Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Pimecrolimus (formerly known as ASM-981; SDZ-ASM981) is an ascomycin analog which acts as an immunomodulating agent and is used in the treatment of atopic dermatitis. As a potent immunophilin ligand, it binds specifically to the cytosolic receptor, immunophilin macrophilin-12. It is an immunomodulating agent used in the treatment of atopic dermatitis (eczema). Pimecrolimus is a cell-selective inflammatory cytokines secretion inhibitor. Pimecrolimus inhibited the secretion of inflammatory cytokines in mast cells and T cells and also inhibited the release of preformed inflammatory mediators from mast cells. Pimecrolimus exhibited a low potential to impair systemic immune reactions in the skin. In peripheral blood leukocytes contained basophil or mast cells, pimecrolimus inhibited histamine release induced by anti-IgE from basophils and mast cells by 82% and 73%, respectively.
ln Vitro |
Pimecrolimus (SDZ-ASM 981) (100 nM) selectively acts on cells that are essential for the effector phase of an inflammatory reaction, specifically targeting T-cells and mast cells. It inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals necessary for the activation of inflammatory T-lymphocytes[1]. In both murine and human mixed lymphocyte reactions, cipecrolimus (10 nM; 3 days) reduces the polyclonal development of peripheral blood T cells[2]. after antigen-specific stimulation, inhibits the production of cytokines IL-2, IL-4, IL-10, and interferon-γ from T-cell clone CFTS4:3.1 with IC50s of 0.28, 0.3, 0.2, and 0.42 nM, respectively[2].
|
---|---|
ln Vivo |
In mice and pigs, pimecrolimus (SDZ-ASM 981) (0-0.4%; topical; 10 μL once) prevents allergic contact dermatitis[3]. In mice and rats, dipecrolimus (0-90 mg/kg; po or sc; twice or once) significantly reduces allergic contact dermatitis[3].
|
Cell Assay |
Cell Proliferation Assay[2]
Cell Types: T-cell clone (TCC), murine and human mixed lymphocyte reactions (MLR) Tested Concentrations: 0-10 nM Incubation Duration: 3 days Experimental Results: Inhibited proliferation of TCC CFTS 4:3.1 with IC50s of 0.78- 2.6 nM. Inhibited murine and human MLR with IC50s of both 1.3 nM. |
Animal Protocol |
Animal/Disease Models: Female NMRl mice, allergic contact dermatitis model[3]
Doses: 0.004%, 0.01%, 0.04%, 0.13% and 0.4% in10 μL ethanolic solution Route of Administration: Topical application, once Experimental Results: Inhibited oedema formation by 17% at concentration of 0.004%. Animal/Disease Models: Female NMRl mice, allergic contact dermatitis model[3] Doses: 10, 30, 90 mg/kg (oral) or 1.5, 4.5, 13.5 mg/ kg (subcutaneous) Route of Administration: Oral (twice) or subcutaneous (sc) administration (once) Experimental Results: Signiticantiy inhibited inflammatory ear oedema formation. |
References |
[1]. Grassberger M, et al. Pimecrolimus -- an anti-inflammatory drug targeting the skin. Exp Dermatol. 2004 Dec;13(12):721-30.
[2]. Grassberger M, et al. A novel anti-inflammatory drug, SDZ ASM 981, for the treatment of skin diseases: in vitro pharmacology. Br J Dermatol. 1999 Aug;141(2):264-73. [3]. Meingassner JG, et al. A novel anti-inflammatory drug, SDZ ASM 981, for the topical and oral treatment of skin diseases: in vivo pharmacology. Br J Dermatol. 1997 Oct;137(4):568-76. |
Molecular Formula |
C43H68CLNO11
|
---|---|
Molecular Weight |
810.45
|
CAS # |
137071-32-0
|
Related CAS # |
Pimecrolimus hydrate;1000802-56-1
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=C(C(N1CCCC[C@@]1([H])C(O[C@H](/C(C)=C/[C@H]2C[C@@H](OC)[C@@H](Cl)CC2)[C@H](C)[C@@H](O)C3)=O)=O)[C@@](O4)(O)[C@H](C)C[C@H](OC)[C@@]4([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@@H](CC)C3=O
|
Synonyms |
SDZ ASM 981; ASM-981; SDZ-ASM 981; ASM 981; SDZ-ASM-981; ASM981; ASM 981; Pimecrolimus; Pimecrolimusum; 33-epi-Chloro-33-desoxyascomycin; Brand name: Aregen; Rizan; Elidel.
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2339 mL | 6.1694 mL | 12.3388 mL | |
5 mM | 0.2468 mL | 1.2339 mL | 2.4678 mL | |
10 mM | 0.1234 mL | 0.6169 mL | 1.2339 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.