Valnemulin
(Synonyms: 伐奈莫林) 目录号 : GC45136
A pleuromutilin antibiotic
Cas No.:101312-92-9
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
Valnemulin is a broad-spectrum pleuromutilin antibiotic that binds to peptidyl transferase in the 50S ribosomal subunit. It has been used in veterinary medicine to treat swine diseases including, B. hyodysenteriae and M. hyopneumoniae.
| Cas No. | 101312-92-9 | SDF | |
| 别名 | 伐奈莫林 | ||
| Canonical SMILES | O=C1CC[C@@]2(CC[C@H]3C)[C@@H](C)[C@H](O)[C@@](C=C)(C)C[C@@H](OC(CSC(C)(C)CNC([C@H](N)C(C)C)=O)=O)[C@@]3(C)[C@@]21[H] | ||
| 分子式 | C31H52N2O5S | 分子量 | 564.8 |
| 溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 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 | 1.7705 mL | 8.8527 mL | 17.7054 mL |
| 5 mM | 0.3541 mL | 1.7705 mL | 3.5411 mL |
| 10 mM | 0.1771 mL | 0.8853 mL | 1.7705 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。
Preparation and Evaluation of Valnemulin Hydrochloride Taste-Masking Granules
Curr Drug Deliv 2022;19(3):337-346.PMID:34477518DOI:10.2174/1567201818666210903151658.
Background: The bitter taste and strong irritation of Valnemulin hydrochloride limit its wide clinical application in pigs by oral. Method: In order to improve its palatability and residence time in the body, the Valnemulin hydrochloride taste-masking granules with sustained-release were prepared by combining solid dispersion based on fatty acid with wet granulation. The formulation was screened by orthogonal test with content, yield, grain size and angle of repose as evaluation indexes. Result: The results showed that the optimal granules were composed of corn starch, sucrose, citric acid, Valnemulin hydrochloride and myristic acid at a ratio of 40: 20: 20: 11: 19. The daily feed intake of pigs in the optimum taste-masking granule groups was similar to that of its self-control, and significantly higher than that in the Valnemulin hydrochloride active ingredient group, suggesting that the optimum granules have satisfactory palatability. The prepared granules improved the oral bioavailability of Valnemulin hydrochloride by 3.04 folds and extended its mean residence time (MRT) by 2.33 folds. Conclusion: The granules developed in this study could obviously improve the palatability and sustained release of Valnemulin hydrochloride. The producing method of granules by combining solid dispersion powder with wet granulation can provide ideas for other drugs with poor palatability and a short half-life.
Valnemulin downregulates nitric oxide, prostaglandin E2, and cytokine production via inhibition of NF-kappaB and MAPK activity
Int Immunopharmacol 2009 Jul;9(7-8):810-6.PMID:19293003DOI:10.1016/j.intimp.2009.02.018.
Valnemulin is a pleuromutilin antibiotic used in clinics for the treatment of various infections. We studied the in vitro anti-inflammatory effects of Valnemulin and associated signal transduction mechanisms in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. We found that Valnemulin inhibited nitric oxide (NO), prostaglandin E2 (PGE2), tumour necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6), and increased interleukin-10 (IL-10) production. Inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expression were also inhibited by Valnemulin. We further observed that Valnemulin prevented the LPS-induced NF-kappaB translocation from the cytoplasm into the nucleus. Valnemulin also blocked phosphorylation of three mitogen-activated protein kinases (MAPKs): extracellular signal receptor-activated kinase (ERK) 1/2, p38, and c-Jun N-terminal kinase (JNK). Our data indicate that Valnemulin may have therapeutic anti-inflammatory effects independent of its antibacterial activity.
Synthesis, characterization and in vitro release performance of the pegylated Valnemulin prodrug
J Vet Med Sci 2018 Feb 2;80(1):173-180.PMID:29187697DOI:10.1292/jvms.17-0434.
Valnemulin, successfully developed by Sandoz in 1984, is a new generation derivative of pleuromutilin related to tiamulin. Valnemulin has low water-solubility, a short half-life period, low bioavailability, and instability. The application of Valnemulin was restricted. Therefore, finding a more moderate delivery system is necessary to improve the shortcomings of Valnemulin. The purpose of the study was to improve the strong stability and the irritation caused by of Valnemulin hydrochloride power through pegylated-valnemulin prodrug mode. The prepared pegylated-valnemulin prodrug was characterized and evaluated by in vitro release performance under buffer solutions with pH levels of 7.4 and 3.6. The loading rate of Valnemulin in PEG-succinic-valnemulin prodrug was determined by ultraviolet spectrophotometer and high performance liquid chromatography (HPLC). HPLC with evaporative light scattering detector was applied to determine the amount of PEG-succinic acid. The loading rate of Valnemulin in PEG-succinic-valnemulin prodrug was 6.46%. PEG-succinic-valnemulin prodrug demonstrated a satisfactory solubility of Valnemulin with 523 mg·ml-1 and excellent stability verified by the stability experiment. The result of the in vitro release test showed that the prepared PEG-valnemulin prodrug has controlled release ability and the release rate of Valnemulin from PEG-valnemulin prodrug with a pH of 7.4 was 64.98%, which was higher than that of pH3.6 with release rate of 31.90%. Therefore, the prepared PEG-succinic-valnemulin prodrug has great application potential.
Preparation of Valnemulin hydrogen fumarate and its enhanced stability compared with Valnemulin hydrochloride
Pharm Dev Technol 2016;21(3):338-45.PMID:25597619DOI:10.3109/10837450.2014.1003656.
Context: It is necessary to develop a new salt of Valnemulin to replace the veterinary antibiotic, e.g. Valnemulin hydrochloride, in order to overcome its instability during storage and preparation. Objective: The objective of this study was to prepare a novel organic acid salt, Valnemulin hydrogen fumarate, and to investigate its stability compared with Valnemulin hydrochloride. Materials and methods: The crystal of Valnemulin hydrogen fumarate was prepared by modified crystallization method; the enhanced stabilities of Valnemulin hydrogen fumarate were conducted under irradiation and humid conditions, and the experimental results were simulated at AM1 level of calculations. Results: Valnemulin hydrogen fumarate was more stable than Valnemulin hydrochloride. After irradiation for 180 days, the content of Valnemulin hydrogen fumarate decreased slightly 2.7%, whereas the content of Valnemulin hydrochloride had an obvious decrease of 32.8%. Meanwhile, Valnemulin hydrogen fumarate showed better anti-RH (relative humidity) ability than Valnemulin hydrochloride. Under conditions of 65% and 85% RH, the absorption values of Valnemulin hydrogen fumarate towards water were 0.75% and 1.20% at 48 h, whereas those of Valnemulin hydrochloride were 4.50% and 9.71%, respectively. Conclusion: The enhanced stability of Valnemulin hydrogen fumarate could be attributed to its good crystallinity in comparison with the amorphous Valnemulin hydrochloride.
Chemotherapeutic Strategies with Valnemulin, Tilmicosin, and Tulathromycin to Control Mycoplasma hyopneumoniae Infection in Pigs
Antibiotics (Basel) 2022 Jul 4;11(7):893.PMID:35884148DOI:10.3390/antibiotics11070893.
Mycoplasma hyopneumoniae is the primary agent of Swine Enzootic Pneumonia (SEP). Vaccines reduce the clinical manifestation of the disease but do not prevent infection. The present study aimed to evaluate the use of antimicrobial drugs to minimize the impact of M. hyopneumoniae. For this, 32 pregnant female pigs and their litters were selected and then followed from birth to slaughter. The study involved three experimental groups that received metaphylactic treatment with different protocols involving tilmicosin, Valnemulin, tulathromycin, and a control group to compare the effect of treatments against M. hyopneumoniae infection throughout the phases. Performance data were recorded, and the piglets were evaluated for the occurrence of cough. Nasal swab and blood collection was conducted periodically to detect M. hyopneumoniae shedding and anti-M. hyopneumoniae IgG, respectively. At slaughter, the lungs of animals from all groups were evaluated, and samples were collected for histopathological examination and qPCR for M. hyopneumoniae detection. All protocols promoted a reduction in consolidation lung lesions when compared to the control group. Individuals treated with Valnemulin showed increased performance results, lower mortality, and low bacterial load in the lung. The results are promising and may indicate an alternative in the strategic control of M. hyopneumoniae infection in pigs.