Vapreotide伐普肽,103222-11-3

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Vapreotide

CAS No. : 103222-11-3

MCE 国际站：Vapreotide

产品活性：Vapreotide 是 神经激肽-1 (NK1) 受体拮抗剂，其 IC₅₀ 值为 330 nM。

研究领域：GPCR/G Protein | Neuronal Signaling

作用靶点：Neurokinin Receptor

In Vitro: Vapreotide attenuates the effect of SP on calcium release in a concentration-dependent manner. The concentration required for Vapreotide to completely inhibit the effect of SP is about 100 times higher than that required for the NK1R antagonist aprepitant. The effect of Vapreotide on cell proliferation is mediated primarily by SSTR2. In order to further establish the NK1R antagonist effect of Vapreotide, U373MG cells are pretreated 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 mRNA expression. Vapreotide reduces HIV-1 replication in MDM as indicated by limited HIV gag mRNA expression compared to control MDM. In addition, SP treatment (10 μM) reverses Vapreotide inhibition of HIV-1 replication in MDM. This observation indicates that the inhibition of HIV-1 replication by Vapreotide is most likely due to its interaction with NK1R.

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