Verbascoside-Acteoside-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVerbascosideCat. No.: HY-N0021CAS No.: 61276-17-3Synonyms: Acteoside; Kusaginin; TJC160分式: CHO分量: 624.59作靶点: PKC作通路: Epigenetics; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO

2、: 6.3 mg/mL (10.09 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6011 mL 8.0053 mL 16.0105 mL5 mM 0.3202 mL 1.6011 mL 3.2021 mL10 mM 0.1601 mL 0.8005 mL 1.6011 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Verbascoside是从 Lantan

3、a camara 中得到的糖苷类物质，为 ATP 竞争性的 PKC 抑制剂，IC50 值为 25 M，具有抗肿瘤，抗炎，抗神经性疼痛等作。IC50 & Target PKC25 M (IC50)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Verbascoside acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 M. Verbascoside shows Kisof 22 and 28 M with respect to ATP and histone,

4、 respectively. Verbascoside has potent antitumor activityagainst L-1210 cells, with an IC50 of 13 M 1. Verbascoside (5, 10 M) suppresses 2,4-dinitrochlorobenzene (DNCB)-induced T cell costimulatory factors CD86 and CD54, proinflammatorycytokines, and NFB pathway activation in THP-1 cells 2.体内研究 Verb

5、ascoside (1%) reduces the overall scratching behavior incidence as well as the severity of the skinlesions in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD) mice model. Verbascoside alsoblocks DNCB-induced expression of proinflammatory cytokine TNF-, IL-6, and IL-4 mRNA in skin lesio

6、ns2. Verbascoside (50, 100 mg/kg, i.p.) does not modify chronic constriction injury (CCI)-induced coldallodynia. Verbascoside (200 mg/kg, i.p.) decreases hyper-sensitivity to cold stimulus, acetone, on day 3 inrats. Verbascoside also significantly reduces behavioral changes associated with neuropath

7、y. Moreover,Verbascoside decreases Bax and increases Bcl-2 on day 3 3.PROTOCOLCell Assay 1 The lymphocytic mouse leukemia L1210 cells (ATCC, CCL 219) are plated sparsely at 104 cells per well in24-well cluster plates in Dulbeccos modified Eagle medium containing 10% fetal calf serum, 4 mMglutamine,

8、100 U/mL penicillin, 100 g/mL streptomycin sulfate, and Verbascoside (solubilized in DMSO).After a 2-day incubation period at 37C in a humidified atmosphere (5% CO2 in air), growth is monitored bycounting cell numbers in a Coulter-counter. IC50 values are calculated on the basis of the linear regres

9、sionlines established for each compound tested 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 To induce atopic dermatitis (AD)-like symptoms, 2,4-dinitrochlorobenzene (DNCB) is used. Briefly, the dorsalhair of the mice i

10、s removed using an electronic clipper 2 days before DNCB treatment. An application of 200L of 1% DNCB (in acetone:olive oil = 4:1) is made to the shaved dorsal skin for sensitization. The repeatedchallenge is performed on the same site with 0.2% DNCB once every 3 days for about 2 weeks. The miceare

11、divided into 4 groups (n = 6 per group): (1) vehicle-treated controls, (2) DNCB-treated only, (3) 1%Verbascoside (in acetone:olive oil 4:1)-treated only, and (4) DNCB + 1% Verbascoside-treated group 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFE

12、RENCES1. Herbert JM, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C. J Nat Prod. 1991 Nov-Dec;54(6):1595-600.2. Li Y, et al. Verbascoside Alleviates Atopic Dermatitis-Like Symptoms in Mice via Its Potent Anti-Inflammatory Effect. Int Arch AllergyImmunol. 2018;175(4):220-230.3. Amin B, et al. The Effect of Verbascoside in Neuropathic Pain Induced by Chronic Constriction Injury in Rats. Phytother Res. 2016Jan;30(1):128-35.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChem