Name: Nicotinamide (Niacinamide)
Brand: Selleck Chemicals
SKU: S1899
Rating: 5 (48 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.98%

99.98

Relaterade mål	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Casein Kinase eIF
Övrigt Sirtuin Inhibitorer	SRT 1720 Hydrochloride Selisistat (EX-527) Sirtinol Fisetin 3-TYP AGK2 SRT2104 (GSK2245840) OSS_128167 SirReal2 SRT2183

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning	PMID
BL21 (DE3)	Function assay			Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=6.2μM.	25275824
BL21 (DE3)	Function assay			Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=10.5μM.	25275824
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of substrate deacetylation using ZMAL as substrate, IC50=23.1μM.	31496251
SK-MEL-28	Function assay	100 uM	24 hrs	Reduction in ATP level in human SK-MEL-28 cells at 100 uM maintained in Locke's solution after 24 hrs by luciferase-based assay in absence of GF and glucose	22835719
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of ZMAL	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(But)Lys-AMC	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Hex)Lys-AMC	31496251
BL21(DE3)	Function assay			Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Oct)Lys-AMC	31496251
HEK293T	Function assay		60 mins	Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in HEK293T cells assessed as reduction in NADase activity in presence of NAD+ incubated for 60 mins by HPLC analysis, IC50=43.8μM.	ChEMBL
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	122.12	Formel	C₆H₆N₂O	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	98-92-0	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452,NSC 13128			Smiles	C1=CC(=CN=C1)C(=O)N

Löslighet (Solubility)

In vitro
Batch:

DMSO : 24 mg/mL (196.52 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : 24 mg/mL

Ethanol : 24 mg/mL

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 40%PEG300 2 5%Tween80 3 50%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	1.200mg/ml (9.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 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 make it clear; 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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	Sirtuin
In vitro	Nicotinamide strongly inhibits yeast silencing, increases rDNA recombination, and shortens replicative life span to that of a sir2 mutant. This compound abolishes silencing and leads to an eventual delocalization of Sir2 even in G(1)-arrested cells, demonstrating that silent heterochromatin requires continual Sir2 activity. It results in a twofold increase in DNA content and a threefold increase in insulin content in the fetal cells. This chemical induces differentiation and maturation of human fetal pancreatic islet cells. It regulates sirtuins by switching between deacetylation and base exchange. This switching is quantitated for the Sir2s from Archeaglobus fulgidus (Sir2Af2), Saccharomyces cerevisiae (Sir2p), and mouse (Sir2alpha). The compound selectively reduces a specific phospho-species of tau (Thr231) that is associated with microtubule depolymerization in Alzheimer's disease transgenic mice, in a manner similar to inhibition of SirT1. It also dramatically increases acetylated alpha-tubulin, a primary substrate of SirT2, and MAP2c in Alzheimer's disease transgenic mice, both of which are linked to increased microtubule stability. This chemical fosters DNA integrity and maintains phosphatidylserine membrane asymmetry to prevent cellular inflammation, cellular phagocytosis and vascular thrombosis. It both prevents and reverses neuronal and vascular cell injury.
In vivo	In the mouse, nicotinamide given i.p. at doses of 100-500 mg/kg showed biphasic elimination with dose-dependent changes in half-life. The initial half-life increased significantly (P <0.05) from 0.8 to 2 h and the terminal half-life increased from 3.4 to 5.6 h over the dose range studied. Clearance, however, decreased significantly from 0.3 to 0.24 L/kg/h only at the highest dose. Peak concentrations increased in a dose-dependent manner from 1,000 to 4,800 nmol/ml. The bioavailability given via the i.p. as compared with the i. v. route was close to 100%.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/12297502/ [2] https://pubmed.ncbi.nlm.nih.gov/8104197/ [3] https://pubmed.ncbi.nlm.nih.gov/12899610/ [4] https://pubmed.ncbi.nlm.nih.gov/18987186/ [5] https://pubmed.ncbi.nlm.nih.gov/12767721/ [6] https://pubmed.ncbi.nlm.nih.gov/8070006/ [7] https://pubmed.ncbi.nlm.nih.gov/17997992/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	PMID
Western blot	Sp1 / ERK p-β-catenin / β-catenin p-MLC / MLC / p-MYPT1 / MYPT1		18446063
Immunofluorescence	p-MLC		30503259

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT06280482	Recruiting	Smooth Muscle Dysfunction Syndrome (SMDS)	The University of Texas Health Science Center Houston	March 6 2024	Phase 1
NCT05938036	Not yet recruiting	Acute Respiratory Distress Syndrome (ARDS)	Aqualung Therapeutics Corp.	January 14 2024	Phase 2
NCT06249581	Active not recruiting	Chronic Stable Angina	Auxilius Pharma sp.z.o.o.	November 27 2023	Early Phase 1
NCT06036355	Not yet recruiting	Postoperative Prevention of Tumor	Shanghai Cell Therapy Group Co.Ltd	September 30 2023	Early Phase 1

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):

Nicotinamide (Niacinamide) Sirtuin Hämmare

Molekylvikt: 122.12

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Nicotinamide (Niacinamide) Sirtuin Hämmare

Molekylvikt: 122.12

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)