Vapreotide(Synonyms: RC160 BMY 41606)

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Vapreotide;(Synonyms: RC160; BMY 41606) 纯度: 98.75%

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

Vapreotide (Synonyms: RC160; BMY 41606)

Vapreotide Chemical Structure

CAS No. : 103222-11-3

规格 价格 是否有货 数量
10;mM;*;1 mL in Water ￥3485 In-stock
1 mg ￥1100 In-stock
5 mg ￥2200 In-stock
10 mg ￥2800 In-stock
50 mg ￥6000 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

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生物活性

Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.

IC50 & Target

330 nM (NK1R)[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

1131.37

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

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro:;

H2O : 100 mg/mL (88.39 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8839 mL 4.4194 mL 8.8388 mL
5 mM 0.1768 mL 0.8839 mL 1.7678 mL
10 mM 0.0884 mL 0.4419 mL 0.8839 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；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, 6 months; -20°C, 1 month (protect from light)。-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。
参考文献

  • [1]. 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.
Cell Assay
[1]

The HEK293-NK1R cells and U373MG cells are incubated with or without Vapreotide (0, 5, 10, 20 μM) for 10 minutes and then incubated with or without SP for 3 hours. In some experiments, cells are first incubated with CYN for 10 minutes, and then Vapreotide is added and incubated for an additional 10 minutes, followed by stimulation 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.
参考文献

  • [1]. 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.