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Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

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| 50 mg | Inquiry | Inquiry | Inquiry | |
| 100 mg | Inquiry | Inquiry | Inquiry |
| Description | Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM). |
| Targets&IC50 | NK1R:330 nM |
| In vitro | In a concentration-dependent manner, Vapreotide attenuates the effect of SP on calcium release . 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. As compared to control MDM, limited HIV gag mRNA expression may indicate that Vapreotide can reduce HIV-1 replication in MDM. In addition, SP treatment (10 μM) reversed the inhibitory effect of pentoprofen on HIV-1 replication in MDM. This observation indicates that the inhibitory effect of Vapreotide on HIV-1 replication is most likely due to its interaction with NK1R. |
| Synonyms | RC160, BMY 41606 |
| Molecular Weight | 1131.38 |
| Formula | C57H70N12O9S2 |
| Cas No. | 103222-11-3 |
| Smiles | [H][C@@]1(Cc2ccc(O)cc2)NC(=O)[C@H](CSSC[C@H](NC(=O)C(NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)NC(=O)[C@H](N)Cc1ccccc1 |@:49| |
| Relative Density. | 1.4 g/cm3 |
| Sequence | {d-Phe}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7) |
| Sequence Short | {d-Phe}-CY-{d-Trp}-KVCW (Disulfide bridge: Cys2-Cys7) |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | H2O: 60 mg/mL (53.03 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
H2O
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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