GNF179 Metabolite - CAS 1310455-86-7
Catalog number: 1310455-86-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H16FN3
Molecular Weight:
245.3
COA:
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Targets:
Antiparasitic
Description:
GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
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Purity:
>98%
Synonyms:
GNF 179 Metabolite; GNF-179 Metabolite
MSDS:
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1.Divergent behavior of hydrogen sulfide pools and of the sulfur metabolite lanthionine, a novel uremic toxin, in dialysis patients.
Perna AF1, Di Nunzio A2, Amoresano A3, Pane F3, Fontanarosa C3, Piero P3, Vigorito C4, Cirillo G2, Zacchia M2, Trepiccione F2, Ingrosso D4. Biochimie. 2016 Apr 26. pii: S0300-9084(16)30071-2. doi: 10.1016/j.biochi.2016.04.018. [Epub ahead of print]
Dialysis patients display a high cardiovascular mortality, the causes of which are still not completely explained, but are related to uremic toxicity. Among uremic toxins, homocysteine and cysteine are both substrates of cystathionine β-synthase and cystathionine γ-lyase in hydrogen sulfide biosynthesis, leading to the formation of two sulfur metabolites, lanthionine and homolanthionine, considered stable indirect biomarkers of its production. Hydrogen sulfide is involved in the modulation of multiple pathophysiological responses. In uremia, we have demonstrated low plasma total hydrogen sulfide levels, due to reduced cystathionine γ-lyase expression. Plasma hydrogen sulfide levels were measured in hemodialysis patients and healthy controls with three different techniques in comparison, allowing to discern the different pools of this gas. The protein-bound (the one thought to be the most active) and acid-labile forms are significantly decreased, while homolanthionine, but especially lanthionine, accumulate in the blood of uremic patients.
2.Pharmacokinetics of mangiferin and its metabolite-Norathyriol, Part 1: Systemic evaluation of hepatic first-pass effect in vitro and in vivo.
Tian X1, Gao Y1, Xu Z2, Lian S3, Ma Y3, Guo X1, Hu P1, Li Z1, Huang C1. Biofactors. 2016 Apr 30. doi: 10.1002/biof.1291. [Epub ahead of print]
Mangiferin (MGF), a glucoside of xanthone existing in phytomedicines and food, is increasingly attracting attention on diabetes treatment, while the underlying mechanism leading to its low oral bioavailability is unclear. Norathyriol (NTR), an active metabolite with hypoglycemic activity and its exposure after MGF dosing remains unclear. Hence, a rapid and sensitive LC-MS/MS method was established and validated to determine MGF and NTR and applied in the PK study in rats. Correspondingly, the in vitro experiments on temperature-dependent uptake, and MGF metabolism in hepatocyte and enterobacteria samples were performed. Results revealed that hepatic first-pass effect slightly contributed to the poor bioavailability of MGF, based on the MGF exposure in portal vein plasma was nearly similar to that in systemic plasma, and the MGF accumulation in the liver was limited, so was that of NTR. Correspondingly, the in vitro study revealed the MGF uptake was mainly dependent on poor passive transport, possibly leading to its limited hepatic metabolism and accumulation.
3.The Molting Biomarker Metabolite N-acetylglucosamino-1,5-lactone in Female Urine of the Helmet Crab Telmessus cheiragonus.
Yano H1, Kamio M2, Nagai H1. Biol Bull. 2016 Apr;230(2):143-151.
N-acetylglucosamino-1,5-lactone (NAGL) is a molting biomarker in the blue crab Callinectes sapidus The concentration of this compound in urine is highest at the premolt stage. Since sexually mature premolt females release sex pheromone in their urine, NAGL is a candidate sex pheromone molecule in C. sapidus This compound has not been reported in other species. In the present study, we quantified the concentration of NAGL in the urine of the helmet crab Telmessus cheiragonus, using nuclear magnetic resonance spectroscopy, and found that the concentration increases toward the day of molting and decreases after molting. However, the total amount of NAGL collected from individual animals was greatest two to five days after molting, because the amount of urine collected was the lowest at the premolt stage, and it increased after molting. The highest median concentration of NAGL in T. cheiragonas was 29 μmol l-1, which is 75% of the highest concentration reported in C.
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CAS 1310455-86-7 GNF179 Metabolite

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