Tìm theo
Ardeparin
antithrombins, heparins
Thuốc Gốc
Small Molecule
ATC: B01AB05, B01AB01
CTHH: C26H42N2O37S5
PTK: 1134.928
Ardeparin, marketed under the US trade name Normiflo, is a low molecular weight heparin (LMWH) anticoagulant used for the prevention of postoperative venous thrombosis. Ardeparin is derived via peroxide degradation of heparin extracted from porcine intestinal mucosa. Its molecular weight ranges from 2000 to 15,000 with an average molecular weight of 5500 to 6500. Normiflo was withdrawn from the US market in March 2000.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H42N2O37S5
Phân tử khối
1134.928
Monoisotopic mass
1134.006993818
InChI
InChI=1S/C26H42N2O37S5/c1-4(30)27-7-9(31)13(6(56-23(7)39)3-55-67(43,44)45)58-26-19(65-70(52,53)54)12(34)16(20(62-26)22(37)38)60-24-8(28-66(40,41)42)15(63-68(46,47)48)14(5(2-29)57-24)59-25-18(64-69(49,50)51)11(33)10(32)17(61-25)21(35)36/h5-20,23-26,28-29,31-34,39H,2-3H2,1H3,(H,27,30)(H,35,36)(H,37,38)(H,40,41,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)(H,52,53,54)
InChI Key
InChIKey=HTTJABKRGRZYRN-UHFFFAOYSA-N
IUPAC Name
3-[(5-{[6-carboxy-4,5-dihydroxy-3-(sulfooxy)oxan-2-yl]oxy}-6-(hydroxymethyl)-3-(sulfoamino)-4-(sulfooxy)oxan-2-yl)oxy]-6-({5-acetamido-4,6-dihydroxy-2-[(sulfooxy)methyl]oxan-3-yl}oxy)-4-hydroxy-5-(sulfooxy)oxane-2-carboxylic acid
Traditional IUPAC Name
3-[(5-{[6-carboxy-4,5-dihydroxy-3-(sulfooxy)oxan-2-yl]oxy}-6-(hydroxymethyl)-3-(sulfoamino)-4-(sulfooxy)oxan-2-yl)oxy]-6-({5-acetamido-4,6-dihydroxy-2-[(sulfooxy)methyl]oxan-3-yl}oxy)-4-hydroxy-5-(sulfooxy)oxane-2-carboxylic acid
SMILES
CC(=O)NC1C(O)OC(COS(O)(=O)=O)C(OC2OC(C(OC3OC(CO)C(OC4OC(C(O)C(O)C4OS(O)(=O)=O)C(O)=O)C(OS(O)(=O)=O)C3NS(O)(=O)=O)C(O)C2OS(O)(=O)=O)C(O)=O)C1O
Độ hòa tan
Soluble
logP
-8.3
logS
-2
pKa (strongest acidic)
-2.8
PSA
610.49 Å2
Refractivity
195.91 m3·mol-1
Polarizability
93.37 Å3
Rotatable Bond Count
20
H Bond Acceptor Count
33
H Bond Donor Count
15
Physiological Charge
-7
Number of Rings
4
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : Ardeparin, an anticoagulant, is a fractionated heparin. It acts at multiple sites in the normal coagulation system to inhibit reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo.
Cơ Chế Tác Dụng : Ardeparin, marketed under the US trade name Normiflo, is a low molecular weight heparin (LMWH) anticoagulant used for the prevention of postoperative venous thrombosis. Ardeparin is derived via peroxide degradation of heparin extracted from porcine intestinal mucosa. Its molecular weight ranges from 2000 to 15,000 with an average molecular weight of 5500 to 6500. Normiflo was withdrawn from the US market in March 2000. Ardeparin binds to antithrombin III, accelerating its activity in inactivating factor Xa and thrombin, thereby inhibiting thrombosis. Ardeparin also binds to heparin cofactor II, inhibiting thrombin. Ardeparin does not effect prothrombin time (PT) assays and may prolong activated partial thromboplastin time (APTT). Ardeparin has double the anti-factor Xa activity versus anti-factor IIa activity, compared to unfractionated heparin which has approximately equal anti-factor Xa activity and anti-factor IIa activity.
Dược Động Học :
▧ Absorption :
Well absorbed following subcutaneous administration, with a mean bioavailability of 92% (based on anti-factor Xa activity).
▧ Metabolism :
Liver and the reticulo-endothelial system are the sites of biotransformation.
▧ Half Life :
Elimination half-life for anti-factor Xa activity averages 3.3 hours following a single intravenous dose, while elimination half-life for anti-factor IIa activity averages 1.2 hours following a single intravenous dose.
Độc Tính : Symptoms of overdose may include excessive bleeding and bruising.
Chỉ Định : For prevention of deep vein thrombosis, which may result in pulmonary embolism, following knee surgery.
Liều Lượng & Cách Dùng : Injection - Subcutaneous
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00407
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=772
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505194
ChemSpider
http://www.chemspider.com/Chemical-Structure.751.html
PharmGKB
http://www.pharmgkb.org/drug/PA164754878
Wikipedia
http://en.wikipedia.org/wiki/Ardeparin
Drugs.com
http://www.drugs.com/mtm/ardeparin.html
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