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| 10mg |
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| 25mg |
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Castanospermine, a novel indolizidine alkaloid first isolated from the seeds of Castanospermum australe, is a potent inhibitor of some glucosidase enzymes and has antiviral activity in vitro and in mouse models. Castanospermine was a lead to celgosivir. Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
| ln Vitro |
In BGK-21 cells, castanospermine (0.01-1000 μM, 48 hours) suppresses the formation of DEN infectious virus in a dose-dependent manner and decreases the glycosylated structural protein DEN prM's electrophoretic mobility [1].
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| ln Vivo |
Mice can become more susceptible to DEN-2 virus infection when given castanospermine (10, 50, or 250 mg/kg) intraperitoneally once every ten days [1]. Mice's susceptibility to DEN-2 virus infection can be boosted by intraperitoneal injection of castanospermine (10–500 mg/kg) [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: BHK-21 Tested Concentrations: 100, 500 μM Incubation Duration: 48 hrs (hours) Experimental Results: A modest reduction of up to 20 to 40% in marker gene expression or proliferation of WNV or DEN replicons, respectively. The effect on secretion of infectious WNV or WNV RNA-containing viral particles was minor, but the amount of DEN viral RNA and infectious virus was diminished. |
| Animal Protocol |
Animal/Disease Models: A/J mouse model [1]
Doses: 10, 50, 250 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: The secretion and virus infectivity of DEN-infected mice were diminished, and the survival rate of the virus was increased. Animal/Disease Models: Acute pancreatitis (AP) rat model [2] Doses: 10, 50, 100, 200, 500 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: The extent and severity of pancreatic damage were Dramatically diminished. Reduces serum interleukin production and NF-kB activation. Increased levels of TNF-a, ICAM-1 and VCAM-1. |
| References |
[1]. Whitby K, et al. Castanospermine, a potent inhibitor of dengue virus infection in vitro and in vivo. J Virol. 2005 Jul;79(14):8698-706.
[2]. Hong YP, et al. Effects of Castanospermine on Inflammatory Response in a Rat Model of Experimental Severe Acute Pancreatitis. Arch Med Res. 2016 Aug;47(6):436-445. [3]. Elbein AD. Glycosidase inhibitors: inhibitors of N-linked oligosaccharide processing. FASEB J. 1991 Dec;5(15):3055-63 [4]. den Dulk M, et al. Combined donor leucocyte administration and immunosuppressive drug treatment for survival of rat heart allografts. Transpl Immunol. 2004 Nov;13(3):177-84. |
| Molecular Formula |
C8H15NO4
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|---|---|
| Molecular Weight |
189.209
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| CAS # |
79831-76-8
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| Related CAS # |
141117-12-6 (HCl);79831-76-8;
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| SMILES |
O[C@H]1CCN2C[C@H](O)[C@@H](O)[C@H](O)[C@@]12[H]
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| InChi Key |
JDVVGAQPNNXQDW-TVNFTVLESA-N
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| InChi Code |
InChI=1S/C8H15NO4/c10-4-1-2-9-3-5(11)7(12)8(13)6(4)9/h4-8,10-13H,1-3H2/t4-,5-,6+,7+,8+/m0/s1
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| Chemical Name |
(1S,6S,7R,8R,8aR)-1,2,3,5,6,7,8,8a-octahydroindolizine-1,6,7,8-tetrol
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| Synonyms |
Castanospermine
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~100 mg/mL (~528.51 mM)
DMSO : ~100 mg/mL (~528.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (13.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (13.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (634.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2851 mL | 26.4257 mL | 52.8513 mL | |
| 5 mM | 1.0570 mL | 5.2851 mL | 10.5703 mL | |
| 10 mM | 0.5285 mL | 2.6426 mL | 5.2851 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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