Specifications
- Purity
- ≥97% (HPLC)
- Appearance
- White to beige powder
- Identity
- 1H-NMR
Properties
- Solvents
- DMSO (20 mg/ml), DMF (20 mg/ml), ethanol (20 mg/ml)
- Melting Point
- 142-144° C
Category: API's & Intermediates
Pimecrolimus is a immunosuppressive natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase). Presumably through these actions, it blocks the activation of T cells by allogeneic dendritic cells (IC50=0.55nM) without affecting dendritic cells. Moreover, pimecrolimus suppresses the generation of pro-inflammatory cytokines by T cells, the release of pre-formed inflammatory mediators from mast cells and the activation of eosinophils. These effects support the use of pimecrolimus in countering inflammatory skin diseases, such as atopic dermatitis (eczema) and psoriasis.
Synonyms | Elidel, SDZ-ASM 981, 33-Epichloro-33-desoxyascomycin |
---|---|
Purity | ≥97% (HPLC) |
Appearance | White to beige powder |
CAS-Number | 137071-32-0 |
Molecular Formula | C43H68ClNO11 |
Molecular Weight | 810.45 |
Identity | 1H-NMR |
Solvents | DMSO (20 mg/ml), DMF (20 mg/ml), ethanol (20 mg/ml) |
Melting Point | 142-144° C |
Smiles | Cl[C@@H]1[C@@H](C[C@@H](CC1)/C=C(C)/[C@H]([C@H](C)[C@H](C2)O)OC([C@H](CCCC3)N3C(C([C@@](O)([C@H](C)C4)O[C@H]([C@H](C[C@@H](C)C/C(C)=C/[C@@H](CC)C2=O)OC)[C@H]4OC)=O)=O)=O)OC |
InChi Key | KASDHRXLYQOAKZ-XDSKOBMDSA-N |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | +4°C |
Handling Advice | Protect from light and moisture. |
Use / Stability | Stable for at least 2 years after receipt when stored at +4°C. |
Transportation | Not dangerous goods |
References | (1) D. Bochelen, et al., J. Pharmacol. Exp. Therap. 288, 653 (1999), (2) M. Grassberger, et al., Br. J. Dermatol. 141, 264 (1999), (3) T. Zuberbier, et al., J. All. Clin. Immunol. 108, 275 (2001), (4) F.S. Kalthoff, et al., Clin. Exp. Immunol. 130, 85 (2002), (5) K. Rappersberger, et al., J. Invest. Dematol. 119, 876 (2002), (6) J.G. Meingassner, et al., J. Invest. Dermatol. 121, 77 (2003), (7) F.S. Kalthoff, et al., Clin. Exp. Immunol. 133, 350 (2003), (8) J.G. Meingassner, et al., Br. J. Dermatol. 149, 853 (2003), (9) D.A. Plager, et al., Int. Arch. Allergy Immunol. 149, 119 (2009), (10) Z. Ma & Z. Jiao, Curr. Pharm. Des. 17, 3823 (2011) (Review), (11) S.G. Danby & M.J. Cork, Br. J. Dermatol. 168, 235 (2013) |
Quantity | 10 mg, 50 mg, Bulk |