cyclosporine

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1).

Cyclosporin A-BSA is a hapten-carrier protein conjugate formed by coupling Cyclosporin A to bovine serum albumin (BSA). As a hapten, Cyclosporin A alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Cyclosporin A-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M PBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

Cyclosporin E (11-Demethylcyclosporin A) is a cyclic oligopeptide isolated from imperfect fungi such as Trichoderma polysporum and is a member of the Cyclosporins family. It is valuable for investigating the structure-activity relationships and molecular dynamics of cyclosporin compounds. Cyclosporin E serves as a structural reference compound with significant research importance in medicinal chemistry and biophysics.

ZX-J-19J (N-(2,3-Diphenyl-6-quinoxalinyl)octanamide), an inhibitor of Cyclophilin J (CyPJ), demonstrates remarkable inhibition of tumor cell growth, comparable to cyclosporine A but much stronger than 5-fluorouracil.

Mocravimod is an agonist of sphingosine 1-phosphate receptor type 1. Mocravimod ameliorates atherosclerosis in LDL-R-/- mice. KRP-203 attenuates rat autoimmune myocarditis. KRP-203 combined with cyclosporine prolonged graft survival and abrogated transpla

Gusperimus was synthesized by chemical modification of spergualin and in combination with cyclosporine A to prevent diabetes in susceptible NOD mice.

UNIL088 is a water-soluble prodrug of cyclosporine A (CsA) designed for topical ocular delivery. The pro-moiety is grafted via an ester function to CsA and the solubilizing group is a phosphate ion. UNIL-088 can be rapidly hydrolysed under physiological c

Oxeclosporin is a hydroxyethyl derivative of serine(8)-cyclosporine; inhibits proliferation and functions of lymphocytes.

Cyclosporin A-D4 is a deuterated form of Cyclosporin A. Cyclosporin A (Cyclosporine A) functions as an immunosuppressant by binding to cyclophilin and inhibiting calcineurin activity with an IC50 value of 7 nM. It also obstructs the adhesion molecules CD11a/CD18.

Cyclosporin A acetate-D4 is a deuterium-labeled form of Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressive agent that binds to cyclophilin, inhibiting the activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 value of 7 nM. Additionally, Cyclosporin A impedes the adhesion molecules CD11a/CD18.

Cyclosporin A-D12 is a deuterium-labeled form of Cyclosporin A. Cyclosporin A (T0945) (Cyclosporine A) functions as an immunosuppressant by binding to cyclophilin and inhibiting protein phosphatase 2B (PP2B/calcineurin) with an IC50 value of 7 nM. It also inhibits the adhesion molecule CD11a/CD18.

Cyclosporin A-D4 (Major) is a deuterated compound of Cyclosporin A. Cyclosporin A (T0945) has a CAS number of 59865-13-3. Cyclosporine A is a Calcineurin Inhibitor Immunosuppressant. The mechanism of action of cyclosporine is as a Calcineurin Inhibitor, and Cytochrome P450 3A4 Inhibitor, and P-Glycoprotein Inhibitor.

2-[O-(2-Azidoethyl)-D-serine]-cyclosporin A (Compound 33) is a derivative of Cyclosporine. This compound exhibits an IC50 of 0.11 μg/mL in mixed lymphocyte reaction assays.

NSP-DMAE-HEG-Giu-NHS (Fig.18) is an activated labeling reagent containing acridinium ester and is a crucial component of the Cyclosporine A tracer.