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

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.92%

99.92

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

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	1202.61	Formule	C₆₂H₁₁₁N₁₁O₁₂	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	79217-60-0	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant

Solubilité (Solubility)

In vitro
Lot:

DMSO : 100 mg/mL (83.15 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 100 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (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.
Références	[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/

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
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

Foire aux questions (Frequently Asked Questions)

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

Réponse :
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Cyclosporine phosphatase Inhibiteur

Poids moléculaire: 1202.61