Pimecrolimus

Description

What is Pimecrolimus?

Pimecrolimus is a 33-epi-chloro-derivative of the ascomycin macrolactam with immunosuppressant property. Pimecrolimus binds to the receptor macrophilin-12 (FKBP-12) forming a complex that blocks the calcium-dependent signal transduction cascade mediated by calcineurin. Via dephosphorylation, calcineurin is the enzyme responsible for activating nuclear factor of activated T-cells (NF-AT), a T cell transcriptional regulatory factor. As a consequence, the synthesis and release of Th1- (T helper 1) and Th2- (T helper 2) type cytokines, and other inflammatory mediators from T-cells and mast cells are blocked and the expression of signals essential for the activation of inflammatory T-lymphocytes is inhibited. However, pimecrolimus mode of action is cell-selective and does not affect Langerhans’ cells/dendritic cells and primary fibroblasts.

Basic Information

Product Name:	Pimecrolimus
Synonyms:	Pimecrolimus powder, Pimecrolimus INN, Pimecrolimus USAN, Pimecrolimus JAN
CAS:	137071-32-0
MF:	C43H68ClNO11
MW:	810.45
EINECS:	603-999-7
Product Categories:	Pharmaceutical raw materials;APIs;Biochemical Engineering

Chemical Structure

Pimecrolimus

Chemical Properties

Melting point	135-136 °C
Boiling point	866.1±75.0 °C(Predicted)
density	1.19
storage temp.	Keep in dark place,Sealed in dry,2-8°C
pka	9.97±0.70(Predicted)

Pimecrolimus Uses

Pimecrolimus is a topical immunomodulator. It is a semi-synthetic product of ascomycin produced by Streptomyces. It is more lipophilic than tacrolimus, has a stronger affinity with the skin, and can effectively and safely control facial fat The symptoms and signs of dermatitis can quickly relieve the itching symptoms of patients with dermatitis and eczema, reduce the area of skin lesions, and clear the signs of atopic dermatitis (eczema). It is an effective treatment method for early relief and long-term control of atopic dermatitis (eczema). Seborrheic dermatitis is an inflammatory immune response of the body to lipophilic Malassezia. Both humoral immunity and cellular immunity are involved in the pathogenesis. Pimecrolimus can inhibit the calcium dependence required to activate T cells. Sex nerve transcription protein selectively inhibits the activation of T cells, prevents the release of cytokines and pro-inflammatory mediators, and exhibits strong anti-inflammatory activity. Therefore, it is speculated that the mechanism of pimecrolimus in the treatment of seborrheic dermatitis is anti-inflammatory and immune regulation. There is no report that can directly participate in the antifungal effect. However, in recent years, there have been reports that tacrolimus (a kind of Immunomodulators with similar chemical structure and mechanism of action) have activity against certain Malassezia species.

Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

MSDS: MSDS available.

COA: COA can be available if you send us inquiry.

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