Vapreotide-RC160-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVapreotideCat. No.: HY-P0061CAS No.: 103222-11-3Synonyms: RC160; BMY 41606分式: CHNOS分量: 1131.37Sequence: Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7)Sequence Shortening: FCYWKVCW-NH2 (Disulfide bridge: Cys2-C

2、ys7)作靶點: Others作通路: Others儲存式: Protect from lightPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實驗 H2O : 60 mg/mL (53.03 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 0.8839 mL 4.4194 mL 8.8388 mL5 mM

3、0.1768 mL 0.8839 mL 1.7678 mL10 mM 0.0884 mL 0.4419 mL 0.8839 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Vapreotide是NK1R 的拮抗劑，其 IC50 值為 330 nM。IC50 & Target 330 nM (NK1R) 1.體外研究 Vapreotide attenuates the effect of SP on calci

4、um release in a concentration-dependent manner. Theconcentration required for Vapreotide to completely inhibit the effect of SP is about 100 times higher than thatrequired for the NK1R antagonist aprepitant. The effect of Vapreotide on cell proliferation is mediatedprimarily by SSTR2. In order to fu

5、rther establish the NK1R antagonist effect of Vapreotide, U373MG cells arepretreated with SSTR2 selective antagonist CYN followed by incubation with Vapreotide and SP stimulation.The results show that pretreatment with CYN does not reverse the inhibitory effect of Vapreotide on SP-stimulated IL-8 mR

6、NA expression. Vapreotide reduces HIV-1 replication in MDM as indicated by limited HIVgag mRNA expression compared to control MDM. In addition, SP treatment (10 M) reverses Vapreotideinhibition of HIV-1 replication in MDM. This observation indicates that the inhibition of HIV-1 replication byVapreot

7、ide is most likely due to its interaction with NK1R 1.PROTOCOLCell Assay 1 The HEK293-NK1R cells and U373MG cells are incubated with or without Vapreotide (0, 5, 10, 20 M) for 10minutes and then incubated with or without SP for 3 hours. In some experiments, cells are first incubated withCYN for 10 m

8、inutes, and then Vapreotide is added and incubated for an additional 10 minutes, followed bystimulation with SP for 3 hours. Mock treated cells are used as controls 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Spitsin S et al. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor.Neuroimmunomodulation. 2013;20(5):247-55.McePdfHeightCaution: Product has not been fully validated for medical appli