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

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Control de calidad (Quality Control)

Lote: Pureza: 99.98%

99.98

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

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	122.12	Fórmula	C₆H₆N₂O	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	98-92-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452,NSC 13128			Smiles	C1=CC(=CN=C1)C(=O)N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 24 mg/mL (196.52 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 24 mg/mL

Ethanol : 24 mg/mL

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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%.
Referencias	[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/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	Sp1 / ERK p-β-catenin / β-catenin p-MLC / MLC / p-MYPT1 / MYPT1		18446063
Immunofluorescence	p-MLC		30503259

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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 Inhibidor

Peso molecular: 122.12

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

Nicotinamide (Niacinamide) Sirtuin Inhibidor

Peso molecular: 122.12

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)