Name | Sodium Stibogluconate |
Synonyms | SSG NASB NASBV Solustin Stibatin Stibinol Myostibin trisodium Stibanate myostibin Stibanose Pentostam Solusurmin Solyusurmin Solustibosan nonahydrate UNII-V083S0159D Natrii stibogluconas Sodium stibogluconate estibogluconatosodico Sodium Stibogluconate SODIUM STIBOGLUCONATE Estibogluconato sodico Stibogluconate sodique Stibogluconate de sodium Antimony sodium gluconate oxo-oxostibanyloxy-stibane Natrii stibogluconas [INN-Latin] Estibogluconato sodico [Spanish] Estibogluconato sodico [INN-Spanish] Stibogluconate de sodium [INN-French] Antimony(V) derivative of sodium gluconate Antimony (V) derivative of sodium gluconate (2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanoate Trinatrium bis(gluconato(3)-O2,O3,O4)hydroxooxido-oxy-bis-antimonat(V) |
CAS | 16037-91-5 |
InChI | InChI=1/2C6H12O7.3Na.12H2O.2Sb/c2*7-1-2(8)3(9)4(10)5(11)6(12)13;;;;;;;;;;;;;;;;;/h2*2-5,7-11H,1H2,(H,12,13);;;;12*1H2;;/q;;3*+1;;;;;;;;;;;;;;/p-3 |
InChIKey | VJCZMGLJTJZFEN-ZYPIZMQFSA-K |
Molecular Formula | C12H37Na3O27Sb2 |
Molar Mass | 925.9 |
Melting Point | >250°C (dec,) |
Boling Point | 673.6°C at 760 mmHg |
Flash Point | 375.1°C |
Solubility | H2O: 1mg/mL at~75°C |
Vapor Presure | 4.95E-21mmHg at 25°C |
Appearance | solid |
Color | pale yellow |
Storage Condition | 2-8°C |
Stability | Hygroscopic |
Physical and Chemical Properties | White or slightly yellowish amorphous powder. Soluble in hot water, soluble in water, insoluble in ethanol or ether. Odorless. The aqueous solution showed right rotation. |
Use | Anti-kala-azar drugs |
In vitro study | Sodium stibogluconate (Stibogluconate trisodium nonahydrate) inhibits 99% of SHP-1 activity at 10 μg/mL, a therapeutic concentration of the drug for leishmaniasis. Similar degrees of inhibition of SHP-2 and PTP1B required 100 μg/mL Sodium stibogluconate. The inhibition of cellular PTPases by the Sodium stibogluconate is suggested by its rapid induction of tyrosine phosphorylation of cellular proteins in Baf3 cells and its augmentation of IL-3-induced Janus family kinase 2/Stat5 tyrosine phosphorylation and proliferation of Baf3 cells. The augmentation of the opposite effects of GM-CSF and IFN-α on TF-1 cell growth by Sodium stibogluconate indicate its broad activities in the signaling of various cytokines. |
In vivo study | Sodium stibogluconate (Stibogluconate trisodium nonahydrate) induces 61% growth inhibition of Renca tumors in BALB/c mice coincident with an increase (2-fold) in tumor-infiltrating macrophages. A combination of Sodium stibogluconate and IL-2 is more effective in inhibiting tumor growth (91%) and inducing tumor-infiltrating (4-fold), whereas IL-2 alone has little effect. |
Risk Codes | R20/22 - Harmful by inhalation and if swallowed. R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | 3282 |
WGK Germany | 3 |
RTECS | CC7930000 |
Hazard Class | 6.1(b) |
Packing Group | III |
Toxicity | LD50 ipr-mus: 33 mg/kg CLDND* 11,155,49 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.08 ml | 5.4 ml | 10.8 ml |
5 mM | 0.216 ml | 1.08 ml | 2.16 ml |
10 mM | 0.108 ml | 0.54 ml | 1.08 ml |
5 mM | 0.022 ml | 0.108 ml | 0.216 ml |