Tìm theo
Sodium stibogluconate
Các tên gọi khác (13 ) :
  • Antimony (v) derivative OF sodium gluconate
  • Antimony sodium gluconate
  • Estibogluconato sodico
  • Myostibin
  • Natrii stibogluconas
  • Pentostam
  • Sodium stibogluconate
  • Stibanate
  • Stibanose
  • Stibatin
  • Stibinol
  • Stibogluconate de sodium
  • Trisodium 1-{[3-carboxylato-5-(1,2-dihydroxyethyl)-1-hydroxy-2,6,7-trioxa-1lambda(5)-stibabicyclo[2.2.1]hept-1-yl]oxy}-5-(1,2-dihydroxyethyl)-1-oxido-2,6,7-trioxa-1lambda(5)-stibabicyclo[2.2.1]heptane-3-carboxylate nonahydrate
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 16037-91-5
ATC: P01CB02
CTHH: C12H35Na3O26Sb2
PTK: 907.88
Sodium stibogluconate is a medicine used to treat leishmaniasis and is only available for administration by injection. It belongs to the class of medicines known as the pentavalent antimonials. Sodium stibogluconate is sold in the UK as Pentostam (manufactured by GlaxoSmithKline). Widespread resistance has limited the utility of sodium stibogluconate, and in many parts of the world, amphotericin or miltefosine are used instead. It is also being investigated as an anti-tumor agent.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H35Na3O26Sb2
Phân tử khối
907.88
Monoisotopic mass
905.918601405
InChI
InChI=1S/2C6H9O7.3Na.10H2O.2O.2Sb/c2*7-1-2(8)3(9)4(10)5(11)6(12)13;;;;;;;;;;;;;;;;;/h2*2-5,7-8H,1H2,(H,12,13);;;;10*1H2;;;;/q2*-3;3*+1;;;;;;;;;;;;-1;+3;+4/p-3/t2*2-,3-,4+,5-;;;;;;;;;;;;;;;;;/m11................./s1
InChI Key
InChIKey=YQDGWZZYGYKDLR-UZVLBLASSA-K
IUPAC Name
trisodium (3R,4S,5R)-1-{[(3R,4S,5R)-3-carboxylato-5-[(1R)-1,2-dihydroxyethyl]-1-oxido-2,6,7-trioxa-1$l^{5}-stibabicyclo[2.2.1]heptan-1-yl]oxy}-5-[(1R)-1,2-dihydroxyethyl]-1-hydroxy-2,6,7-trioxa-1$l^{5}-stibabicyclo[2.2.1]heptane-3-carboxylate nonahydrate
Traditional IUPAC Name
trisodium (3R,4S,5R)-1-{[(3R,4S,5R)-3-carboxylato-5-[(1R)-1,2-dihydroxyethyl]-1-oxido-2,6,7-trioxa-1$l^{5}-stibabicyclo[2.2.1]heptan-1-yl]oxy}-5-[(1R)-1,2-dihydroxyethyl]-1-hydroxy-2,6,7-trioxa-1$l^{5}-stibabicyclo[2.2.1]heptane-3-carboxylate nonahydrate
SMILES
O.O.O.O.O.O.O.O.O.[Na+].[Na+].[Na+].[H][C@@]1(O[Sb]2(O)(O[Sb]34([O-])O[C@@H](C([O-])=O)[C@@]([H])(O3)[C@]([H])(O4)[C@H](O)CO)O[C@@H](C([O-])=O)[C@@]1([H])O2)[C@H](O)CO
logP
-3.4
pKa (strongest acidic)
2.29
pKa (Strongest Basic)
-3
PSA
269.08 Å2
Refractivity
96.29 m3·mol-1
Polarizability
39.78 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
17
H Bond Donor Count
5
Physiological Charge
-2
Number of Rings
4
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : The mode of action of sodium stibogluconate is not clearly understood. In vitro exposure of amastigotes to 500 mg pentavalent antimony/ml results in a greater than 50% decrease in parasite DNA, RNA protein and purine nucleoside triphosphate levels. It has been postulated that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis.
Cơ Chế Tác Dụng : Sodium stibogluconate is a medicine used to treat leishmaniasis and is only available for administration by injection. It belongs to the class of medicines known as the pentavalent antimonials. Sodium stibogluconate is sold in the UK as Pentostam (manufactured by GlaxoSmithKline). Widespread resistance has limited the utility of sodium stibogluconate, and in many parts of the world, amphotericin or miltefosine are used instead. It is also being investigated as an anti-tumor agent. Sodium stibogluconate directly inhibits DNA topoisomerase I leading to inhibition of both DNA replication and transcription.
Độc Tính : The main symptoms of antimony overdosage are gastro-intestinal disturbances (nausea, vomiting and severe diarrhoea). Haemorrhagic nephritis and hepatitis may also occur.
Chỉ Định : For the treatment of various types of a protozoal infection called leishmaniasis, which may result from sandfly bites in tropical and temperate parts of the world. Also investigated for use/treatment in cancer/tumors (unspecified) and solid tumors.
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05630
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00582
PharmGKB
http://www.pharmgkb.org/drug/PA164743129
Wikipedia
http://en.wikipedia.org/wiki/Sodium_stibogluconate
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