NSAH
目录号 : GC62679
NSAH 是可逆的、竞争性的非核苷类的核苷酸还原酶 (RR)的抑制剂，其 cell-free 和 cell-bases 的 IC50 值分别为 32 μM 和 ~250 nM。
Cas No.:1099592-35-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively[1].
NSAH depresses dGTP and dATP levels in the dNTP pool causing S-phase arrest, providing evidence for RR inhibition in cells[1].NSAH (0-10 μM, 2, 6, 24, or 72 h) exhibits potent anti-tumor activity in 3 cancer cell lines[1].NSAH blocks S-phase progression well to the extent and timing of the decreases in dATP and dGTP[1].
[1]. Md Faiz Ahmad, et al. Potent competitive inhibition of human ribonucleotide reductase by a nonnucleoside small molecule. Proc Natl Acad Sci U S A. 2017 Aug 1;114(31):8241-8246.
| Cas No. | 1099592-35-4 | SDF | |
| 分子式 | C18H14N2O3 | 分子量 | 306.32 |
| 溶解度 | DMSO : 62.5 mg/mL (204.03 mM; Need ultrasonic) | 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 | 3.2646 mL | 16.3228 mL | 32.6456 mL |
| 5 mM | 0.6529 mL | 3.2646 mL | 6.5291 mL |
| 10 mM | 0.3265 mL | 1.6323 mL | 3.2646 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。
Altered Gut Microbiota in H1-Antihistamine-Resistant Chronic Spontaneous Urticaria Associates With Systemic Inflammation
Front Cell Infect Microbiol 2022 Mar 16;12:831489.PMID:35372130DOI:10.3389/fcimb.2022.831489.
Background and objective: Chronic spontaneous urticaria (CSU) is a histamine-mediated inflammatory skin disease, and second-generation non-sedating H1-antihistamines (NSAH) at licensed doses have long been the first-line therapy in CSU. However, about 50% of patients are resistant to NSAH, and the precise pathogenesis remains largely unknown but seems to be associated with low-level systemic or intestinal inflammation. We aim to determine the fecal microbial composition and clarify its correlation with the clinical profiles og CSU with NSAH resistance. Methods: A total of 25 CSU patients with or 19 CSU patients without NSAH resistance and 19 healthy controls (HC) were enrolled in this study. The intestinal microbiome was detected by 16S rRNA sequencing. The data were analyzed using R language software. Results: Significantly higher urticarial activity score for 7 days, stool calprotectin, erythrocyte sedimentation rate, serum C-reactive protein, and interleukin-6, but much lower alpha-diversity and evenness of fecal bacterial community were observed in CSU patients with NSAH resistance than in those without (P <0.05 for all variables). Compared to patients with nsAH-responsiveness, the abundance of fecal genera Prevotella, Megamonas, and Escherichia were significantly increased, while that of Blautia, Alistipes, Anaerostipes, and Lachnospira were remarkably reduced in nsAH-resistant patients (uncorrected P <0.05 for all variables). Finally, systemic not intestinal inflammation degree was positively correlated with genera Escherichia, while negatively with genera Blautia, Dorea, Lactobacillus, Eubacterium_hallii_group, and Roseburia. CSU without NSAH resistance and HC individuals showed almost unchanged genera bacterium. Conclusions: Among CSU patients, pro-inflammation phenotype relating to enteric dysbacteriosis features NSAH resistance in CSU patients. The results provide clues for future microbial-based or anti-inflammatory therapies on NSAH resistant CSU.
Negative Self-Assessment of Health in Women: Association with Sociodemographic Characteristics, Physical Inactivity and Multimorbidity
Int J Environ Res Public Health 2022 Feb 25;19(5):2666.PMID:35270359DOI:10.3390/ijerph19052666.
Introduction: Women present a higher prevalence of negative self-assessment of health (NSAH) when compared to men. However, there is a gap in the literature of factors associated with NSAH in women from developing countries such as Brazil. In addition, few studies have assessed the magnitude of the association between multimorbidity and NSAH in this population. Thus, the aim of this study was to evaluate the association between NSAH and sociodemographic characteristics, lifestyle and multimorbidity in women from the Midwest region of Brazil. Methods: A study based on data from the National Health Survey, a household survey that investigated health situation, lifestyle and risk factors for chronic diseases in the adult population of Brazil, was held. Sampling was performed in multiple stages. The selected women answered a standardized questionnaire on sociodemographic data, self-assessment of health and potential determinants. Poisson regression was used to analyze the association between NSAH and sociodemographic characteristics, lifestyle and multimorbidity. A significance level of 0.05% was established. Results: The study included 4233 women. The prevalence of NSAH found was 6.0% (95% Confidence Interval [95% CI]: 5.1-7.0%). There was an association between NSAH and advancing age, low schooling, physical inactivity and multimorbidity. Furthermore, there was an association between NSAH and diseases/disorders such as chronic back pain, systemic arterial hypertension, mental disorders, depression, cardiovascular diseases, stroke, cancer, hypercholesterolemia and diabetes mellitus. Conclusion: The prevalence of NSAH was low. A strong association was found between this variable and multimorbidity. In addition, increased age, low schooling and physical inactivity were predictors of NSAH in women.
Structure-guided design of anti-cancer ribonucleotide reductase inhibitors
J Enzyme Inhib Med Chem 2019 Dec;34(1):438-450.PMID:30734609DOI:10.1080/14756366.2018.1545226.
Ribonucleotide reductase (RR) catalyses the rate-limiting step of dNTP synthesis, establishing it as an important cancer target. While RR is traditionally inhibited by nucleoside-based antimetabolites, we recently discovered a naphthyl salicyl acyl hydrazone-based inhibitor (NSAH) that binds reversibly to the catalytic site (C-site). Here we report the synthesis and in vitro evaluation of 13 distinct compounds (TP1-13) with improved binding to hRR over NSAH (TP8), with lower KD's and more predicted residue interactions. Moreover, TP6 displayed the greatest growth inhibiting effect in the Panc1 pancreatic cancer cell line with an IC50 of 0.393 µM. This represents more than a 2-fold improvement over NSAH, making TP6 the most potent compound against pancreatic cancer emerging from the hydrazone inhibitors. NSAH was optimised by the addition of cyclic and polar groups replacing the naphthyl moiety, which occupies the phosphate-binding pocket in the C-site, establishing a new direction in inhibitor design.
The cost of treating allergic rhinitis
Curr Allergy Asthma Rep 2002 May;2(3):223-30.PMID:11918864DOI:10.1007/s11882-002-0023-0.
Allergic rhinitis is a high-cost, high-prevalence disease. In the year 2000, over $6 billion was spent on prescription medications to treat this illness. Although it is not associated with severe morbidity and mortality, allergic rhinitis has a major effect on the quality of life of the more than 50 million Americans with this illness. Intranasal corticosteroids (INCS) and nonsedating antihistamines (NSAH) are the most common prescription medications for this disease. INCS are recognized as the most effective treatment regimen for chronic symptoms. NSAH are perceived as important in the treatment of patients with mild disease, or as add-on therapy to INCS. When the literature is reviewed, the INCS produce the greatest decrease in total nasal symptom scores, the largest effect size, when compared with NSAH. Both classes of medications produce similar effects on concurrent allergic conjunctivitis. Further recent studies indicate that the INCS are also superior when used on an as-needed basis, and that there is little clinical benefit from the addition of loratadine to intranasal fluticasone. INCS have lower average wholesale prices as a class than the NSAH. Since the INCS are the dominant medication in efficacy studies and cost less, cost-effectiveness studies always favor intranasal corticosteroids.
MR angiography follow-up 10 years after cryptogenic nonperimesencephalic subarachnoid hemorrhage
PLoS One 2015 Feb 17;10(2):e0117925.PMID:25688554DOI:10.1371/journal.pone.0117925.
Objectives: Long-term magnetic resonance angiography (MRA) follow-up studies regarding cryptogenic nonperimesencephalic subarachnoid hemorrhage (NSAH) are scarce. This single-centre study identified all patients with angiographically verified cryptogenic NSAH from 1998 to 2007: The two main objectives were to prospectively assess the incidence of de novo aneurysm with 3.0-MRI years after cryptogenic NSAH in patients without evidence for further hemorrhage, and retrospectively assess patient demographics and outcome. Methods: From prospectively maintained report databases all patients with angiographically verified cryptogenic NSAH were identified. 21 of 29 patients received high-resolution 3T-MRI including time-of-flight and contrast-enhanced angiography, 10.2 ± 2.8 years after cryptogenic NSAH. MRA follow-up imaging was compared with initial digital subtraction angiography (DSA) and CT/MRA. Post-hemorrhage images were related to current MRI with reference to persistent lesions resulting from delayed cerebral ischemia (DCI) and post-hemorrhagic siderosis. Patient-based objectives were retrospectively abstracted from clinical databases. Results: 29 patients were identified with cryptogenic NSAH, 17 (59%) were male. Mean age at time of hemorrhage was 52.9 ± 14.4 years (range 4 - 74 years). 21 persons were available for long-term follow-up. In these, there were 213.5 person years of MRI-follow-up. No de novo aneurysm was detected. Mean modified Rankin Scale (mRS) during discharge was 1.28. Post-hemorrhage radiographic vasospasm was found in three patients (10.3%); DCI-related lesions occurred in one patient (3.4%). Five patients (17.2%) needed temporary external ventricular drainage; long-term CSF shunt dependency was necessary only in one patient (3.4%). Initial DSA retrospectively showed a 2 x 2 mm aneurysm of the right distal ICA in one patient, which remained stable. Post-hemorrhage siderosis was detected 8.1 years after the initial bleeding in one patient (4.8%). Conclusion: Patients with cryptogenic NSAH have favourable outcomes and do not exhibit higher risks for de novo aneurysms. Therefore the need for long-term follow up after cryptogenic NSAH is questionable.