alleen voor onderzoeksdoeleinden

ISX-9 (Isoxazole 9) Inductor van neurale stamceldifferentiatie

Name: ISX-9 (Isoxazole 9)
Brand: Selleck Chemicals
SKU: S7914
Rating: 5 (8 reviews)

Cat.nr.S7914

ISX-9 (Isoxazole 9) is een synthetische promotor van volwassen neurogenese door neuronale differentiatie van volwassen neurale stam-/voorlopercellen (NSPC's) te stimuleren. ISX-9 (Isoxazole 9) activeert meerdere routes, waaronder TGF-β-geïnduceerde epitheliale-mesenchymale transitie (EMT)-signalering, canonieke en niet-canonieke Wnt-signalering in verschillende stadia van cardiale differentiatie.

ISX-9 (Isoxazole 9) Activator Chemical Structure

Chemische structuur

Molecuulgewicht: 234.27

Spring naar

Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.87%

99.87

Gerelateerde doelwitten	JAK TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT
Overig Inhibitoren	Concanamycin A YAP-TEAD Inhibitor 1 (Peptide 17) L-Buthionine-(S,R)-sulfoximine (L-BSO) PF-3644022 NSC 23766 GW3965 WAY-641966 WAY-320461 Vaborbactam Maribavir

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

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HCN	Function assay			Induction of NMDA receptor-mediated Ca2+ influx in rat HCN cells in presence of NMDA receptor antagonist MK801	18552832
HCN	Function assay	5 uM		Induction of L-type calcium channel/NMDA receptor-mediated Ca2+ influx in rat HCN cells at 5 uM by Fura-2 imaging analysis in presence of multiple of inhibitors	18552832
HCN	Function assay	50 uM	3 hrs	Induction of NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 3 hrs by RT-PCR analysis in presence of NMDA receptor antagonist MK801	18552832
HCN	Function assay	25 uM	4 days	Inhibition of gliogenesis differentiation in rat HCN cells at 25 uM after 4 days	18552832
HCN	Function assay	5 uM		Induction of L-type calcium channel/NMDA receptor-mediated Ca2+ influx in rat HCN cells at 5 uM by Fura-2 imaging analysis	18552832
HCN	Function assay	5 uM		Induction of NMDA receptor-mediated Ca2+ influx in rat HCN cells at 5 uM by Fura-2 imaging analysis in presence of NMDA receptor antagonist MK801	18552832
HCN	Function assay	50 uM	3 hrs	Induction of L-type calcium channel/NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 3 hrs by RT-PCR analysis in presence of multiple inhibitors	18552832
HCN	Function assay			Induction of L-type calcium channel/NMDA receptor-mediated Ca2+ influx in rat HCN cells	18552832
HCN	Function assay			Induction of L-type calcium channel/NMDA receptor-mediated Ca2+ influx in rat HCN cells in presence multiple inhibitors	18552832
HCN	Function assay	50 uM	24 hrs	Induction of NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 24 hrs by RT-PCR analysis in presence of NMDA receptor antagonist MK801	18552832
HCN	Function assay	50 uM	24 hrs	Induction of NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 24 hrs by RT-PCR analysis in presence of NMDA receptor antagonist nifedipine	18552832
HCN	Function assay	50 uM	24 hrs	Induction of L-type calcium channel/NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 24 hrs by RT-PCR analysis in presence of multiple inhibitors	18552832
HCN	Function assay	8 to 64 uM	9 hrs	Induction of neurogenesis in undifferentiated rat HCN cells assessed as MAP2AB protein level at 8 to 64 uM after 9 hrs by protein blotting analysis	18552832
HCN	Function assay			Induction of HDAC5 translocation in cytoplasm of rat HCN cells assessed as phosphorylated HDAC5 accumulation	18552832
HCN	Function assay			Induction of CAMK-mediated MREx3 activity in rat HCN cells by luciferase reporter gene assay in presence of 2.5 uM potassium channel inhibitor KN92	18552832
HCN	Function assay	8 to 64 uM	9 hrs	Induction of neurogenesis in undifferentiated rat HCN cells assessed as GlR2/3 protein level at 8 to 64 uM after 9 hrs by protein blotting analysis	18552832
HCN	Function assay		6 hrs	Induction of HDAC5 phosphorylation in rat HCN cells after 6 hrs	18552832
HCN	Function assay		24 hrs	Induction of HDAC5 phosphorylation in rat HCN cells after 24 hrs	18552832
HCN	Function assay			Induction of HDAC5 translocation in nucleus of rat HCN cells assessed as phosphorylated HDAC5 accumulation	18552832
HCN	Function assay	5 uM		Induction of HDAC5 translocation in nucleus of rat HCN cells assessed as GFP-HDAC5 S258A S498A mutant fusion protein accumulation at 5 uM by fluorescence assay	18552832
HCN	Function assay	50 uM	3 hrs	Induction of NMDA receptor-mediated neuroD gene expression in rat HCN cells at 50 uM after 3 hrs by RT-PCR analysis in presence of NMDA receptor antagonist nifedipine	18552832
HCN	Function assay	20 uM		Induction of HDAC5 translocation in nucleus of rat HCN cells assessed as GFP-HDAC5 fusion protein accumulation at 20 uM by fluorescence assay	18552832
HCN	Function assay			Induction of CAMK-mediated MREx3 activity in rat HCN cells by luciferase reporter gene assay in presence of 200 nM PKC inhibitor Go6976	18552832
HCN	Function assay		24 hrs	Induction of L-type calcium channel-mediated neuroD gene expression in rat HCN cells after 24 hrs by luciferase reporter gene assay in presence of multiple inhibitors	18552832
HCN	Function assay		24 hrs	Induction of L-type calcium channel-mediated neuroD gene expression in rat HCN cells after 24 hrs by luciferase reporter gene assay in presence of NMDA receptor antagonist MK801	18552832
HCN	Function assay		24 hrs	Induction of L-type calcium channel-mediated neuroD gene expression in rat HCN cells after 24 hrs by luciferase reporter gene assay in presence of NMDA receptor antagonist nifedipine	18552832
Klik om meer experimentele gegevens over cellijnen te bekijken

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

Molecuulgewicht	234.27	Formule	C₁₁H₁₀N₂O₂S	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	832115-62-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	N/A			Smiles	C1CC1NC(=O)C2=NOC(=C2)C3=CC=CS3

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 47 mg/mL (200.62 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 12 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	5%DMSO 1 55%PEG300 2 40%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	10.000mg/ml (42.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 550 μL of PEG 300, mix evenly to clarify it; then continue to add 400 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	ISX-9 (Isoxazole 9) verhoogt het aantal cellen en bevordert celdifferentiatie in NSPC's, terwijl het celbeschadiging induceert in OPC's. In uitgroei-EPC's vermindert deze verbinding de buisvorming zonder effect op vroege EPC's.
In vivo	Bij muizen passeert ISX-9 (Isoxazole 9) (20 mg/kg, i.p.) de BBB en verhoogt het de proliferatie van neuroblasten en neurogenese via Mef2-specifieke mechanismen in de hippocampale SGZ. Deze verbinding verhoogt ook de differentiatie en dendritische complexiteit van onrijpe neuronen en verbetert het geheugen. In MWM verbetert het het ruimtelijk geheugen.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/26407349/ [2] https://pubmed.ncbi.nlm.nih.gov/22542682/

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):