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Nicaraven

CAS# 79455-30-4

Nicaraven

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Chemical Properties of Nicaraven

Cas No. 79455-30-4 SDF Download SDF
PubChem ID 71234 Appearance Powder
Formula C15H16N4O2 M.Wt 284.31
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (351.73 mM)
H2O : ≥ 50 mg/mL (175.86 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-(pyridine-3-carbonylamino)propyl]pyridine-3-carboxamide
SMILES CC(CNC(=O)C1=CN=CC=C1)NC(=O)C2=CN=CC=C2
Standard InChIKey KTXBOOWDLPUROC-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H16N4O2/c1-11(19-15(21)13-5-3-7-17-10-13)8-18-14(20)12-4-2-6-16-9-12/h2-7,9-11H,8H2,1H3,(H,18,20)(H,19,21)
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Nicaraven

DescriptionNicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.In Vitro:The maximum aggregation rate induced by adenosine diphosphate (ADP) is significantly inhibited by nicaraven at concentration ranges of 350 μM or higher in the healthy volunteer platelets. The maximum aggregation rate induced by collagen is significantly inhibited by 1.75 mM of nicaraven[1].In Vivo:Nicaraven inhibits lipid peroxidation in the liver, improves hepatic and systemic hemodynamics and energy metabolism, and suppresses liver enzyme release, endothelin-1 elevation in hepatic venous blood, histologic damage, and neutrophil infiltration into the liver[1]. Nicaraven increases the number of c-kit(+) stem/progenitor cells in bone marrow and peripheral blood, with a recovery rate around 60-90% of age-matched non-irradiated healthy mice. The potency of colony forming from hematopoietic stem/progenitor cells as indicator of function is completely protected with nicaraven treatment[2]. Administration of nicaraven significantly increases the number, improves the colony-forming capacity, and decreases the DNA damage of hematopoietic stem/progenitor cells. The urinary levels of 8-oxo-2′-deoxyguanosine, a marker of DNA oxidation, are significantly lower in mice that are given nicaraven compared with those that receive a placebo. The administration of nicaraven significantly decreases the levels of the inflammatory cytokines IL-6 and TNF-α in the plasma of mice[3].

References:
[1]. Komiya T, et al. A novel free radical scavenger, nicaraven, inhibits human platelet aggregation in vitro. Clin Neuropharmacol. 1999 Jan-Feb;22(1):11-4. [2]. Yokota R, et al. A novel hydroxyl radical scavenger, nicaraven, protects the liver from warm ischemia and reperfusion injury. Surgery. 2000 Jun;127(6):661-9. [3]. Ali H, et al. The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures. [4]. Nicaraven attenuates radiation-induced injury in hematopoietic stem/progenitor cells in mice. PLoS One. 2013;8(3):e60023.

Protocol

Animal Administration [3]
Mice: To investigate the protective effect and related mechanisms of nicaraven on radiation-induced injury in hematopoietic stem/progenitor cells, 12 mice are exposed to 1 Gy γ-rays daily for 5 days in succession (a total of 5 Gy) and are then given intraperitoneal injections of nicaraven (100 mg/kg/day, Nicaraven group; n=6) or saline only (Placebo group; n=6), respectively, soon after each exposure. The mice are sacrificed 2 days after the last exposure, and samples of urine, blood, and bone marrow cells are collected and used for the following experiments[3].

References:
[1]. Komiya T, et al. A novel free radical scavenger, nicaraven, inhibits human platelet aggregation in vitro. Clin Neuropharmacol. 1999 Jan-Feb;22(1):11-4. [2]. Yokota R, et al. A novel hydroxyl radical scavenger, nicaraven, protects the liver from warm ischemia and reperfusion injury. Surgery. 2000 Jun;127(6):661-9. [3]. Ali H, et al. The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures. [4]. Nicaraven attenuates radiation-induced injury in hematopoietic stem/progenitor cells in mice. PLoS One. 2013;8(3):e60023.

Nicaraven Dilution Calculator

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Preparing Stock Solutions of Nicaraven

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5173 mL 17.5864 mL 35.1729 mL 70.3457 mL 87.9322 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 mL 14.0691 mL 17.5864 mL
10 mM 0.3517 mL 1.7586 mL 3.5173 mL 7.0346 mL 8.7932 mL
50 mM 0.0703 mL 0.3517 mL 0.7035 mL 1.4069 mL 1.7586 mL
100 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.7035 mL 0.8793 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Nicaraven

Nicaraven, a Potential Radioprotective Agent, has Very Limited Effects on the Survival of Cancer Cells and the Growth of Established Tumors.[Pubmed:28225650]

Radiat Res. 2017 Feb 22.

Radiotherapy is one of the major treatment modalities for the management of various cancers, however, it is limited by the severe side effects and complications experienced by some patients. Nicaraven, a chemically synthesized hydroxyl radical-specific scavenger, has been shown to protect normal tissues from radiation-induced injury. We investigated the role of Nicaraven in cancer cells and tumor growth. While Nicaraven did not significantly change the colony-forming abilities and DNA damage levels in several cancer cell lines after irradiation, it significantly protected mouse bone marrow-derived hematopoietic stem cells from radiation injury. In established mouse tumor models in which radiation exposure significantly inhibited the growth of tumors, Nicaraven did not significantly mitigate the radiation-induced inhibition of tumor growth. The results of this study showed that while Nicaraven attenuated the toxicity of radiotherapy in hematopoietic stem cells, it had very limited effects on the survival of cancer cells and tumor growth. Nicaraven may be an ideal drug for mitigating the side effects of radiotherapy in patients with cancer.

Nicaraven attenuates radiation-induced injury in hematopoietic stem/progenitor cells in mice.[Pubmed:23555869]

PLoS One. 2013;8(3):e60023.

Nicaraven, a chemically synthesized hydroxyl radical-specific scavenger, has been demonstrated to protect against ischemia-reperfusion injury in various organs. We investigated whether Nicaraven can attenuate radiation-induced injury in hematopoietic stem/progenitor cells, which is the conmen complication of radiotherapy and one of the major causes of death in sub-acute phase after accidental exposure to high dose radiation. C57BL/6 mice were exposed to 1 Gy gamma-ray radiation daily for 5 days in succession (a total of 5 Gy), and given Nicaraven or a placebo after each exposure. The mice were sacrificed 2 days after the last radiation treatment, and the protective effects and relevant mechanisms of Nicaraven in hematopoietic stem/progenitor cells with radiation-induced damage were investigated by ex vivo examination. We found that post-radiation administration of Nicaraven significantly increased the number, improved the colony-forming capacity, and decreased the DNA damage of hematopoietic stem/progenitor cells. The urinary levels of 8-oxo-2'-deoxyguanosine, a marker of DNA oxidation, were significantly lower in mice that were given Nicaraven compared with those that received a placebo treatment, although the levels of intracellular and mitochondrial reactive oxygen species in the bone marrow cells did not differ significantly between the two groups. Interestingly, compared with the placebo treatment, the administration of Nicaraven significantly decreased the levels of the inflammatory cytokines IL-6 and TNF-alpha in the plasma of mice. Our data suggest that Nicaraven effectively diminished the effects of radiation-induced injury in hematopoietic stem/progenitor cells, which is likely associated with the anti-oxidative and anti-inflammatory properties of this compound.

The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures.[Pubmed:25173934]

Biochem Biophys Res Commun. 2014 Sep 26;452(3):548-53.

Nicaraven, a hydroxyl radical-specific scavenger has been demonstrated to attenuate radiation injury in hematopoietic stem cells with 5Gy gamma-ray exposures. We explored the effect and related mechanisms of Nicaraven for protecting radiation injury induced by sequential exposures to a relatively lower dose gamma-ray. C57BL/6 mice were given Nicaraven or placebo within 30min before exposure to 50mGy gamma-ray daily for 30days in sequences (cumulative dose of 1.5Gy). Mice were victimized 24h after the last radiation exposure, and the number, function and oxidative stress of hematopoietic stem cells were quantitatively estimated. We also compared the gene expression in these purified stem cells from mice received Nicaraven and placebo treatment. Nicaraven increased the number of c-kit(+) stem/progenitor cells in bone marrow and peripheral blood, with a recovery rate around 60-90% of age-matched non-irradiated healthy mice. The potency of colony forming from hematopoietic stem/progenitor cells as indicator of function was completely protected with Nicaraven treatment. Furthermore, Nicaraven treatment changed the expression of many genes associated to DNA repair, inflammatory response, and immunomodulation in c-kit(+) stem/progenitor cells. Nicaraven effectively protected against damages of hematopoietic stem/progenitor cells induced by sequential exposures to a relatively low dose radiation, via complex mechanisms.

Description

Nicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.

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