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Pimecrolimus (SDZ-ASM 981), a calcineurin inhibitor immunosuppressant, binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $31 | In Stock | |
25 mg | $48 | In Stock | |
50 mg | $70 | In Stock | |
100 mg | $98 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
Description | Pimecrolimus (SDZ-ASM 981), a calcineurin inhibitor immunosuppressant, binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. |
In vitro | Pimecrolimus effectively alleviates allergic symptoms in a variety of (allergic) animals. Within the context of both the acute allergic dermatitis low-magnesium hairless rat model and the moderate allergic contact dermatitis mouse model, Pimecrolimus inhibits inflammatory responses and pruritic (itching) symptoms. |
In vivo | In mast cells, Pimecrolimus inhibits the transcription and synthesis of cytokines, while simultaneously promoting the release of 5-hydroxytryptamine and β-hexosaminidase. In T lymphocytes, Pimecrolimus suppresses activation by inhibiting phosphatase activity, thereby blocking T-cell activation. |
Alias | SDZ-ASM 981, ASM 981 |
Molecular Weight | 810.45 |
Formula | C43H68ClNO11 |
Cas No. | 137071-32-0 |
Smiles | [H][C@]12O[C@](O)([C@H](C)C[C@@H]1OC)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@]([H])([C@H](C)[C@@H](O)CC(=O)[C@H](CC)\C=C(C)\C[C@H](C)C[C@@H]2OC)C(\C)=C\[C@@H]1CC[C@H](Cl)[C@@H](C1)OC |
Relative Density. | 1.19 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 93 mg/mL (114.8 mM) DMSO: 93 mg/mL (114.8 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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