Apremilast-d5 (Synonyms: APR-d5) |
Catalog No.GC46867
One-Click Copy Product Info
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An internal standard for the quantification of apremilast
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1258597-47-5
Sample solution is provided at 25 µL, 10mM.
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Apremilast-d5 is intended for use as an internal standard for the quantification of apremilast by GC- or LC-MS. Apremilast is an inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP.1,2 It is orally active, significantly decreasing epidermal thickness and the epithelial cell proliferation index in a mouse model of psoriasis.2 Apremilast reduces both TNF-α and matrix metalloproteinase-3 production in gut lamina propria mononuclear cells from patients with inflammatory bowel disease.3 It also blocks spontaneous production of TNF-α from human rheumatoid synovial cells and improves the clinical score in mouse models of arthritis.4
1.Man, H.W., Schafer, P., Wong, L.M., et al.Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitorJournal of Medicinal Chemistry52(6)1522-1524(2009) 2.Schafer, P.H., Parton, A., Gandhi, A.K., et al.Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasisBritish Journal of Pharmacology159(4)842-855(2010) 3.Gordon, J.C., Prothero, J.D., Thornton, C.A., et al.CC-10004 but not thalidomide or lenalidomide inhibits lamina propria mononuclear cell TNF-α and MMP-3 production in patients with inflammatory bowel diseaseJ.Crohns.Colitis.3(3)175-182(2009) 4.McCann, F.E., Palfreeman, A.C., Andrews, M., et al.Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritisArthritis Research & Therapy12(3)(2010)
| Cas No. | 1258597-47-5 | SDF | |
| Synonyms | APR-d5 | ||
| Canonical SMILES | O=C1N([C@H](CS(C)(=O)=O)C2=CC(OC([2H])([2H])C([2H])([2H])[2H])=C(OC)C=C2)C(C3=C(NC(C)=O)C=CC=C31)=O | ||
| Formula | C22H19D5N2O7S | M.Wt | 465.5 |
| Solubility | DMSO : 100 mg/mL (214.81 mM; Need ultrasonic); DMSO : 44 mg/mL (94.52 mM; Need ultrasonic) | 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 | 2.1482 mL | 10.7411 mL | 21.4823 mL |
| 5 mM | 429.6 μL | 2.1482 mL | 4.2965 mL |
| 10 mM | 214.8 μL | 1.0741 mL | 2.1482 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)