BGC 20-1531 (hydrochloride)
(Synonyms: PGN 1531) 目录号 : GC42927
A potent and selective EP4 receptor antagonist
Cas No.:1962928-26-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively. It is selective for EP4, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. BGC 20-1531 antagonizes PGE2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.
| Cas No. | 1962928-26-2 | SDF | |
| 别名 | PGN 1531 | ||
| Canonical SMILES | COC1=CN=C(C2=CC=C(OCC3=C(C)OC(C(NS(C4=CC=CC=C4C)(=O)=O)=O)=C3)C=C2)C=C1.Cl | ||
| 分子式 | C26H24N2O6S•HCl | 分子量 | 529 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 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 | 1.8904 mL | 9.4518 mL | 18.9036 mL |
| 5 mM | 0.3781 mL | 1.8904 mL | 3.7807 mL |
| 10 mM | 0.189 mL | 0.9452 mL | 1.8904 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。
Central Composite Designed Fast Dissolving Tablets for Improved Solubility of the Loaded Drug Ondansetron hydrochloride
Biomed Res Int 2022 Aug 21;2022:2467574.PMID:36046453DOI:10.1155/2022/2467574.
Ondansetron tablets that are directly compressed using crospovidone and croscarmellose as a synthetic super disintegrant are the subject of this investigation. A central composite, response surface, randomly quadratic, nonblock (version 13.0.9.0) 32 factorial design is used to optimize the formulation (two-factor three-level). To make things even more complicated, nine different formulation batches (designated as F1-F9) were created. There were three levels of crospovidone and croscarmellose (+1, 0, -1). In addition to that, pre- and postcompressional parameters were evaluated, and all evaluated parameters were found to be within acceptable range. Among all postcompressional parameter dispersion and disintegration time, in vitro drug release experiments (to quantify the amount of medication released from the tablet) and their percentage prediction error were shown to have a significant influence on three dependent variables. Various pre- and postcompression characteristics of each active component were tested in vitro. Bulk density, tap density, angle of repose, Carr's index, and the Hausner ratio were all included in this analysis, as were many others. This tablet's hardness and friability were also assessed along with its dimension and weight variations. Additional stability studies may be conducted using the best batch of the product. For this study, we utilised the Design-Expert software to select the formulation F6, which had dispersion times of 17.67 ± 0.03 seconds, disintegration times of 120.12 ± 0.55 seconds, and percentage drug release measurements of 99.25 ± 0.36 within 30 minutes. Predicted values and experimental data had a strong correlation. Fast dissolving pills of ondansetron hydrochloride may be created by compressing the tablets directly.
Development of new bioactive molecules to treat breast and lung cancer with natural myricetin and its derivatives: A computational and SAR approach
Front Cell Infect Microbiol 2022 Sep 27;12:952297.PMID:36237438DOI:10.3389/fcimb.2022.952297.
Each biopharmaceutical research and new drug development investigation is targeted at discovering novel and potent medications for managing specific ailments. Thus, to discover and develop new potent medications, it should be performed sequentially or step by step. This is because drug development is a lengthy and risky work that requires significant money, resources, and labor. Breast and lung cancer contributes to the death of millions of people throughout the world each year, according to the report of the World Health Organization, and has been a public threat worldwide, although the global medical sector is developed and updated day by day. However, no proper treatment has been found until now. Therefore, this research has been conducted to find a new bioactive molecule to treat breast and lung cancer-such as natural myricetin and its derivatives-by using the latest and most authentic computer-aided drug-design approaches. At the beginning of this study, the biological pass prediction spectrum was calculated to select the target protein. It is noted that the probability of active (Pa) score is better in the antineoplastic (Pa: 0.788-0.938) in comparison with antiviral (Pa: 0.236-0.343), antibacterial (Pa: 0.274-0.421), and antifungal (Pa: 0.226-0.508). Thus, cancerous proteins, such as in breast and lung cancer, were picked up, and the computational investigation was continued. Furthermore, the docking score was found to be -7.3 to -10.4 kcal/mol for breast cancer (standard epirubicin hydrochloride, -8.3 kcal/mol), whereas for lung cancer, the score was -8.2 to -9.6 kcal/mol (standard carboplatin, -5.5 kcal/mol). The docking score is the primary concern, revealing that myricetin derivatives have better docking scores than standard chemotherapeutic agents epirubicin hydrochloride and carboplatin. Finally, drug-likeness, ADME, and toxicity prediction were fulfilled in this investigation, and it is noted that all the derivatives were highly soluble in a water medium, whereas they were totally free from AMES toxicity, hepatotoxicity, and skin sensitization, excluding only ligands 1 and 7. Thus, we proposed that the natural myricetin derivatives could be a better inhibitor for treating breast and lung cancer.
Studies on alginate-chitosan microcapsules and renal arterial embolization in rabbits
J Control Release 2002 Dec 5;84(3):87-98.PMID:12468213DOI:10.1016/s0168-3659(02)00214-6.
Spherical and well-dispersed alginate-chitosan microcapsules, with a mean diameter of 77.28+/-0.93 microm (n=3), were prepared by the emulsification-gelation method. Adriamycin hydrochloride (ADM) was used as a model drug to investigate the drug loading capacity and release characteristics of the microcapsules. The drug/carrier ratio and chitosan concentration influenced the encapsulation efficiency of adriamycin. The adriamycin release from microcapsules was obviously different in 0.1 mol/l HCl from that in phosphate-buffered saline (PBS, pH 7.4). The drug was completely and rapidly released in 0.1 mol/l HCl, while it showed a sustained release after a burst release in PBS. The increase in chitosan concentration had no effect on adriamycin release in PBS. Using sulforhodamin B (SRB)-staining survival assay, the inhibition of adriamycin alginate-chitosan microcapsules (ADM-ACM) to different cancer cell lines (human BGC-823 cells, Bel-7402 cells and Hela cells) in vitro was determined. The inhibitory rate of ADM-ACM suspension to the three cell lines significantly outran that of ADM solution, no matter at high or low concentration. The effects of blank alginate-chitosan microcapsules (BACM) on renal arterial embolization were examined with transcatheter arterial embolization in rabbits. The angiogram and histopathological results indicated the blank microcapsules had excellent short- and long-term effects on renal arterial embolization.