NO-prednisolone
Based on 1 Customer Validation
NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.
For research use only. We do not sell to patients.
- Purity: 98.58%
- CAS No.: 327610-87-7
- Formula: C29H33NO9
- Molecular Weight:539.57
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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IL-10 |
NO-prednisolone (NCX-1015), an NO-releasing derivative of Prednisolone, is demonstrated to be more effective than Prednisolone in reducing inflammation, inhibiting cytokine and chemokine generation, and up-regulating the expression of the steroid-sensitive cell-surface marker CD163 in human peripheral blood mononuclear cells[1] Incubation of PBMCs with NO-prednisolone (NCX-1015) and Prednisolone produces a concentration-dependent activation of CD163. NO-prednisolone is more potent than Prednisolone at inducing CD163 cell surface expression. The increased efficacy of NO-prednisolone, compared with the parent molecule Prednisolone, is also observed when assessing inhibition of LPS induced IL-1β production[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 327610-87-7
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Appearance Solid
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Molecular Weight 539.57
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Formula C29H33NO9
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Color White to yellow
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SMILES
C[C@@]12[C@](C(COC(C3=CC=C(CO[N+]([O-])=O)C=C3)=O)=O)(O)CC[C@@]1([H])[C@]4([H])CCC5=CC(C=C[C@]5(C)[C@@]4([H])[C@@H](O)C2)=O
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Synonyms
NCX-1015
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (46.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.32 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Peripheral blood mononuclear cells (PBMCs) are isolated from heparinized human whole venous blood using Ficoll-Hypaque (d=1.077 g). PBMCs are then washed three times with HEPES buffered RPMI 1640 containing 0.05% gentamycin and 10% donor serum. Cells (1×106, ~20% monocytes, the remainder having been lymphocytes) are transferred to a 48 well plate and pre-incubated for 1 h with Prednisolone, NO-prednisolone (10 μM-0.1 nM) or vehicle, followed by activation with LPS (1 μg/mL) for 24 h at 37°C and 5% CO2. Supernatants are removed and IL-1β production measured using a commercially available human IL-1β ELISA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
BALB/c and male Swiss Albino mice (6-8 weeks old) are used. Mice (12 per group) are injected intrarectally with 50% ethanol or 1, 1.5, 2, or 2.5 mg per mouse of TNBS. TNBS-treated mice then are treated s.c. with 5 mg/kg/day Prednisolone or NO-prednisolone for 7 days. Surviving mice are killed 8 days after TNBS administration, colonic inflammation is scored, and myeloperoxidase (MPO) activity is measured. After instillation of 1.5 mg per mouse of TNBS, animals are allocated randomly into one of three treatment groups [placebo, NO-prednisolone (5 or 0.5 mg/kg/day s.c.), or Prednisolone (10 or 5 mg/kg/day s.c.)] and followed for 7 days. Mice are monitored for the appearance of diarrhea, loss of body weight, and overall mortality. At the end of the experiment, surviving mice are killed, blood samples are collected by cardiac puncture, and a 7 cm segment of the colon is excised for macroscopic and microscopic damage evaluation. Colonic IL-2, IL-10, IFN-γ, and tumor necrosis factor-α (ELISA and RT-PCR) and MPO activity are assessed according to published methods. In duplicate experiments, the colons of surviving mice are excised for LPMC preparation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Fiorucci S, et al. NCX-1015, a nitric-oxide derivative of prednisolone, enhances regulatory T cells in the lamina propria and protects against 2,4,6-trinitrobenzene sulfonic acid-induced colitis in mice. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15770-5. [Content Brief]
[2]. Paul-Clark M, et al. 21-NO-prednisolone is a novel nitric oxide-releasing derivative of prednisolone with enhanced anti-inflammatory properties. Br J Pharmacol. 2000 Dec;131(7):1345-54. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8533 mL | 9.2666 mL | 18.5333 mL | 46.3332 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7067 mL | 9.2666 mL | |
| 10 mM | 0.1853 mL | 0.9267 mL | 1.8533 mL | 4.6333 mL | |
| 15 mM | 0.1236 mL | 0.6178 mL | 1.2356 mL | 3.0889 mL | |
| 20 mM | 0.0927 mL | 0.4633 mL | 0.9267 mL | 2.3167 mL | |
| 25 mM | 0.0741 mL | 0.3707 mL | 0.7413 mL | 1.8533 mL | |
| 30 mM | 0.0618 mL | 0.3089 mL | 0.6178 mL | 1.5444 mL | |
| 40 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL |
NO-prednisolone Related Classifications
HY-101757 Related Classifications
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