ASM 981
Pimecrolimus
CAS: 137071-32-0
Molecular Formula: C43H68ClNO11
ASM 981 - Names and Identifiers
ASM 981 - Physico-chemical Properties
| Molecular Formula | C43H68ClNO11 |
| Molar Mass | 810.45 |
| Density | 1.19 |
| Melting Point | 135-136 °C |
| Boling Point | 866.1±75.0 °C(Predicted) |
| Flash Point | 477.6°C |
| Solubility | DMSO (Slightly, Sonicated), Chloroform (Slightly), Methanol (Slightly) |
| Vapor Presure | 5.44E-35mmHg at 25°C |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 9.97±0.70(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
| Refractive Index | 1.543 |
| In vitro study | Pimecrolimus blocks the T-lymphocyte activation pathway by inhibiting phosphatase function. Pimecrolimus prevents the release of cytokines and pro-inflammatory mediators from mast cells. Pimecrolimus binds to macrophilin-12 to form a pimecrolimus-macrophilin complex, which then binds to the cytosolic enzyme calcineurin. The Pimecrolimus-macrophilin complex prevents dephosphorylation of cytoplasmic components of nuclear factor in activated T cells by inhibiting the action of calcineurin. Pimecrolimus not only inhibits the transcription and synthesis of cytokines in mast cells, the release of preformed mediators serotonin and β-hexosaminidase is also inhibited by inhibition of Fc ∈-RI-mediated degranulation and secretion. Pimecrolimus treatment caused a strong down-regulation of mRNA expression of genes associated with macrolactam target pathways and inflammation. |
| In vivo study | In mice, Pimecrolimus was as effective as cyclosporine A after oral administration and slightly more effective than cyclosporine A after subcutaneous injection. In mice with allergic contact dermatitis, Pimecrolimus, in contrast to cyclosporine A and tacrolimus, continuously suppressed the secondary inflammatory response, but did not impair the primary immune response. In the allergic contact dermatitis (ACD) pig model, Pimecrolimus is as effective as the potent corticosteroid chlorbetasol -17-propionate. Pimecrolimus also effectively reduced skin inflammation and itching in low-magnesium Hairless rats, a model that mimics the signals of acute atopic dermatitis. In (1) local graft-versus-host reaction,(2) antibody formation with sheep red blood cells, and (3) kidney-transplanted rats, compared with tacrolimus, pimecrolimus showed only a low potential to attenuate the systemic immune response. |
ASM 981 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.234 ml | 6.169 ml | 12.339 ml |
| 5 mM | 0.247 ml | 1.234 ml | 2.468 ml |
| 10 mM | 0.123 ml | 0.617 ml | 1.234 ml |
| 5 mM | 0.025 ml | 0.123 ml | 0.247 ml |
Last Update：2024-01-02 23:10:35
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CAS: 137071-32-0
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