Vapreotide acetate salt

Modify Date: 2024-01-02 08:06:47

Vapreotide acetate salt structure	Common Name	Vapreotide acetate salt
	CAS Number	103222-11-3	Molecular Weight	1131.371
	Density	1.4±0.1 g/cm3	Boiling Point	1540.9±65.0 °C at 760 mmHg
	Molecular Formula	C₅₇H₇₀N₁₂O₉S₂	Melting Point	N/A
	MSDS	N/A	Flash Point	885.7±34.3 °C

Use of Vapreotide acetate salt

Vapreotide is a NK1R antagonist, with an IC50 of 330 nM. Sequence: Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2(Disulfide bridge: Cys2-Cys7).

Name	rc 160
Synonym	More Synonyms

Description	Vapreotide is a NK1R antagonist, with an IC50 of 330 nM. Sequence: Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2(Disulfide bridge: Cys2-Cys7).
Related Catalog	Signaling Pathways >> Others >> Others Peptides Research Areas >> Cancer
Target	330 nM (NK1R)[1].
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].
Cell Assay	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].
References	[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.

Density	1.4±0.1 g/cm3
Boiling Point	1540.9±65.0 °C at 760 mmHg
Molecular Formula	C₅₇H₇₀N₁₂O₉S₂
Molecular Weight	1131.371
Flash Point	885.7±34.3 °C
Exact Mass	1130.483032
PSA	401.24000
LogP	3.47
Vapour Pressure	0.0±0.3 mmHg at 25°C
Index of Refraction	1.699
Storage condition	−20°C

Safety Phrases	22-24/25

D-PHE-CYS-TYR-D-TRP-LYS-VAL-CYS-TRP-NH2

1H-indole-3-propanamide, α-[[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-1-oxo-3-phenylpropyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-7-(1-methylethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloeicos-4-yl]carbonyl]amino]-, (αS)-

H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2

Octastatin

(4R,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-16-(4-hydroxybenzyl)-13-(1H-indol-3-ylmethyl)-7-isopropyl-6,9,12,15,18-pentaoxo-19-(D-phenylalanylamino)-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide

Vapreotide Acetate

(4R,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxo-2-propanyl]-16-(4-hydroxybenzyl)-13-(1H-indol-3-ylmethyl)-7-isopropyl-6,9,12,15,18-pentaoxo-19-(D-phenylalanylamino)-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide

1H-Indole-3-propanamide, α-[[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-1-oxo-3-phenylpropyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-7-(1-methylethyl)-6,9,12 ,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloeicos-4-yl]carbonyl]amino]-, (αS)-

vapreotide

FCYWKVCW-NH2

(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-16-(4-hydroxybenzyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-(D-phenylalanylamino)-7-(propan-2-yl)-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide

RC-160

D-Phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-cysteinyl-L-tryptophanamide Cyclic (2®7)-Disulfide