Mapracorat (Synonyms: ZK-245186; BOL-303242X) |
| Katalog-Nr.GC19239 |
Mapracorat ist ein neuartiger nicht-steroidaler selektiver Glukokortikoid-Rezeptor-Agonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 887375-26-0
Sample solution is provided at 25 µL, 10mM.
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Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
Mapracorat concentration dependently inhibited TNFα secretion from activated canine PBMC with IC50 value of approximately 0.2 nM.
Intradermal injection of compound 48/80 (50 ug in 50 uL saline) resulted in a clear wheal and flare reaction over the 60 min observation period. Topical pre-treatment with mapracorat (0.1%) and triamcinolone acetonide (0.015%) led to significant reduction in the wheal and flare responses compared to vehicle (acetone) treated areas. However, once daily topical administration of triamcinolone acetonide significantly reduced skin fold thickness from day 8 to 14, whereas no such reduction was observed for mapracorat.
References:
[1]. Baumer W , et al. The selective glucocorticoid receptor agonist mapracorat displays a favourable safety-efficacy ratio for the topical treatment of inflammatory skin diseases in dogs. Vet Dermatol. 2017 Feb; 28(1):46-e11.
[2]. Baiula M, et al. Mapracorat, a novel non-steroidal selective glucocorticoid receptor agonist for the treatment of allergic conjunctivitis.Inflamm Allergy Drug Targets. 2014; 13(5):289-98.
| Cas No. | 887375-26-0 | SDF | |
| Überlieferungen | ZK-245186; BOL-303242X | ||
| Canonical SMILES | CC(C)(C1=C(OCC2)C2=CC(F)=C1)C[C@@](O)(CNC3=C4C=CC(C)=NC4=CC=C3)C(F)(F)F | ||
| Formula | C25H26F4N2O2 | M.Wt | 462.48 |
| Löslichkeit | DMSO : ≥ 50.6 mg/mL (109.41 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1623 mL | 10.8113 mL | 21.6226 mL |
| 5 mM | 0.4325 mL | 2.1623 mL | 4.3245 mL |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1623 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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