| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
More potent than prednisolone CD163 in human peripheral blood mononuclear cells [1], NO-prednisolone (NCX-1015) is a NO-releasing derivative of prednisolone that has been shown to reduce inflammation, inhibit cytokine and chemokine production, and upregulate the expression of steroid-sensitive cell surface markers. CD163 is activated concentration-dependently when PBMC are incubated with both NO-prednisolone (NCX-1015) and prednisolone. Prednisolone was not as successful in eliciting CD163 cell surface expression as NO-prednisolone was. Additionally, NO-prednisolone was found to be more effective than prednisolone when assessing the inhibitory effect of LPS-induced IL-1β production [2].
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| ln Vivo |
NO-prednisolone (NCX-1015) therapy in vivo efficiently increased IL-10 production, indicating that NO steroids cause a regulatory fraction of T cells that suppress intestinal inflammation. The two tested doses of NO-prednisolone, 0.5 and 5 mg/kg/day (corresponding to 0.33 and 3.3 mg/kg/day prednisone, respectively), were successful in lowering the colitis score and lessening the severity of wasting syndrome. The activity of myeloperoxidase (MPO). The treatment of NO-prednisolone also decreased the amount of tumor necrosis factor-α, IL-12, and IFN-γ protein and colonic mRNA. Inducible NO synthase and cyclooxygenase 2 expression were likewise decreased by NO-prednisolone, although colonic IL-10 mRNA or protein expression was not inhibited. In fact, mice given NO-prednisolone show increased expression of IL-10 [1].
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| References |
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| Molecular Formula |
C29H33NO9
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|---|---|
| Molecular Weight |
539.57
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| Exact Mass |
539.215
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| CAS # |
327610-87-7
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| PubChem CID |
9850209
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
736.2±60.0 °C at 760 mmHg
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| Flash Point |
399.0±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
4.21
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
39
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| Complexity |
1100
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@]12C[C@@H]([C@H]3[C@H]([C@@H]1CC[C@@]2(C(=O)COC(=O)C4=CC=C(C=C4)CO[N+](=O)[O-])O)CCC5=CC(=O)C=C[C@]35C)O
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| InChi Key |
MJHYBJOMJPGNMM-KGWLDMEJSA-N
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| InChi Code |
InChI=1S/C29H33NO9/c1-27-11-9-20(31)13-19(27)7-8-21-22-10-12-29(35,28(22,2)14-23(32)25(21)27)24(33)16-38-26(34)18-5-3-17(4-6-18)15-39-30(36)37/h3-6,9,11,13,21-23,25,32,35H,7-8,10,12,14-16H2,1-2H3/t21-,22-,23-,25+,27-,28-,29-/m0/s1
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| Chemical Name |
[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 4-(nitrooxymethyl)benzoate
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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 |
| 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 : ~25 mg/mL (~46.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.32 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 12.5 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. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.32 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 12.5 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 | 1.8533 mL | 9.2666 mL | 18.5333 mL | |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7067 mL | |
| 10 mM | 0.1853 mL | 0.9267 mL | 1.8533 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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