Name: Tranilast
Brand: Selleck Chemicals
SKU: S1439
Rating: 5 (17 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.97%

99.97

Gerelateerde doelwitten	PD-1/PD-L1 CXCR STING AhR CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor
Overig Immunology & Inflammation related Inhibitoren	Cl-amidine Bestatin (Ubenimex) Bindarit (AF 2838) Tempol Sinomenine GI254023X (GI4023) Geniposidic acid CORM-3 Oxymatrine Germacrone

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Activiteitsbeschrijving	PMID
ECs	Function assay	Evaluated for inhibition of proliferation of human coronary artery endothelial cells (ECs), induced by 5 % FBS., IC50 = 19.1 μM.	11229768
SMCs	Function assay	Inhibition of human coronary artery smooth muscle cells (SMC's) proliferation, induced by platelet-derived growth factor (PDGF-BB) 20 ng mL., IC50 = 24.5 μM.	11229768
Klik om meer experimentele gegevens over cellijnen te bekijken

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

Molecuulgewicht	327.33	Formule	C₁₈H₁₇NO₅	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	53902-12-8	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	SB 252218, MK-341			Smiles	COC1=C(C=C(C=C1)C=CC(=O)NC2=CC=CC=C2C(=O)O)OC

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 65 mg/mL (198.57 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : 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	5%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.500mg/ml (10.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	7.000mg/ml (21.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 140 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 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)

In vitro	Tranilast is an anti-allergic drug inhibiting the release of substances such as histamine and prostaglandins from mast cells, which suppresses collagen synthesis of fibroblasts derived from keloid tissues. This compound (3-300 mM) suppresses the collagen synthesis of fibroblasts from keloid and hypertrophic scar tissue but not healthy skin fibroblasts. It (30-300 mM) inhibits the release of transforming growth factor (TGF)-beta 1 from keloid fibroblasts, which enhances the collagen synthesis of keloid fibroblasts. This drug improves keloids and hypertrophic scars which originate from the abnormal proliferation and excessive collagen accumulation of fibroblasts. It inhibits the release of TGF-beta 1, IL-1 beta and PGE2 from the human monocytes-macrophages. This chemical inhibits the proliferation stimulated with fetal bovine serum (FBS), TGF-beta 1 and platelet-derived growth factor-BB (PDGF-BB) as well as PDGF-BB-induced migration. It exhibits inhibitory effects on spontaneous collagen synthesis and TGF-beta 1-induced collagen and glycosaminoglycan synthesis.
In vivo	Tranilast results in a 58% reduction in TGF-beta1-induced 3[H]-hydroxyproline incorporation in the diabetic heart of rats. This compound attenuates cardiac fibrosis by 37% in association with reduction in phospho-Smad2 in the diabetic heart of rats. It completely prevents the increase in chymaselike activity, reduces the chymase mRNA levels by 43%, and decreases the carotid intima/media ratio by 63% in the carotid artery of dogs.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/1282576/ [2] https://pubmed.ncbi.nlm.nih.gov/1282575/ [3] https://pubmed.ncbi.nlm.nih.gov/8770315/ [4] https://pubmed.ncbi.nlm.nih.gov/15664396/ [5] https://pubmed.ncbi.nlm.nih.gov/10051304/

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
NCT05626829	Recruiting	Nasopharyngeal Carcinoma\|Recurrent Cancer	Jian Guan\|Nanfang Hospital Southern Medical University	July 20 2022	Phase 2
NCT00882024	Completed	Active Rheumatoid Arthritis	Nuon Therapeutics Inc.	March 2009	Phase 2
NCT01003613	Completed	Pterygium	Gildasio Castello de Almeida Junior\|Hospital de Base\|Sao Jose do Rio Preto Medical School	February 2009	Phase 3
NCT00717808	Withdrawn	Rheumatoid Arthritis	Imperial College London\|Nuon Therapeutics Inc.	September 2008	Phase 1

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Tranilast Immunology & Inflammation related chemical

Chemische structuur

Molecuulgewicht: 327.33

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Tranilast Immunology & Inflammation related chemical

Chemische structuur

Molecuulgewicht: 327.33

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)