RC3095 | CAS#138147-78-1 | MedKoo Biosciences

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RC-3095

Description RC-3095: RC-3095 is a bombesin/gastrin-releasing peptide (BN/GRP) antagonist with potential anticancer activity.

Current developer: AEterna Zentaris Inc。

MedKoo Code#: 202430

Name: RC-3095

CAS#: 138147-78-1

Synonym: RC3095; RC-3095.

Amino acid sequences: (D-TPI6, LEU13 y(CH2-NH)-LEU14)BOMBESIN (6-14).

IUPAC/Chemical name:

(S)-N1-((2S,5S,8S,14S,17S,20S)-14-((1H-imidazol-5-yl)methyl)-20-carbamoyl-1-(1H-indol-3-yl)-17-isobutyl-8-isopropyl-5,22-dimethyl-3,6,9,12,15-pentaoxo-4,7,10,13,16,19-hexaazatricosan-2-yl)-2-((R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamido)pentanediamide

Chemical structure:

Theoretical analysis

Chemical Formula: C56H79N15O9

Exact Mass: 1105.61852

Molecular Weight: 1106.32

Elemental Analysis: C, 60.80; H, 7.20; N, 18.99; O, 13.02

Availability and price:

This agent is not in stock, which may be available through custom synthesis.

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Quality control data:

Product will be shipped with supporting analytical data.

Information about this agent

RC-3095 is a potent BB2 (GRP-preferring) bombesin receptor antagonist.

References

1: Oliveira PG, Grespan R, Pinto LG, Meurer L, Brenol JC, Roesler R, Schwartsmann G, Cunha FQ, Xavier RM. Protective effect of RC-3095, an antagonist of the gastrin-releasing peptide receptor, in experimental arthritis. Arthritis Rheum. 2011 Oct;63(10):2956-65. doi: 10.1002/art.30486. PubMed PMID: 21953084.

2: Merali Z, Mountney C, Kent P, Anisman H. Effects of intracerebral ventricular administration of gastrin-releasing peptide and its receptor antagonist RC-3095 on learned fear responses in the rat. Behav Brain Res. 2011 Jan 20;216(2):519-24. doi: 10.1016/j.bbr.2010.08.027. Epub 2010 Aug 27. PubMed PMID: 20801162.

3: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL, Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects of N-acetylcysteine/deferoxamine, taurine and RC-3095 on respiratory chain complexes and creatine kinase activities in rat brain after sepsis. Neurochem Res. 2010 Apr;35(4):515-21. doi: 10.1007/s11064-009-0089-3. PubMed PMID: 20238483.

4: Sotomayor S, Muñoz-Moreno L, Carmena MJ, Schally AV, Sánchez-Chapado M, Prieto JC, Bajo AM. Regulation of HER expression and transactivation in human prostate cancer cells by a targeted cytotoxic bombesin analog (AN-215) and a bombesin antagonist (RC-3095). Int J Cancer. 2010 Oct 15;127(8):1813-22. doi: 10.1002/ijc.25192. PubMed PMID: 20099275.

5: Damin DC, Santos FS, Heck R, Rosito MA, Meurer L, Kliemann LM, Roesler R, Schwartsmann G. Effects of the gastrin-releasing peptide antagonist RC-3095 in a rat model of ulcerative colitis. Dig Dis Sci. 2010 Aug;55(8):2203-10. doi: 10.1007/s10620-009-1032-9. Epub 2009 Nov 6. PubMed PMID: 19894117.

6: de Oliveira MS, Cechim G, Braganhol E, Santos DG, Meurer L, de Castro CG Jr, Brunetto AL, Schwartsmann G, Battastini AM, Lenz G, Roesler R. Anti-proliferative effect of the gastrin-release peptide receptor antagonist RC-3095 plus temozolomide in experimental glioblastoma models. J Neurooncol. 2009 Jun;93(2):191-201. doi: 10.1007/s11060-008-9775-2. Epub 2009 Jan 8. Erratum in: J Neurooncol. 2009 Jun;93(2):203. Schwarstmann, Gilberto [corrected to Schwartsmann, Gilberto]. PubMed PMID: 19129973.

7: Dantas Ados S, Luft T, Henriques JA, Schwartsmann G, Roesler R. Opposite effects of low and high doses of the gastrin-releasing peptide receptor antagonist RC-3095 on memory consolidation in the hippocampus: possible involvement of the GABAergic system. Peptides. 2006 Sep;27(9):2307-12. Epub 2006 May 2. PubMed PMID: 16650508.

8: Martins MR, Reinke A, Valvassori SS, Machado RA, Quevedo J, Schwartsmann G, Roesler R. Non-associative learning and anxiety in rats treated with a single systemic administration of the gastrin-releasing peptide receptor antagonist RC-3095. Peptides. 2005 Dec;26(12):2525-9. Epub 2005 Jul 14. PubMed PMID: 16023260.

9: Pereira AS, DiLeone L, Souza FH, Lilla S, Richter M, Schwartsmann G, De Nucci G. Quantification of the bombesin/gastrin releasing peptide antagonist RC-3095 by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 25;816(1-2):321-6. PubMed PMID: 15664365.

10: Meller CA, Henriques JA, Schwartsmann G, Roesler R. The bombesin/gastrin releasing peptide receptor antagonist RC-3095 blocks apomorphine but not MK-801-induced stereotypy in mice. Peptides. 2004 Apr;25(4):585-8. PubMed PMID: 15165713.

11: Roesler R, Kopschina MI, Rosa RM, Henriques JA, Souza DO, Schwartsmann G. RC-3095, a bombesin/gastrin-releasing peptide receptor antagonist, impairs aversive but not recognition memory in rats. Eur J Pharmacol. 2004 Feb 13;486(1):35-41. PubMed PMID: 14751406.

12: Roesler R, Meller CA, Kopschina MI, Souza DO, Henriques JA, Schwartsmann G. Intrahippocampal infusion of the bombesin/gastrin-releasing peptide antagonist RC-3095 impairs inhibitory avoidance retention. Peptides. 2003 Jul;24(7):1069-74. PubMed PMID: 14499286.

13: Chatzistamou I, Schally AV, Szepeshazi K, Groot K, Hebert F, Arencibia JM. Inhibition of growth of ES-2 human ovarian cancers by bombesin antagonist RC-3095, and luteinizing hormone-releasing hormone antagonist Cetrorelix. Cancer Lett. 2001 Sep 28;171(1):37-45. PubMed PMID: 11485826.

14: Kahán Z, Sun B, Schally AV, Arencibia JM, Cai RZ, Groot K, Halmos G. Inhibition of growth of MDA-MB-468 estrogen-independent human breast carcinoma by bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II. Cancer. 2000 Mar 15;88(6):1384-92. PubMed PMID: 10717621.

15: Koppán M, Halmos G, Arencibia JM, Lamharzi N, Schally AV. Bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II inhibit tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma. Cancer. 1998 Oct 1;83(7):1335-43. PubMed PMID: 9762934.

16: Miyazaki M, Lamharzi N, Schally AV, Halmos G, Szepeshazi K, Groot K, Cai RZ. Inhibition of growth of MDA-MB-231 human breast cancer xenografts in nude mice by bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095. Eur J Cancer. 1998 Apr;34(5):710-7. PubMed PMID: 9713279.

17: Szepeshazi K, Schally AV, Halmos G, Lamharzi N, Groot K, Horvath JE. A single in vivo administration of bombesin antagonist RC-3095 reduces the levels and mRNA expression of epidermal growth factor receptors in MXT mouse mammary cancers. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10913-8. PubMed PMID: 9380734; PubMed Central PMCID: PMC23529.

18: Halmos G, Schally AV. Reduction in receptors for bombesin and epidermal growth factor in xenografts of human small-cell lung cancer after treatment with bombesin antagonist RC-3095. Proc Natl Acad Sci U S A. 1997 Feb 4;94(3):956-60. PubMed PMID: 9023364; PubMed Central PMCID: PMC19621.

19: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K. Somatostatin analogues and bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. Cancer Res. 1994 Nov 15;54(22):5895-901. PubMed PMID: 7954420.

20: Pinski J, Halmos G, Yano T, Szepeshazi K, Qin Y, Ertl T, Schally AV. Inhibition of growth of MKN45 human gastric-carcinoma xenografts in nude mice by treatment with bombesin/gastrin-releasing-peptide antagonist (RC-3095) and somatostatin analogue RC-160. Int J Cancer. 1994 May 15;57(4):574-80. PubMed PMID: 7910153.

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