Solifenacin-d5 (succinate)
(Synonyms: YM905-d5) 目录号 : GC49196
An internal standard for the quantification of solifenacin
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
carbamoylcholine Solifenacin-d5 is intended for use as an internal standard for the quantification of solifenacin by GC- or LC-MS. Solifenacin is a competitive antagonist of M1, M2, and M3 muscarinic acetylcholine receptors (Kis = 25, 125, and 10 nM, respectively, for the human receptors).1 It inhibits calcium mobilization induced by carbamoylcholine in isolated guinea pig detrusor muscle cells (Ki = 4 nM).2 Solifenacin inhibits carbachol-induced contraction of isolated guinea pig urinary bladder smooth muscle. In vivo, solifenacin (0.03-1 mg/kg) inhibits carbachol-induced increases in urinary bladder pressure in anesthetized rats. Formulations containing solifenacin have been used in the treatment of overactive bladder.
1.Hegde, S.S.Muscarinic receptors in the bladder: From basic research to therapeuticsBr. J. Pharmacol.147(2)S80-S87(2006) 2.Ikeda, K., Koboyashi, S., Suzuki, M., et al.M3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary glandNaunyn Schmiedebergs Arch. Pharmacol.366(2)97-103(2002)
| Cas No. | N/A | SDF | |
| 别名 | YM905-d5 | ||
| Canonical SMILES | O=C(O[C@H]1CN2CCC1CC2)N3[C@@H](C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H])C5=CC=CC=C5CC3.OC(CCC(O)=O)=O | ||
| 分子式 | C23H21D5N2O2·C4H6O4 | 分子量 | 485.6 |
| 溶解度 | DMSO: soluble,Methanol: soluble,Water: soluble | 储存条件 | -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 | 2.0593 mL | 10.2965 mL | 20.5931 mL |
| 5 mM | 0.4119 mL | 2.0593 mL | 4.1186 mL |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0593 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。
Coupling Krebs cycle metabolites to signalling in immunity and cancer
Nat Metab 2019 Jan;1:16-33.PMID:31032474DOI:10.1038/s42255-018-0014-7.
Metabolic reprogramming has become a key focus for both immunologists and cancer biologists, with exciting advances providing new insights into underlying mechanisms of disease. Metabolites traditionally associated with bioenergetics or biosynthesis have been implicated in immunity and malignancy in transformed cells, with a particular focus on intermediates of the mitochondrial pathway known as the Krebs cycle. Among these, the intermediates succinate, fumarate, itaconate, 2-hydroxyglutarate isomers (D-2-hydroxyglutarate and L-2-hydroxyglutarate) and acetyl-CoA now have extensive evidence for "non-metabolic" signalling functions in both physiological immune contexts and in disease contexts, such as the initiation of carcinogenesis. This review will describe how metabolic reprogramming, with emphasis placed on these metabolites, leads to altered immune cell and transformed cell function. The latest findings are informative for new therapeutic approaches which could be transformative for a range of diseases.
Krebs Cycle Reimagined: The Emerging Roles of succinate and Itaconate as Signal Transducers
Cell 2018 Aug 9;174(4):780-784.PMID:30096309DOI:10.1016/j.cell.2018.07.030.
Krebs cycle intermediates traditionally link to oxidative phosphorylation whilst also making key cell components. It is now clear that some of these metabolites also act as signals. succinate plays an important role in inflammatory, hypoxic, and metabolic signaling, while itaconate (from another Krebs cycle intermediate, cis-aconitate) has an anti-inflammatory role.
Cytokine-like Roles for Metabolites in Immunity
Mol Cell 2020 Jun 4;78(5):814-823.PMID:32333837DOI:10.1016/j.molcel.2020.04.002.
Metabolites have functions in the immune system independent of their conventional roles as sources or intermediates in biosynthesis and bioenergetics. We are still in the pioneering phase of gathering information about the functions of specific metabolites in immunoregulation. In this review, we cover succinate, itaconate, α-ketoglutarate, and lactate as examples. Each of these metabolites has a different story of how their immunoregulatory functions were discovered and how their roles in the complex process of inflammation were revealed. Parallels and interactions are emerging between metabolites and cytokines, well-known immunoregulators. We depict molecular mechanisms by which metabolites prime cellular and often physiological changes focusing on intra- and extra-cellular activities and signaling pathways. Possible therapeutic opportunities for immune and inflammatory diseases are emerging.
Host succinate inhibits influenza virus infection through succinylation and nuclear retention of the viral nucleoprotein
EMBO J 2022 Jun 14;41(12):e108306.PMID:35506364DOI:10.15252/embj.2021108306.
Influenza virus infection causes considerable morbidity and mortality, but current therapies have limited efficacy. We hypothesized that investigating the metabolic signaling during infection may help to design innovative antiviral approaches. Using bronchoalveolar lavages of infected mice, we here demonstrate that influenza virus induces a major reprogramming of lung metabolism. We focused on mitochondria-derived succinate that accumulated both in the respiratory fluids of virus-challenged mice and of patients with influenza pneumonia. Notably, succinate displays a potent antiviral activity in vitro as it inhibits the multiplication of influenza A/H1N1 and A/H3N2 strains and strongly decreases virus-triggered metabolic perturbations and inflammatory responses. Moreover, mice receiving succinate intranasally showed reduced viral loads in lungs and increased survival compared to control animals. The antiviral mechanism involves a succinate-dependent posttranslational modification, that is, succinylation, of the viral nucleoprotein at the highly conserved K87 residue. Succinylation of viral nucleoprotein altered its electrostatic interactions with viral RNA and further impaired the trafficking of viral ribonucleoprotein complexes. The finding that succinate efficiently disrupts the influenza replication cycle opens up new avenues for improved treatment of influenza pneumonia.
Improved succinate production by metabolic engineering
Biomed Res Int 2013;2013:538790.PMID:23691505DOI:10.1155/2013/538790.
succinate is a promising chemical which has wide applications and can be produced by biological route. The history of the biosuccinate production shows that the joint effort of different metabolic engineering approaches brings successful results. In order to enhance the succinate production, multiple metabolical strategies have been sought. In this review, different overproducers for succinate production, including natural succinate overproducers and metabolic engineered overproducers, are examined and the metabolic engineering strategies and performances are discussed. Modification of the mechanism of substrate transportation, knocking-out genes responsible for by-products accumulation, overexpression of the genes directly involved in the pathway, and improvement of internal NADH and ATP formation are some of the strategies applied. Combination of the appropriate genes from homologous and heterologous hosts, extension of substrate, integrated production of succinate, and other high-value-added products are expected to bring a desired objective of producing succinate from renewable resources economically and efficiently.