Pimecrolimus

SKU: orb1305220

Description

Pimecrolimus (SDZ-ASM 981) is a calcineurin inhibitor that forms a complex with FKBP-12, blocking calcineurin-mediated calcium signaling. This immunosuppressant is widely used in research for studying T-cell activation and has applications in both in vitro assays and in vivo models of inflammatory skin diseases.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 137071-32-0
• MW: 810.45
• Purity: 98.64% (May vary between batches)
• Formula: C₄₃H₆₈ClNO₁₁
• 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
• Target: Phosphatase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:93 mg/mL (114.75 mM);DMSO:93 mg/mL (114.75 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.07 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

orally active, oral erosive lichen planus, inhibit, inflammatory skin diseases, mast cells, Inhibitor, cytosolic receptor, ASM981, ASM-981, ASM 981, atopic dermatitis, anti-inflammatory, T-cells, Pimecrolimus, Phosphatase, SDZ-ASM 981, SDZ-ASM981, SDZ-ASM-981

Compound Identifiers

PubChem CID

6509979