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Pimecrolimus (Synonyms: Elidel, SDZASM 981)

Catalog No.GC10825

inhibitor of inflammatory cytokines secretion, cell-selective

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Pimecrolimus Chemical Structure

Cas No.: 137071-32-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$94.00
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10mg
$54.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

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Background

Pimecrolimus is a cell-selective inhibitor of inflammatory cytokines secretion in T cells and mast cells [1].

Inflammatory cytokines are cytokines which promote systemic inflammation. Pimecrolimus can be used for the treatment of inflammatory skin diseases, such as plaque-type psoriasis, atopic dermatitis, irritant contact dermatitis and allergic contact dermatitis [1].

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 [1]. 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. Also, pimecrolimus inhibited tryptase, LTC4 and TNF-alpha release [2]. In CD4+ T cells stimulated by dendritic cells (DC), pimecrolimus inhibited the up-regulation of CD25 and CD54 and surface expression of OX40. Pimecrolimus inhibited T cell proliferation with IC50 value of 0.55 nM and inhibited the synthesis of IFN-γ and TNF-α [3].

In treatment of allergic contact dermatitis (ACD) mice and rats, pimecrolimus exhibited a higher potency. In atopic dermatitis rats, pimecrolimus effectively reduced pruritus and skin inflammation [1].

References:
[1].  Stuetz A, Grassberger M, Meingassner JG. Pimecrolimus (Elidel, SDZ ASM 981)--preclinical pharmacologic profile and skin selectivity. Semin Cutan Med Surg, 2001, 20(4): 233-241.
[2].  Zuberbier T, Chong SU, Grunow K, et al. The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils. J Allergy Clin Immunol, 2001, 108(2): 275-280.
[3].  Kalthoff FS, Chung J, Stuetz A. Pimecrolimus inhibits up-regulation of OX40 and synthesis of inflammatory cytokines upon secondary T cell activation by allogeneic dendritic cells. Clin Exp Immunol, 2002, 130(1): 85-92.

Chemical Properties

Cas No. 137071-32-0 SDF
Synonyms Elidel, SDZASM 981
Canonical SMILES CO[C@@H]1C[C@H](/C=C(C)/[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@H]([C@@H](OC)C[C@H](C/C(C)=C/4)C)[C@@H](OC)C[C@H]3C)=O)=O)=O)[C@H](C)[C@H](CC([C@@H]4CC)=O)O)CC[C@@H]1Cl
Formula C43H68ClNO11 M.Wt 810.45
Solubility ≥ 32.05mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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