Detail introduction: Vapratide/valprotide/RC-160/103222-11-3
| English name | Vapratide |
| CAS NO | 103222-11-3 |
| Peptide sequence | DPhe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2(Cys2&Cys7 bridge） |
| Molecular formula | C57H70N12O9S2 |
| Molecular weight | 1131.37 |
| storage temperature | 2-8℃ |
| purity | ≥98% |
| Package | 1mg;5mg;10mg;50mg;100mg,1g or according to customer’s detail requirement. |
| Product English synonyms | RC-160;D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Trp-NH2 (Disulfide bridge Cys2-Cys7) |
A brief introduction of valprotide
Valprotide (trade name SanvarIR, formerly name: RC – 160). H3Pharma has acquired a global research development and a commercial license for Valprotide from Debiopharm of Switzerland. New England Journal of Medicine, 2001
Chemical book is an early treatment for acute esophageal variceal hemorrhage (EVB) and hemostasis prior to endoscopic intervention and can prevent bleeding recurrence within 5 days after endoscopic treatment.
In 2004, H3Pharma, a Canadian cancer and endocrinology specialist, developed and manufactured the drug.
Pharmacological action
SST plays its role through the somatostatin receptor (SSTR). The somatostatin receptor G protein-coupled receptor family is a family of glycoproteins with seven transmembrane segments, including SSTR5 subtypes, which can be further divided into SSTRI and SSTR and SSTR, SSTR3, and SSTR according to their affinity for ligands.
Studies have shown that valprotide has high affinity with SSTR and SSTR subtypes, and the mechanism of action is mainly manifested in direct and indirect effects.
Direct action By binding to a specific SSTR, SSTR is activated and acts directly through the following information transduction pathways.
1. Bind adenylate cyclase and inhibit its active Chemicalbook force, thereby reducing the content of cAMP in tumor cells that promotes cell proliferation;
2, make cell membrane hyperpolarized, promote K+ influx, inhibit extracellular Ca2+ influx, reduce intracellular Ca2+ concentration;
3. Activate protein phosphatase, which inhibits DNA and protein synthesis, interferes with cell cycle [5], and inhibits tumor cell proliferation. Indirect effects of various growth factors and gastrointestinal hormones such as epidermal growth factor (EGF), growth hormone (GH), insulin-like growth factor (IGF-1), cholecystokinin (CCK), gastrin can stimulate tumor growth. It indirectly inhibits tumor growth by inhibiting the release of these growth factors and binding to SSTR of normal cells in the host.
Future development of valprotide
It has a long biological half-life, is easy to use, has a wide range of anti-tumor effects, has little toxic and side effects, and can play a better anti-tumor effect. The current study has achieved good results, but due to the lack of multi-center, large sample and prospective controlled studies, its efficacy needs to be further evaluated.
The further development and application of highly effective and specific SST derivatives, a radioactive SST derivative, will provide new targets for the diagnosis and treatment of gynecological tumors.
At present, radio-labeled targeted radiotherapy mediated by valprotide has been applied in the clinical treatment of some GEP tumors, but the research on solid tumors is basically blank at present. Therefore, radiotherapy for solid tumors of digestive system will be one of the directions of future research.
How to buy Vapratide in the U. S.
Peptide supplier Remetide specializes in the production and sales of peptides in the USA, as well as Professional Drug peptide R&D. Feel free to contact us if you have any questions or inquiries about Vapratide Peptides.