Policresulen
目录号 : GC65864
Policresulen 是一种有效的 DENV2 NS2B/NS3 蛋白酶抑制剂 (IC50 为 0.48 μg/mL)。Policresulen 抑制 BHK-21 细胞中的 DENV2 复制，IC50 为 4.99 μg/mL。Policresulen 作为蛋白酶的竞争性抑制剂，对蛋白酶的稳定性有轻微影响。
Cas No.:101418-00-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >50.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability[1].
| Cas No. | 101418-00-2 | SDF | Download SDF |
| 分子式 | (C8H10O4S)n | 分子量 | |
| 溶解度 | H2O : 100 mg/mL (Need ultrasonic); DMSO : 50 mg/mL (Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| 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。 |
||
| 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。 | ||
| 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。
Policresulen, a novel NS2B/NS3 protease inhibitor, effectively inhibits the replication of DENV2 virus in BHK-21 cells
Acta Pharmacol Sin 2015 Sep;36(9):1126-36.PMID:26279156DOI:10.1038/aps.2015.56.
Aim: Dengue is a severe epidemic disease caused by dengue virus (DENV) infection, for which no effective treatment is available. The protease complex, consisting of nonstructural protein 3 (NS3) and its cofactor NS2B, plays a pivotal role in the replication of DENV, thus may be a potential target for anti-DENV drugs. Here, we report a novel inhibitor of DENV2 NS2B/NS3 protease and its antiviral action. Methods: An enzymatic inhibition assay was used for screening DENV2 NS2B/NS3 inhibitors. Cytotoxicity to BHK-21 cells was assessed with MTT assay. Antiviral activity was evaluated in BHK-21 cells transfected with Rlu-DENV-Rep. The molecular mechanisms of the antiviral action was analyzed using surface plasmon resonance, ultraviolet-visible spectral analysis and differential scanning calorimetry assays, as well as molecular docking analysis combined with site-directed mutagenesis. Results: In our in-house library of old drugs (~1000 compounds), a topical hemostatic and antiseptic 2-hydroxy-3,5-bis[(4-hydroxy-2-methyl-5-sulfophenyl)methyl]-4-methyl-benzene-sulfonic acid (Policresulen) was found to be a potent inhibitor of DENV2 NS2B/NS3 protease with IC50 of 0.48 μg/mL. Furthermore, Policresulen inhibited DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL, whereas its IC50 for cytotoxicity to BHK-21 cells was 459.45 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability. Using biophysical technology-based assays and molecular docking analysis combined with site-directed mutagenesis, we demonstrated that the residues Gln106 and Arg133 of DENV2 NS2B/NS3 protease directly interacted with Policresulen via hydrogen bonding. Conclusion: Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease that inhibits DENV2 replication in BHK-21 cells. The binding mode of the protease and Policresulen provides useful hints for designing new type of inhibitors against the protease.
Oral chemical burns caused by topical application of Policresulen: a case report
J Yeungnam Med Sci 2022 Oct 20.PMID:36262098DOI:10.12701/jyms.2022.00472.
Oral mucosal burns can occur after contact with various chemical agents, and commonly manifest as areas of mucosal sloughing and ulceration. Policresulen (Albothyl, Celltrion Pharm Inc.) is an over-the-counter topical antiseptic that is frequently used to treat stomatitis. Policresulen solution is highly acidic, with an approximate pH of 0.6; it can thus cause mucosal injury when improperly applied in the oral cavity. Here, we present a rare case of an oral mucosal burn resulting from incorrect self-administration of Policresulen and emphasize the importance of increasing understanding of this adverse drug event among consumers and health professionals.
A synchronous fluorescence spectrofluorometric method for the simultaneous determination of Policresulen and cinchocaine hydrochloride in ointment and suppositories
Spectrochim Acta A Mol Biomol Spectrosc 2021 Jul 5;255:119648.PMID:33744839DOI:10.1016/j.saa.2021.119648.
For the treatment of internal and external hemorrhoids, Policresulen (POL) and cinchocaine hydrochloride (CIN) are used in combination. Using a new, simple, fast, and economical first-derivative synchronous fluorescence spectroscopic process, both drugs were simultaneously determined and validated. At Δλ60 nm and with a scanning rate of 600 nm/min, methanol was used as the solvent for both products. In the concentration ranges of 5.0-21.0 μg mL-1 and 0.5-6.0 μg mL-1 for POL and CIN, the amplitude-concentration plots were rectilinear. The detection limits were found to be 0.770 μg mL-1 and 0.118 μg mL-1 and the quantitation limits for POL and CIN were 2.541 μg mL-1 and 0.391 μg mL-1. To evaluate all compounds in synthetic mixtures and medicinal dosage types, the proposed method has been successfully applied. These findings were in line with the results obtained using high-performance thin layer chromatography, the comparison process.
Postoperative topical analgesia of hemorrhoidectomy with Policresulen and cinchocaine: a prospective and controlled study
Rev Col Bras Cir 2014 Mar-Apr;41(2):92-8.PMID:24918721DOI:10.1590/s0100-69912014000200004.
Objective: To evaluate the effects of topical Policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy. Methods: We conducted a prospective, double-blinded, controlled study. The control group received the usual guidelines with oral medications. The topical treatment group received, in addition, the application of the ointment and was comprised of two subgroups (Policresulen + cinchocaine, and placebo). Pain intensity was recorded with the visual analogue scale. Results: 43 patients were operated on: control group - n = 13, one excluded; placebo - n = 15; and Policresulen + cinchocaine - n = 15. The mean age was 45.98 years and 37.2% were men. The average pain intensity was 4.09 (immediate postoperative), 3.22 (hospital discharge), 5.73 (day 1) , 5.77 (day 2), 5.74 (day 3), 5.65 (day 7), 5.11 (day 10), 2.75 (day 15) and 7.70 (first bowel movement), with no difference between groups in all periods. Conclusion: This study showed no reduction in pain after hemorrhoidectomy with the use of topical Policresulen and cinchocaine.
New Treatment for Urethral Rent in Stallions
J Equine Vet Sci 2018 May;64:89-95.PMID:30973159DOI:10.1016/j.jevs.2018.02.014.
The aim of this report is to describe a new methodology to successfully treat stallions diagnosed with urethral rent. Four stallions of ages ranging from 7 to 12 years (median 9) with hemospermia were admitted for clinical evaluation, breeding soundness examination, and urethroscopy for inspection of the urethra and vesicular glands. Once the presence of urethral rent was identified and/or other sources of hemorrhage were excluded, a topical treatment was performed with 4% Policresulen solution (Albocresil). The treatment was carried out by infusing 100 mL of the solution into the lumen of the urethra through a catheter placed up to the region of the ischial arch. This procedure was repeated once daily, or at 48 hours intervals, resulting in a total of 4-7 infusions. In all cases, chemical cauterization was efficient in the healing of the urethral rent. However, due to masturbation during treatment, one animal did not completely heal, and the treatment with the Policresulen was prolonged. It is believed that the low pH of the solution resulted in urethritis, which was treated with systemic therapy of antibiotic and anti-inflammatory nonsteroidal. Topical treatment with 4% Policresulen was found to be efficient in the chemical cauterization of urethral rent in stallions. This treatment was efficient, practical, less invasive, and less costly than the alternative of surgical methods, which are more invasive and require longer recovery time of the animal. However, sexual rest and the elimination of sexual stimuli from the environment are essential management in association with this therapeutic method.