(S)-(+)-Ibuprofen

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 1g
ArtNr HY-78131A-1g
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
(S)-Ibuprofen
CAS No.
51146-56-6
Purity
>98%
MW
2062808
Formula
C13H18O2
Solubility
10 mM in H2O; DMSO: < 0.1 mg/mL
Biological Description
S(+)-Ibuprofen is capable of inhibiting cyclooxygenase (COX) at clinically relevant concentrations, R(-)-ibuprofen is not a COX inhibitor.
IC50 Value: 13 uM (COX1); 370 uM (COX2) [1]
Target: COX1/2
The two enantiomers of ibuprofen are therefore different in terms of their pharmacological properties and may be regarded as two different 'drugs'. They also differ in terms of their metabolic profiles.
in vitro: R(-)-ibuprofen becomes involved in pathways of lipid metabolism and is incorporated into triglycerides along with endogenous fatty acids. S(+)-Ibuprofen does not appear to become involved in these unusual metabolic reactions, which is why S(+)-ibuprofen is regarded as being metabolically 'cleaner' than racemic ibuprofen [2]. Cosolvents exponentially increased the solubility of both SIB and racIB, especially in the presence of PG and PEG 300. Glycerol was not very effective in increasing the aqueous solubilities of both compounds, whereas sorbitol solution had a minimal effect on their solubility. PG and PEG 300 increased the solubility of SIB by 400-fold and 1500-fold, respectively, whereas the rise in solubility for racIB was 193-fold and 700-fold, respectively, at 25 degrees C for the highest concentration of the cosolvents used (80% v/v) [3].
in vivo: In the efficacy study the evaluation of the improvement of the WOMAC OA index showed equivalence of dexibuprofen 400 mg t.i.d. compared to racemic ibuprofen 800 mg t.i.d., with dexibuprofen being borderline superior (P = 0.055). The comparison between the 400 mg t.i.d. and 200 mg t.i.d. doses confirmed a significant superior efficacy of dexibuprofen 400 mg (P = 0.023). In the tolerability study the overall incidence of clinical adverse events was 15.2% (GI tract 11.7%, CNS 1.3%, skin 1.3%, others 0.9%). The active enantiomer dexibuprofen proved to be an effective NSAID with a significant dose-response relationship [4]. The S(+)-ibuprofen isomer was found to be more potent than the racemic formulation in analgesic and antiinflammatory tests and presented fewer gastric toxic effects [5].
Clinical trial: No Development Reported
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 1g
Lieferbar: In stock
Listenpreis: 108,93 €
Preis: 108,93 €
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