Benproperine phosphate
(Synonyms: 磷酸苯丙哌林) 目录号 : GC61831
An antitussive agent and ARPC2 inhibitor
Cas No.:19428-14-9
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
Benproperine is an antitussive agent and actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor.1,2 It increases the latency to first cough and decreases the number of coughs during and after a citric acid aerosol challenge in a guinea pig model of cough when administered at a dose of 27 mg/kg.1 It binds to ARPC2 and delays the initiation of actin polymerization in the presence of actin, the Arp2/3 complex, and the Wiskott-Aldrich syndrome protein (WASP) VCA domain, but not actin alone, when used at a concentration of 10 ?M.2 Benproperine (1-10 ?M) inhibits the migration and invasion of DLD-1 and AsPC-1 cancer cells and reduces lung metastasis in an AsPC-1 mouse model of metastasis when administered at a dose of 50 m/kg. Formulations containing benproperine have been used as cough suppressants.
1.Li, Y., Zhong, D.F., Chen, S.W.C., et al.Identification of some benproperine metabolites in humans and investigation of their antitussive effectActa Pharmacol. Sin.26(12)1519-1526(2005) 2.Yoon, Y.J., Han, Y.-M., Choi, J., et al.Benproperine, an ARPC2 inhibitor, suppresses cancer cell migration and tumor metastasisBiochem. Pharmacol.16346-59(2019)
| Cas No. | 19428-14-9 | SDF | |
| 别名 | 磷酸苯丙哌林 | ||
| Canonical SMILES | CC(N1CCCCC1)COC2=CC=CC=C2CC3=CC=CC=C3.O=P(O)(O)O | ||
| 分子式 | C21H30NO5P | 分子量 | 407.44 |
| 溶解度 | DMSO : 250 mg/mL (613.59 mM) | 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 | 2.4543 mL | 12.2717 mL | 24.5435 mL |
| 5 mM | 0.4909 mL | 2.4543 mL | 4.9087 mL |
| 10 mM | 0.2454 mL | 1.2272 mL | 2.4543 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。
Repurposing antitussive Benproperine phosphate against pancreatic cancer depends on autophagy arrest
Mol Oncol 2021 Feb;15(2):725-738.PMID:33226737DOI:10.1002/1878-0261.12854.
Pancreatic cancer (PC) is one of the most common human malignancies worldwide and remains a major clinical challenge. Here, we found that Benproperine phosphate (BPP), a cough suppressant, showed a significant anticancer effect on PC both in vitro and in vivo via the induction of autophagy-mediated cell death. Mechanistic studies revealed that BPP triggered AMPK/mTOR-mediated autophagy initiation and disturbed Ras-related protein Rab-11A (RAB11A)-mediated autophagosome-lysosome fusion, resulting in excessive accumulation of autophagosomes. Inhibition of autophagy or overexpression of RAB11A partially reversed BPP-induced growth inhibition in PC cells, suggesting that BPP might induce lethal autophagy arrest in PC cells. In conclusion, our results identify BPP as a potent antitumor agent for PC via the induction of autophagy arrest, therefore providing a new potential therapeutic strategy for the treatment of PC.
Resonance light scattering study on the interaction of Benproperine phosphate with eriochrome blue black R in the presence of sodium dodecylbenzene sulphonate and its analytical application
Luminescence 2009 Mar-Apr;24(2):67-72.PMID:18800357DOI:10.1002/bio.1064.
The interaction of Benproperine phosphate (BPP) with eriochrome blue black R (EBBR) in the presence of sodium dodecylbenzene sulphonate (SDBS) was studied using resonance light scattering (RLS) technology and ultraviolet-visual (UV-vis) spectrophotometry. Under optimum conditions, BPP reacts with EBBP and SDBS to form a three-component complex, which results in strong RLS signal and a new RLS peak. The enhanced RLS intensities are proportional to the concentration of BPP over the range 0.6-28.0 microg/mL, with a detection limit of 0.053 microg/mL. The affecting factors as well as the influence of coexisting substances were investigated. The results indicate that this assay method could be applied to the determination of BPP in pharmaceuticals, serum and urine samples with satisfactory results.
The nonnarcotic antitussive drug dimemorfan: a review
Clin Ther 1997 Mar-Apr;19(2):215-31.PMID:9152562DOI:10.1016/s0149-2918(97)80111-7.
The antitussive dimemorfan phosphate was discovered through extensive screening of morphinic derivatives and was introduced in Japan in 1975. The majority of studies on dimemorfan have been published in Japanese, and this review aims to make these data more generally available. The antitussive action of dimemorfan appears to be directly on the cough center in the medulla. Dimemorfan does not induce any significant physical or psychologic dependence, and its antitussive action is not affected by the opioid-receptor blocker levallorphan. Dimemorfan is therefore considered a nonnarcotic antitussive. Studies of antitussive effects in animal models indicate that dimemorfan is up to three times more potent than codeine and is equivalent to dextromethorphan. Three major comparative clinical trials and postmarketing surveillance studies showed that dimemorfan is equally or slightly more efficacious than dextromethorphan, Benproperine phosphate, or placebo for the control of coughing. Several animal and clinical studies have confirmed the efficacy and safety of dimemorfan. Dimemorfan was effective in the majority of patients. In contrast to the narcotic antitussives, dimemorfan caused no serious problems with the digestive system, such as constipation and disorders of the bile duct, caused no dependence or tolerance, and was unlikely to have clinical analgesic effects. Minor side effects, such as loss of appetite, nausea, and drowsiness, were seen in less than 10% of patients. A syrup formulation of dimemorphan that retains its efficacy and safety is also available. Overall, these data indicate that dimemorfan is an effective nonnarcotic antitussive agent with a low incidence of adverse events.
[Determination of Benproperine phosphate tablets by high performance liquid chromatography]
Se Pu 2000 Nov;18(6):566-7.PMID:12541753doi
A reversed-phase HPLC method for the determination of Benproperine phosphate tablets is reported. The chromatographic conditions were Hypersil-C18 column(5 microns, 4.6 mm i.d. x 150 mm) at 35 degrees C, mobile phase of methanol-water-glacial acetic acid-triethylamine(60:35:5:0.1, V/V) with a flow rate of 0.9 mL/min and UV detection at 270 nm. Cortisone acetate was selected as the internal standard. The linear relationship of calibration curve was good in the range of 9.96 mg/L-49.8 mg/L(r = 0.9998). The average recovery and RSD were 99.91%(n = 5) and 0.43% respectively. The total time of analysis for a run was within 7 min. The method is simple, sensitive, rapid and accurate.
[Nondestructive quantitative analysis of Cofrel medicines by improved partial least squares-NIR spectroscopy]
Guang Pu Xue Yu Guang Pu Fen Xi 2007 Jun;27(6):1098-101.PMID:17763766doi
In the present paper, improved partial least squares (PLS) method was used to parse near infrared (NIR) reflectance spectrum of Cofrel medicine. The contents of Benproperine phosphate, a availability pharmaceutical in Cofrel medicine, were accurately nondestructively quantitatively predicted. The best number of principal components (PC) was designed by scores plot of samples in PC. The effects of the wavelength range, conventional spectra, first-derivative spectra and second-derivative spectra on the results were discussed respectively. Comparing the results with those of HPLC, the relative errors(RE%) of Benproperine phosphate were less than 0.42%. The analytical results were sufficient for practical manufacture of Cofrel medicine.