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| ln Vitro |
Additionally, XJB-5-131 enhances the activation of caspases 3 and 7, two proapoptotic enzymes, in the ileal mucosa when hemorrhagic shock (HS) is applied [1]. In vitro, XJB-5-131 enhances cell survival and decreases apoptosis in mouse embryonic cells [2]. A radioprotectant for colony-forming units granulocyte macrophages (CFU-GM) is XJB-5-131. When applied after radiation, XJB-5-131 functions as an efficient moderator [3].
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| ln Vivo |
In rats suffering from hemorrhagic shock (HS), XJB-5-131 enhances the peroxidation of cardiolipin and mitochondrial phospholipids in ileal mucosal samples[1]. Even though only a little amount of crystalloid solution (2.8 mL/kg) and no blood transfusion were given, rats with severe blood loss had a much longer survival rate (33.5 mL/kg) after receiving an intravenous injection of XJB-5-131 (2 μMol/kg)[1]. XJB-5-131 promotes mitochondrial function, prevents weight loss and oxidative damage to mitochondrial DNA, preserves the number of copies of mitochondrial DNA, increases neuronal survival, and improves exercise capacity. In a mouse model of Huntington's disease (HD), XJB-5-131 dramatically suppresses the disease phenotype and enhances mitochondrial function[2]. In HD mice models, XJB-5-131 (1 mg/kg; intraperitoneal injection; three times per week for up to 57 weeks) prevents weight loss and the deterioration of motor function[2].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Low density mononuclear cells (MNC) Tested Concentrations: 10 μM Incubation Duration:Added to cells one hour before irradiation or immediately after irradiation Experimental Results: Was a protector when given before irradiation as shown by an increase in the D0 to 1.93±0.13 for CFU-GM with XJB-5-131. |
| Animal Protocol |
Animal/Disease Models: Male specific pathogen-free SD (Sprague-Dawley) rats, weighing 150 to 250 g[1]
Doses: 2 μmol/kg Route of Administration: Administered intravenously (iv) using a syringe pump Experimental Results: The rats treated with XJB-5-131 survived Dramatically longer ( P < 0.01). Three of six survived for longer than 3 hrs (hours) after completion of the hemorrhage protocol and one rat survived for the whole 6 hrs (hours) postbleeding observation period. Animal/Disease Models: HD150KI mice[2] Doses: 1 mg/kg Route of Administration: intraperitoneally (ip) injected; three times a week up to 57 weeks Experimental Results: Chronic treatment suppressed weight loss. Increased the average body mass by 22%. |
| References |
[1]. Carlos A Macias, et al. Treatment with a novel hemigramicidin-TEMPO conjugate prolongs survival in a rat model of lethal hemorrhagic shock. Ann Surg. 2007 Feb;245(2):305-14.
[2]. Zhiyin Xun, et al. Targeting of XJB-5-131 to mitochondria suppresses oxidative DNA damage and motor decline in a mouse model of Huntington's disease. Cell Rep. 2012 Nov 29;2(5):1137-42. [3]. Julie P Goff, et al. Evaluation of potential ionizing irradiation protectors and mitigators using clonogenic survival of human umbilical cord blood hematopoietic progenitor cells. Exp Hematol. 2013 Nov;41(11):957-66. |
| Molecular Formula |
C53H81N7O9
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|---|---|
| Molecular Weight |
960.25
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| CAS # |
866404-31-1
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| SMILES |
C1CC[C@@H](C(=O)N[C@H](C(N[C@@H](CCCNC(=O)OCC2=CC=CC=C2)C(NC2CC(C)(C)N([O-])C(C2)(C)C)=O)=O)C(C)C)N1C(=O)[C@H](/C=C/[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC1C=CC=CC=1
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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) |
DMSO: 125 mg/mL (130.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.17 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 20.8 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: ≥ 2.08 mg/mL (2.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0414 mL | 5.2070 mL | 10.4140 mL | |
| 5 mM | 0.2083 mL | 1.0414 mL | 2.0828 mL | |
| 10 mM | 0.1041 mL | 0.5207 mL | 1.0414 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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