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| Other Sizes |
| ln Vitro |
Sodium antimony gluconate (trisodium gluconate nonahydrate) inhibits 99% of SHP-1 activity at 10 μg/mL (the therapeutic concentration of leishmaniasis medicines). Similar degrees of inhibition of SHP-2 and PTP1B require 100 μg/mL sodium antimony gluconate. The inhibitory impact of stibogluconate on cellular PTPases is revealed by its rapid induction of tyrosine phosphorylation of cellular proteins in Baf3 cells and its augmentation of IL-3-induced Janus family inhibitor 2/Stat5 tyrosine phosphorylation and Baf3 cell proliferation. ..Sodium antimony gluconate promotes the opposing effects of GM-CSF and IFN-α on TF-1 cell proliferation, showing its extensive activity in various cytokine signal transductions [1].
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| ln Vivo |
Stibogluconate trisodium nonawater elicited 61% reduction of Renca tumor growth in the BALB/c probe, followed by an increase (2-fold) in tumor circulating macrophages. The combination of sodium antimony gluconate and IL-2 was more effective in suppressing tumor development (91 %) and generating tumor veins (4 times), but IL-2 alone had minimal impact [2].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of medication use during lactation Limited information available suggests that even with daily administration of up to 1.4 g of sodium antimony gluconate, low concentrations in breast milk are not expected to have any adverse effects on breastfed infants [1], especially in infants older than 2 months. However, if breastfeeding is discontinued during treatment, it can be resumed 24 to 48 hours after the last administration. ◉ Effects on breastfed infants No relevant published information was found as of the revision date. ◉ Effects on breastfeeding and breast milk No relevant published information was found as of the revision date. |
| References |
[1]. Pathak MK, et al. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001 Sep 15;167(6):3391-7.
[2]. Fan K et al. Sodium Stibogluconate Interacts with IL-2 in Anti-Renca Tumor Action via a T Cell-Dependent Mechanism in Connection with Induction of Tumor-Infiltrating Macrophages. J Immunol. 2005 Nov 15;175(10):7003-8 |
| Additional Infomation |
Sodium antimony gluconate is a drug used to treat leishmaniasis and is administered by injection only. It belongs to the pentavalent antimony class of drugs. Sodium antimony gluconate is marketed in the UK under the brand name Pentostam (manufactured by GlaxoSmithKline). Due to the widespread emergence of resistance, the clinical use of sodium antimony gluconate is limited, and in many parts of the world, amphotericin B or mitefoxine are used as alternatives. Currently, it is also being investigated as an anti-tumor drug. Antimony is a metal complex in which the metal can exist in pentavalent or trivalent forms. Pentavalent antimony gluconate is used to treat leishmaniasis. Trivalent antimony gluconate is most commonly used to treat schistosomiasis. Drug Indications Used to treat various types of leishmaniasis, a disease caused by protozoan infection, possibly caused by sandfly bites in tropical and temperate regions. It has also been studied for the treatment of cancer/tumors (unspecified) and solid tumors. Mechanism of Action Sodium antimony gluconate directly inhibits DNA topoisomerase I, thereby inhibiting DNA replication and transcription.
Pharmacodynamics The mechanism of action of sodium antimony gluconate is not fully understood. In vitro experiments have shown that exposure of amastigotes to 500 mg/ml pentavalent antimony leads to a decrease of more than 50% in the levels of parasite DNA, RNA, protein, and purine nucleoside triphosphates. Some studies suggest that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis leads to a reduction in the synthesis of macromolecules. |
| Molecular Formula |
C12H20O17SB2.3[NA].9[H2O]
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|---|---|
| Molecular Weight |
910.903920000001
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| Exact Mass |
908.926
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| CAS # |
16037-91-5
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| PubChem CID |
16683012
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| Appearance |
White to off-white solid powder
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| Boiling Point |
673.6ºC at 760mmHg
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| Flash Point |
375.2ºC
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| Vapour Pressure |
4.95E-21mmHg at 25°C
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
43
|
| Complexity |
699
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| Defined Atom Stereocenter Count |
8
|
| SMILES |
O=[Sb](O[C@]1([H])[C@H](O)CO)(O[C@@H](C(O)=O)[C@H]1O)O[Sb](O[C@]2([H])[C@H](O)CO)(O[C@@H](C(O)=O)[C@H]2O)=O.[9H2O].[3Na]
|
| InChi Key |
CUEDNFKBTFCOSV-UZVLBLASSA-L
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| InChi Code |
InChI=1S/2C6H10O7.3Na.9H2O.3O.2Sb/c2*7-1-2(8)3(9)4(10)5(11)6(12)13;;;;;;;;;;;;;;;;;/h2*2-5,7-8,10H,1H2,(H,12,13);;;;9*1H2;;;;;/q2*-2;3*+1;;;;;;;;;;;;;2*+2/p-2/t2*2-,3-,4+,5-;;;;;;;;;;;;;;;;;/m11................./s1
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| Chemical Name |
trisodium;(4R,5S,6R)-2-[[(4R,5S,6R)-4-carboxylato-6-[(1R)-1,2-dihydroxyethyl]-5-hydroxy-2-oxo-1,3,2λ5-dioxastibinan-2-yl]oxy]-6-[(1R)-1,2-dihydroxyethyl]-5-hydroxy-2-oxo-1,3,2λ5-dioxastibinane-4-carboxylate;nonahydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~3 mg/mL (~3.29 mM)
DMSO : ~1 mg/mL (~1.10 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0978 mL | 5.4891 mL | 10.9782 mL | |
| 5 mM | 0.2196 mL | 1.0978 mL | 2.1956 mL | |
| 10 mM | 0.1098 mL | 0.5489 mL | 1.0978 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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