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Nicotinamide (Vitamin B3)

Catalog No.GN10347

Nicotinamide (Vitamin B3) Chemical Structure

PARP-1 inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$35.00
In stock
500mg
$25.00
In stock
1g
$32.00
In stock
5g
$46.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

DM is induced via a single intraperitoneal (i.p) injection of nicotinamide (110 mg/kg/body weight) dissolved in normal saline 15 min prior to streptozotocin (STZ) (55 mg/kg/body weight) injection, which is dissolved in a freshly prepared 0.1mol/Lcitrate buffer (pH 4.5). These injections are given following an overnight fast. Control rats (n=6) are injected with the same amount of solvent. In order to prevent hypoglycemia in the first 24 h following STZ injection, rats are allowed to have free access to water with 5% dextrose (D5W). Three days after STZ-nicotinamide injection, rats with FBG levels greater than 7.0 mM are considered as diabetic.

References:

[1]. Bhansali SG, et al. Nicotinamide prevents apoptosis in human cortical neuronal cells. Toxicol Mech Methods. 2006;16(4):173-80.
[2]. Roslan J, et al. Quercetin ameliorates oxidative stress, inflammation and apoptosis in the heart of streptozotocin-nicotinamide-induced adult male diabetic rats. Biomed Pharmacother. 2016 Dec 24;86:570-582
[3]. Fushima T, et al. Nicotinamide ameliorates a preeclampsia-like condition in mice with reduced uterine perfusion pressure. Am J Physiol Renal Physiol. 2016 Dec 7:ajprenal.00501.2016
[4]. Suzuki E, et al. Protective effect of nicotinamide against poly(ADP-ribose) polymerase-1-mediated astrocyte death depends on its transporter-mediated uptake. Life Sci. 2010 Apr 24;86(17-18):676-82.
[5]. Peck B, et al. SIRT inhibitors induce cell death and p53 acetylation through targeting both SIRT1 and SIRT2. Mol Cancer Ther. 2010 Apr;9(4):844-55.

Background

IC50: N/A

Nicotinamide is an inhibitor of poly(ADP-ribose) polymerase (PARP-1) enzymes. Poly(ADP-ribose) polymerase-1 (PARP-1) is found as a DNA repair enzyme. The excessive activation of PARP-1, such as ischemia and trauma, can deplete cellular nicotinamide adenine dinucleotide as a substrate and leads to brain cell death eventually.

In vitro: Previous findings suggested that nicotinamide had a protective effect against PARP-1-induced astrocyte death. The transporter-mediated uptake of nicotinamide, which was extracellular pH-sensitive and common to N-methylnicotinamide, was found to be critical for prevention of PARP-1-triggered cell death [1].

In vivo: Type 2 diabetes was induced in Wistar rats by streptozotocin followed by nicotinamide. Test compounds and standard treatment were continued for 15 days. Results showed that there was significant normalisation of liver antioxidant enzymes compared to diabetic rats, suggesting all the tested compounds were beneficial in reducing oxidative stress [2].

Clinical trial: Previous clinical trials showed nicotinamide was well tolerated. Phase 1 showed a dose-response relation for proportional change in frataxin protein concentration. Phases 2 and 3 showed daily dosing resulted in a sustained and significant upregulation of frataxin expression [3].

References:
[1] Suzuki E,Okuda H,Nishida K,Fujimoto S,Nagasawa K.  Protective effect of nicotinamide against poly(ADP-ribose) polymerase-1-mediated astrocyte death depends on its transporter-mediated uptake. Life Sci.2010 Apr 24;86(17-18):676-82.
[2] Yogendra Nayak, Venkatachalam Hillemane,Vijay Kumar Daroji,B.  S. Jayashree,andM. K. Unnikrishnan. Antidiabetic Activity of Benzopyrone Analogues in Nicotinamide-Streptozotocin Induced Type 2 Diabetes in Rats. Scientific World Journal. 2014; 2014: 854267.
[3] Libri V,Yandim C,Athanasopoulos S,Loyse N,Natisvili T,Law PP,Chan PK,Mohammad T,Mauri M,Tam KT,Leiper J,Piper S,Ramesh A,Parkinson MH,Huson L,Giunti P,Festenstein R.  Epigenetic and neurological effects and safety of high-dose nicotinamide in patients with Friedreich's ataxia: an exploratory, open-label, dose-escalation study. Lancet.2014 Aug 9;384(9942):504-13.

Chemical Properties

Cas No. 98-92-0 SDF
Synonyms N/A
Chemical Name pyridine-3-carboxamide
Canonical SMILES C1=CC(=CN=C1)C(=O)N
Formula C6H6N2O M.Wt 122.13
Solubility DMF: 15 mg/ml,DMSO: 15 mg/ml,Ethanol: 2.5 mg/ml,PBS (pH 7.2): 10 mg/ml Storage 4°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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