Name: Cyclosporine
Brand: Selleck Chemicals
SKU: S1514
Rating: 5 (14 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.92%

99.92

Gerelateerde doelwitten	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Overig phosphatase Inhibitoren	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 GSK2830371 Batoprotafib (TNO155) β-Glycerophosphate sodium salt hydrate NSC87877 TPI-1 Suramin sodium salt

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	1202.61	Formule	C₆₂H₁₁₁N₁₁O₁₂	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	79217-60-0	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (83.15 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.000mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	calcineurin phosphatase
In vitro	Cyclosporine induces phenotypic changes, including invasiveness of non-transformed cells, by a cell-autonomous mechanism. This compound's treatment of adenocarcinoma cells results in striking morphological alterations, including membrane ruffling and numerous pseudopodial protrusions, increased cell motility, and anchorage-independent (invasive) growth. It has potent immunosuppressive properties, reflecting its ability to block the transcription of cytokine genes in activated T cells. This chemical, through formation of a complex with cyclophilin, inhibits the phosphatase activity of calcineurin, which regulates nuclear translocation and subsequent activation of NFAT transcription factors. It also blocks the activation of JNK and p38 signaling pathways triggered by antigen recognition, making CsA a highly specific inhibitor of T cell activation. Its-mediated inhibition of the biliary excretion of MPAG by the Mrp2 transporter is the mechanism responsible for the interaction between this compound and mycophenolate mofetil (MMF). It inhibits biochemical and morphological differentiation of skeletal muscle cells while having a minimal effect on proliferation.
In vivo	Cyclosporine enhances tumour growth in immunodeficient SCID-beige mice. This compound inhibits muscle regeneration after induced trauma in mice. It peaks at 1 hour in blood, spleen, and kidney, with higher concentrations in spleen and kidney than in blood.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10028970/ [2] https://pubmed.ncbi.nlm.nih.gov/10878286/ [3] https://pubmed.ncbi.nlm.nih.gov/15816878/ [4] https://pubmed.ncbi.nlm.nih.gov/9763451/ [5] https://pubmed.ncbi.nlm.nih.gov/10573076/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT05702931	Not yet recruiting	Hyperglycemia\|Renal Transplant Complication Primary Non-Function\|Diabetes	Rigshospitalet Denmark\|Aarhus University Hospital\|Odense University Hospital	April 1 2024	Phase 4
NCT05955924	Recruiting	Non-melanoma Skin Cancer\|Carcinoma Squamous Cell\|Carcinoma Basal Cell\|Keratinocyte Carcinoma	Women''s College Hospital\|Canadian Institutes of Health Research (CIHR)\|University Health Network Toronto\|NOW Foods	August 28 2023	Phase 3
NCT04989686	Recruiting	Immunosuppression	Children''s Hospital of Philadelphia\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	June 8 2023	--
NCT05745701	Completed	Healthy	Pfizer	February 22 2023	Phase 1
NCT05056779	Withdrawn	Moderate-to-severe Atopic Dermatitis	Galderma R&D	January 2023	Phase 3

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
What is the difference between S2286 (it) and S1514 (this compound)?

Antwoord:
It is a mixture of Cyclosporine A, derivatives of Cyclosporine A, and salts of Cyclosporine A. Cyclosporine A is an especially useful component of this compound.

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Cyclosporine phosphatase Remmer

Molecuulgewicht: 1202.61