PIMECROLIMUS
Pimecrolimus is a topical calcineurin inhibitor that suppresses Tcell activation and inflammatory cytokine release. It is used for atopic dermatitis and inflammatory skin disorders. Benefits include targeted immune modulation without skin atrophy. Side effects include burning, redness, local irritation, and rare systemic immunosuppression, with caution advised in longterm use. Only GMP materials will be supplied, logistics all according to GDP.
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Product Description
Mechanism of Action
PIMECROLIMUS demonstrates a broad, multilayer biochemical activity profile affecting enzymedriven catalytic pathways, receptorregulated signalling systems, mitochondrial bioenergetics, redoxstate equilibrium, ionchannel behaviour, cytoskeletal integrity and transcriptionfactor regulatory networks. Its structural features indicate potential interactions with catalytic residues, allosteric protein domains, membranebound receptors and intracellular signalling intermediates, enabling influence over phosphorylation kinetics, Ca²⁺/cAMP/IP/DAGmediated secondmessenger systems, ATP turnover, ROS buffering and mitochondrial respiratorychain performance.
Depending on concentration and biological conditions, PIMECROLIMUS may modulate metabolic flux distribution, alter mitochondrial membrane potential, influence chromatin accessibility, impact vesicular trafficking dynamics and reshape geneexpression patterns relevant to survival, inflammation, apoptosis, autophagy, metabolic adaptation and redoxstress response.
Benefits and Advantages
This compound is widely used across advanced biochemical, pharmacological and mechanistic research domains, including:
- Receptorligand interaction studies and affinitymapping
- Enzymekinetic pathway deconstruction and catalyticdomain profiling
- Mitochondrialfunction analysis and ATPflux/oxidativestress modelling
- Multiomics integration (transcriptomics, metabolomics, proteomics, phosphoproteomics)
- Cytoskeletalstructure and membranedynamics research
- Autophagy, apoptosis, necroptosis and ferroptosis signalling investigations
- SAR (structureactivity relationship) profiling and compoundoptimisation workflows
- Pharmacodynamic modelling, thresholdactivation mapping and doseresponse scaling
Side Effects and Risks
Laboratoryobserved or predicted risks include:
- Oxidative imbalance and excessive ROS accumulation
- Mitochondrial overload or respiratorychain suppression
- Dysregulation of Na⁺/K⁺/Ca²⁺ ionchannel homeostasis
- Unintended receptor crosstalk or inhibitory interference
- Cytoskeletal destabilisation and membrane-integrity disruption
- Dosedependent cytotoxicity with apoptosis/autophagy activation
- Transcriptional instability or epigenetic disturbance
- Inflammatory signalling activation via NF-κB, MAPK or JNK pathways
Use strictly within controlled laboratory environments under appropriate biosafety protocols.
Only GMP materials will be supplied, logistics all according to GDP.
Datasheet
| Molecular Formula | C43H68ClNO11 |
|---|---|
| Molecular Weight | 810.4 g/mol |
| CAS Number | 137071-32-0 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance. |
| Purity | Purity information is available upon request (COA). |
| Synonym | Pimecrolimus; Elidel; 137071-32-0; SDZ-ASM 981; SDZ-ASM-981 |
| IUPAC/Chemical Name | (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone |
| InChl Key | KASDHRXLYQOAKZ-XDSKOBMDSA-N |
| InChl Code | InChI=1S/C43H68ClNO11/c1-10-30-18-24(2)17-25(3)19-36(53-8)39-37(54-9)21-27(5)43(51,56-39)40(48)41(49)45-16-12-11-13-32(45)42(50)55-38(28(6)33(46)23-34(30)47)26(4)20-29-14-15-31(44)35(22-29)52-7/h18,20,25,27-33,35-39,46,51H,10-17,19,21-23H2,1-9H3/b24-18+,26-20+/t25-,27+,28+,29-,30+,31-,32-,33-,35+,36-,37-,38+,39+,43+/m0/s1 |
| References |
3D Conformer.
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