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Keywords

1367369-76-3 Entecavir monohydrate Entecavir

Quick Details

Appearance:White to Off-White/Yellow Crystalline Powder
Application:An oral antiviral drug used in the treatment of hepatitis B infection. A guanine analogue that inhhibits all three steps in the viral replication process
PackAge:According to customer requirements
ProductionCapacity:2000|Kilogram|Year
Storage:-20°C Freezer
Transportation:BY AIR

Superiority:

Chemical Name: Entecavir

Molecular Formula: C12H15N5O3

Formula Weight: 277.283

CAS No.:142217-69-4;1367369-76-3

White to Off-White/Yellow Crystalline Powder

Purity:99.5%

Single impurity:NMT0.1%

Total impurity:NMT0.3%

Adefovir dipivoxil regulates the immune system and let the immune system to attack liver cells of the intrusion of HBV , and clear the virus, but this method will develop resistance, at the same time for patients with renal dysfunction or potential renal dysfunction risk, the use of adefovir dipivoxil chronic treatment will lead to renal toxicity. If eating 1 mg every day, in the three months will produce nephrotoxicity, this will lead to severe renal failure. These patients should be closely monitoring renal function and making appropriate dosage adjustments.

Bisphosphonates is quick conversion of adefovir dipivoxil in vivo, adefovir dipivoxil is a kind of single adenosine monophosphate acyclic nucleoside analogues, became to activity of the metabolites of adefovir in cellular kinases by phosphorylation in cellular kinases. A Duff Vee two phosphate through the following two ways to suppress HBV DNA polymerase (reverse transcriptase); one is with the natural substrate of deoxyadenosine triphosphate competition, the second is the integration of viral DNA and induce DNA chain elongation terminated. A Duff Vee two phosphate to HBV DNA polymerase inhibition constant (KI) is 0.1μM, but of human DNA polymeraseα and γ is weak and Ki values were 1.18μM and 0.97 μM.

Anti-viral activity: in the human hepatoma cell line transfected with HBV, the concentration of A Duff Vee inhibited 50% viral DNA replication (IC50) is from 0.2 to 2.5uM.

Adefovir dipivoxil applies for the treatment of hepatitis B virus replication activity and serum amino acid transfer enzyme and persistently elevated liver decompensation adult patients with chronic hepatitis B patients.

Liver injury is often encountered in the course of hepatitis B treatment, hepatitis B therapy is inappropriate, as well as long-term use of drugs on the liver damage, will lead to the occurrence of liver damage.

After long-term taking adefovir dipivoxil tablets, once the withdrawal will aggravate the damage of liver function. Therefore, for stopping taking the patients should be monitored for liver function.

Adefovir dipivoxil is more moderate suitable for long-term use, suitable for patients with lamivudine resistant patients, their chances of producing drug resistance is small, because the amount is less, side effects are small.

Entecavir is new, antiviral effect is also strong, if not treated with lamivudine, the possible resistance is the smallest, but it and lamivudine have cross resistance, if treated with lamivudine to take entecavir produced resistance rate is much greater.

The above information is Chemicalbook Hanya edited.

Details:

Name	Entecavir(monohydrate)
Batch No.	20120303	Quantity		500kg
Date of Production	Mar.3rd,2012	Analysis Date		Mar.4th,2012
Product standard	Enterprise standard	Expiry Date		Mar.2nd,2014

Item	Requirements		Test Results
Description	White crystalline powder		White crystalline powder

Identification	The IR absorption spectrum of the sample must be concordant with entecavir		conform
Optical rotation	+24.0°—+28.0°(MeOH:DMF=1:1 1%)		+26.3°
Water	5.8%—6.5%		6.25%
Residue on ignition	0.2%(max)		0.06%
Total impurities	0.3%(max)		0.06%
Single impurity	0.1%(max)		0.03%
Assay(HPLC)	99.0%(min)		99.9%

Application:An oral antiviral drug used in the treatment of hepatitis B infection. A guanine analogue that inhhibits all three steps in the viral replication process.

142217-69-4;1367369-76-3 entecavir

product Name	entecavir
Synonyms	2-Amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one; 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3,9-dihydro-6H-purin-6-one; 2-amino-9-[(3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3,9-dihydro-6H-purin-6-one; 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-1,9-dihydro-6H-purin-6-one hydrate (1:1); entecavir Baraclude
Molecular Formula	C₁₂H₁₅N₅O₃
Molecular Weight	277.2792
InChI	InChI=1/C12H15N5O3/c1-5-6(3-18)8(19)2-7(5)17-4-14-9-10(17)15-12(13)16-11(9)20/h4,6-8,18-19H,1-3H2,(H3,13,15,16,20)/t6-,7-,8+/m0/s1
CAS Registry Number	142217-69-4;1367369-76-3
Molecular Structure
Refractive index	1.837
Hazard Symbols