Propiconazole-d3 (nitrate)
目录号 : GC47978
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Propiconazole-d3 is intended for use as an internal standard for the quantification of propiconazole by GC- or LC-MS. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption.1 It inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s = 0.04 and >200 µM, respectively).2 Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s = 0.073 and 4.6 µg/ml, respectively), as well as A. niger, M. fructigena, S. nodorum, T. harzanium, R. solani, and S. rolfsii at concentrations ranging from 0.1 to 5 ppm.3 It increases the weight of seminal vesicles and vas deferens, as well as the percentage of sperm with abnormal tail morphology, and decreases the plasma concentration of estradiol in male rats when administered at a dose of 4 mg/kg.4 Propiconazole increases production of reactive oxygen species (ROS), the number of DNA mutations, and the incidence of tumor formation in mouse liver.5 Formulations containing propiconazole have been used in the control of fungi in agriculture.
1.Zarn, J.A., BrÜschweiler, B.J., and Schlatter, J.R.Azole fungicides affect mammalian steroidogenesis by inhibiting sterol 14 α-demethylase and aromataseEnviron. Health Perspect.111(3)255-261(2003) 2.Vanden Bossche, H., Lauwers, W., Willemsens, G., et al.Molecular basis for the antimycotic and antibacterial activity of N-substituted imidazoles and triazoles: The inhibition of isoprenoid biosynthesisPestic. Sci.15(2)188-198(1984) 3.Sancholle, M., Weete, J.D., and Montani, C.Effects of triazoles on fungi: I. Growth and cellular permeabilityPest. Biochem. Phys.21(1)31-44(1984) 4.Costa, N.O., Vieira, M.L., Sgarioni, V., et al.Evaluation of the reproductive toxicity of fungicide propiconazole in male ratsToxicology33555-61(2015) 5.Nesnow, S.Integration of toxicological approaches with "omic" and related technologies to elucidate mechanisms of carcinogenic action: Propiconazole, an exampleCancer Lett.334(1)20-27(2013)
| Cas No. | N/A | SDF | |
| Canonical SMILES | ClC(C=C1)=CC(Cl)=C1C2(CN3C=NC=N3)OC([2H])([2H])C(CCC)([2H])O2.O=[N](O)=O | ||
| 分子式 | C15H14Cl2D3N3O2.HNO3 | 分子量 | 408.3 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 0.1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4492 mL | 12.2459 mL | 24.4918 mL |
| 5 mM | 0.4898 mL | 2.4492 mL | 4.8984 mL |
| 10 mM | 0.2449 mL | 1.2246 mL | 2.4492 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Dietary nitrate supplementation and exercise performance
Sports Med 2014 May;44 Suppl 1(Suppl 1):S35-45.PMID:24791915DOI:10.1007/s40279-014-0149-y.
Dietary nitrate is growing in popularity as a sports nutrition supplement. This article reviews the evidence base for the potential of inorganic nitrate to enhance sports and exercise performance. Inorganic nitrate is present in numerous foodstuffs and is abundant in green leafy vegetables and beetroot. Following ingestion, nitrate is converted in the body to nitrite and stored and circulated in the blood. In conditions of low oxygen availability, nitrite can be converted into nitric oxide, which is known to play a number of important roles in vascular and metabolic control. Dietary nitrate supplementation increases plasma nitrite concentration and reduces resting blood pressure. Intriguingly, nitrate supplementation also reduces the oxygen cost of submaximal exercise and can, in some circumstances, enhance exercise tolerance and performance. The mechanisms that may be responsible for these effects are reviewed and practical guidelines for safe and efficacious dietary nitrate supplementation are provided.
Food sources of nitrates and nitrites: the physiologic context for potential health benefits
Am J Clin Nutr 2009 Jul;90(1):1-10.PMID:19439460DOI:10.3945/ajcn.2008.27131.
The presence of nitrates and nitrites in food is associated with an increased risk of gastrointestinal cancer and, in infants, methemoglobinemia. Despite the physiologic roles for nitrate and nitrite in vascular and immune function, consideration of food sources of nitrates and nitrites as healthful dietary components has received little attention. Approximately 80% of dietary nitrates are derived from vegetable consumption; sources of nitrites include vegetables, fruit, and processed meats. Nitrites are produced endogenously through the oxidation of nitric oxide and through a reduction of nitrate by commensal bacteria in the mouth and gastrointestinal tract. As such, the dietary provision of nitrates and nitrites from vegetables and fruit may contribute to the blood pressure-lowering effects of the Dietary Approaches to Stop Hypertension (DASH) diet. We quantified nitrate and nitrite concentrations by HPLC in a convenience sample of foods. Incorporating these values into 2 hypothetical dietary patterns that emphasize high-nitrate or low-nitrate vegetable and fruit choices based on the DASH diet, we found that nitrate concentrations in these 2 patterns vary from 174 to 1222 mg. The hypothetical high-nitrate DASH diet pattern exceeds the World Health Organization's Acceptable Daily Intake for nitrate by 550% for a 60-kg adult. These data call into question the rationale for recommendations to limit nitrate and nitrite consumption from plant foods; a comprehensive reevaluation of the health effects of food sources of nitrates and nitrites is appropriate. The strength of the evidence linking the consumption of nitrate- and nitrite-containing plant foods to beneficial health effects supports the consideration of these compounds as nutrients.
nitrate tolerance
Int J Cardiol 1986 Jul;12(1):1-19.PMID:3089947DOI:10.1016/0167-5273(86)90094-x.
Nitrates are widely used in anginal prophylaxis. In spite of the fact that the concept of nitrate tolerance was first put forward many years ago, the question of tolerance has remained controversial. There is widespread agreement that tolerance does occur to the effects of nitrates on arterial pressure. In contrast, tolerance to the venous and pulmonary effects is disputed. Similarly, the possibility of tolerance to the antianginal effects remains at issue. In this review, I discuss the factors which may have contributed to conflicting results in different studies, in particular recent findings on the rapidity of onset and reversal of tolerance. Tolerance develops rapidly on initiation of treatment and disappears equally rapidly on its discontinuation. In addition, tolerance appears to be a function of plasma nitrate profile. It is most likely to occur when plasma nitrate levels are constant and least likely when nitrate levels fluctuate. Furthermore, the provision of a daily nitrate free interval may protect against the development of tolerance. I then discuss the implications of these findings for patient management. They suggest that nitrate prophylaxis should not be used continuously, if this can be avoided. Rather, prophylaxis should be tailored to the individual to provide protection at times of maximum susceptibility, while allowing nitrate levels to fall at other times. The adequacy of antianginal protection with drug regimens incorporating a nitrate free interval requires further assessment. Similarly, the possibility that a nitrate free interval might lead to withdrawal effects and exacerbation of angina needs to be excluded.
The Effect of Dietary nitrate Supplementation on Endurance Exercise Performance in Healthy Adults: A Systematic Review and Meta-Analysis
Sports Med 2017 Apr;47(4):735-756.PMID:27600147DOI:10.1007/s40279-016-0617-7.
Background: Recent research into the use of dietary nitrates and their role in vascular function has led to it becoming progressively more popular amongst athletes attempting to enhance performance. Objective: The objective of this review was to perform a systematic review and meta-analysis of the literature to evaluate the effect of dietary nitrate (NO3-) supplementation on endurance exercise performance. An additional aim was to determine whether the performance outcomes are affected by potential moderator variables. Data sources: Relevant databases such as Cochrane Library, Embase, PubMed, Ovid, Scopus and Web of Science were searched for the following search terms 'nitrates OR nitrate OR beetroot OR table beet OR garden beet OR red beet AND exercise AND performance' from inception to October 2015. Study selection: Studies were included if a placebo versus dietary nitrate-only supplementation protocol was able to be compared, and if a quantifiable measure of exercise performance was ≥30 s (for a single bout of exercise or the combined total for multiple bouts). Study appraisal and synthesis: The literature search identified 1038 studies, with 47 (76 trials) meeting the inclusion criteria. Data from the 76 trials were extracted for inclusion in the meta-analysis. A fixed-effects meta-analysis was conducted for time trial (TT) (n = 28), time to exhaustion (TTE) (n = 22) and graded-exercise test (GXT) (n = 8) protocols. Univariate meta-regression was used to assess potential moderator variables (exercise type, dose duration, NO3- type, study quality, fitness level and percentage nitrite change). Results: Pooled analysis identified a trivial but non-significant effect in favour of dietary NO3- supplementation [effect size (ES) = -0.10, 95 % Cl = -0.27 to 0.06, p > 0.05]. TTE trials had a small to moderate statistically significant effect in favour of dietary NO3- supplementation (ES = 0.33, 95 % Cl = 0.15-0.50, p < 0.01). GXT trials had a small but non-significant effect in favour of dietary NO3- supplementation in GXT performance measures (ES = 0.25, 95 % Cl = -0.06 to 0.56, p > 0.05). No significant heterogeneity was detected in the meta-analysis. No statistically significant effects were observed from the meta-regression analysis. Conclusion: Dietary NO3- supplementation is likely to elicit a positive outcome when testing endurance exercise capacity, whereas dietary NO3- supplementation is less likely to be effective for time-trial performance. Further work is needed to understand the optimal dosing strategies, which population is most likely to benefit, and under which conditions dietary nitrates are likely to be most effective for performance.
[nitrate tolerance]
Schweiz Med Wochenschr 1988 Dec 17;118(50):1892-8.PMID:2906173doi
nitrate tolerance is defined as an attenuation or even loss of hemodynamic and anti-ischemic effects during continuous nitrate medication. The blunted response may be due to the development of pseudotolerance and true pharmacologic tolerance. Pseudotolerance is the result of volume and salt retention, as well as the stimulation of counter-regulatory mechanisms which may alter the baseline hemodynamics of a patient during nitrate therapy. Far less important are changes in nitrate pharmacokinetics. True pharmacological tolerance may also be of practical importance. Diminished uptake of nitrates into the vascular smooth muscle cell, a decrease in intracellular SH groups, inhibition of the guanylate-cyclase, and stimulation of a specific phosphodiesterase may result in a decrease of cyclic GMP formation and hence to a decrease in nitrate induced vasodilatation. Tolerance development may be prevented by intermittent nitrate administration providing intervals with low plasma and tissue nitrate levels. In consequence, nitrates should be used predominantly for treatment of ischemic episodes, but 24-hour anti-ischemic action for the prevention of ischemia can be better achieved by treatment with a beta-blocker and/or a calcium antagonist. Nitrates should be added in times of maximum susceptibility to ischemia, while allowing nitrate levels to fall at other times.