Single impurity no more than 0.5%
Conforms
Residual solvents
Ethyl acetate No more than 0.1%
Conforms
Ethanol No more than 0.1%
Conforms
Purity
No less than 99.0%
99.50%
Conclusion
Conforms to the In-house standard.

my contact infomation is:

Email: cloris_2016@tuskwei.com or

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Notice: This product is only suitable for laboratory use, or the use of animals. It can not be used directly on the human body









2016年9月5日星期一

Sulbactam


Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics.
Mechanism
Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.
Uses
Sulbactam is able to inhibit the most common forms of β-lactamase but is not able to interact with the AmpC cephalosporinase. Thus, it confers little protection against bacteria such as Pseudomonas aeruginosa, Citrobacter, Enterobacter, and Serratia, which often express this gene.
In the United States, sulbactam is combined to form cefoperazone/sulbactam and ampicillin/sulbactam. It does possess some antibacterial activity when administered alone, but it is too weak to have any clinical importance. Its use in the UK is restricted to hospitals.
Recently, its use in treating Acinetobacter septicemia is receiving renewed interest.
Basic information
Product Name:Sulbactam
Synonyms:(2S,5R)-3,3-DIMETHYL-4,4,7-TRIOXO-4LAMBDA6-THIA-1-AZA-BICYCLO[3.2.0]HEPTANE-2-CARBOXYLIC ACID;(2S-CIS)-3,3-DIMETHYL-7-OXO-4-THIA-1-AZABICYCLO[3,2,0]HEPTANE-2-CARBOXYLIC ACID 4,4-DIOXIDE;3,3-DIMETHYL-4,4,7-TRIOXO-4LAMBDA6-THIA-1-AZA-BICYCLO[3.2.0]HEPTANE-2-CARBOXYLIC ACID;SULBACTAM;SULBACTAM ACID;sulbactam acid (base);PENICILLANIC ACID SULFONE;(2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide
CAS:68373-14-8
MF:C8H11NO5S
MW:233.24
Product Categories:Peptide Synthesis/Antibiotics;MERITAL
Mol File:68373-14-8.mol
 
Chemical Properties
boiling point567.7 °C at 760 mmHg
density1.62 g/cm3
vapor pressure2.26E-14 mmHg at 25°C
flashing point297.1 °C
storage temp.−20°C
solubilitydissolved in water, methanol and ethyl acetate
Specification:
ITEMS
STANDARD
RESULTS
Characters
White or almost white crystalline  granule and powder
A white crystalline granule and powder
Identification
(1)  The  spectrum obtained with the substance to be examined corresponds with that obtained with reference standard
(2)  Should meet the requirement under water
Comforms
Appearance of solution
≤reference suspension II
(1 mol/L hydrochloric acid)
≤reference suspension II
(2 mol/L ammonia)
≤Reference suspension I

≤Reference suspension I
PH
3.5~5.5
4.4
Specific optical rotation
+280~ +305
+296
Related substances
Any impurity≤1.0%
          0.26%
Dimethylaniline
≤20ppm
Complies
(not used in process) 
Water
12.0%~15.0%
13.3%
Sulphated ash
≤0.5%
0.07%
Bulk density
0.45g/ml - 0.65g/ml
0.57g/ml
Tapped density
≥0.65g/ml
0.76g/ml
Assay
96.0%~102.0%  C16H19N3O4S
(calculated on the anhydrous basis)
99.7%

my contact information is: 

Email: cloris_2016@tuskwei.com

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