CAS NO: | 103222-11-3 |
生物活性 | Vapreotide is aneurokinin-1 (NK1) receptorantagonist, with anIC50of 330 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (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[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 1131.37 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C57H70N12O9S2 | ||||||||||||||||
CAS 号 | 103222-11-3 | ||||||||||||||||
Sequence | Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7) | ||||||||||||||||
Sequence Shortening | FCYWKVCW-NH2 (Disulfide bridge: Cys2-Cys7) | ||||||||||||||||
中文名称 | 伐普肽 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 100 mg/mL(88.39 mM;Need ultrasonic) 配制储备液
* 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。 |
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