Usaramine N-oxide
目录号 : GC37874Usaramine N-oxide 是从 Crotalaria pallida 中提取得到的一类黄酮类化合物,拥有抗炎活性。
Cas No.:117020-54-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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Usaramine N-oxide, a flavonoid isolated from Crotalaria pallida, possesses anti-inflammatory activities[1].
[1]. Hu XR, et al. Flavonoids, alkaloids from the seeds of Crotalaria pallida and their cytotoxicity and anti-inflammatory activities. Phytochemistry. 2017 Nov;143:64-71.
Cas No. | 117020-54-9 | SDF | |
Canonical SMILES | O=C(O[C@]1([H])CC[N+]2([O-])[C@]1([H])C(COC([C@](CO)(O)[C@H](C)C/3)=O)=CC2)C3=C\C | ||
分子式 | C18H25NO7 | 分子量 | 367.39 |
溶解度 | Soluble in DMSO | 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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.7219 mL | 13.6095 mL | 27.219 mL |
5 mM | 0.5444 mL | 2.7219 mL | 5.4438 mL |
10 mM | 0.2722 mL | 1.361 mL | 2.7219 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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Quantification of Usaramine and its N-Oxide Metabolite in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry
J Anal Toxicol 2022 May 20;46(5):512-518.PMID:34086913DOI:10.1093/jat/bkab060.
A sensitive, fast and robust liquid chromatography--tandem mass spectrometry (LC-MS-MS) method was developed and validated for the determination of usaramine (URM) and Usaramine N-oxide (UNO) in rat plasma. The separation was conducted on an ACQUITY UPLC BEH C18 Column (50 × 2.1 mm, 1.7 μm) and gradient eluted with mobile phase A (0.1% formic acid with 5 mM ammonium acetate in water) and B (0.1% formic acid in acetonitrile/methanol, 9/1, v/v). The method was linear over the range of 1-2,000 ng/mL for both analytes. The validated method was applied to investigate the pharmacokinetic behaviors and sex differences of URM and its N-oxide metabolite in rats. After intravenous administration of URM at 1 mg/kg, the AUC0-t values for URM and UNO were 363 ± 65 and 172 ± 32 ng/mL*h in male rats, while 744 ± 122 and 30.7 ± 7.4 ng/mL*h in females, respectively. The clearance of URM was significantly higher in male rats than in females (2.77 ± 0.50 vs 1.35 ± 0.19 L/h/kg, P < 0.05). After oral administration of URM at 10 mg/kg, the AUC0-t values of URM and UNO were 1,960 ± 208 and 1,637 ± 246 ng/mL*h in male rats, while 6,073 ± 488 and 300 ± 62 ng/mL*h in females, respectively. The oral bioavailability of URM in female rats (81.7%) was much higher than in males (54.0%). In conclusion, sex-based differences were observed in the pharmacokinetics, N-oxide metabolism and oral bioavailability of URM.
Pyrrolizidine alkaloids from Jacobaea vulgaris Gaertn and theoretical studies on intramolecular interactions
Nat Prod Res 2023 Feb 1;1-6.PMID:36722688DOI:10.1080/14786419.2023.2174533.
Two undescribed pyrrolizidine alkaloids, 13-dehydrosenkirkine (1) and chloromethylretrorsine (2), along with three known analogues, onetine (3), retrorsine (4), and Usaramine N-oxide (5), were isolated from Jacobaea vulgaris Gaertn. The structures of the undescribed compounds were elucidated by extensive spectrometric and spectroscopic techniques, including HRESIMS, NMR, calculated 13C-NMR DP4+ analysis and comparison with experimental and calculated ECD spectra. The undescribed compounds were evaluated for their antitumour activity against HT29, HeLa, and HepG2 cells. In addition, the intramolecular interactions and quadrupolar couplings were revealed by investigating the geometrical and electronic properties of three typical otonecine-type PAs in DFT theory.