RC-3095

Product NameRC-3095
CAS138147-78-1
MFC56H79N15O9
MW1106.32
EINECS
MOL File138147-78-1.mol

Chemical Properties

Boiling point	1547.9±65.0 °C(Predicted)
Density	1.274±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO
form	powder
pka	13.38±0.46(Predicted)
color	white
InChIKey	ZHNRKEKBKBWCMF-RWWZSYIDSA-N

Safety Information

WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist[1]. RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice[2].

Biochem/physiol Actions

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

in vivo

RC-3095 impairs aversive but not recognition memory in Wistar male rats^[1].
RC-3095 (0.3 mg/kg or 1 mg/kg; S.C.) shows anti-inflammatory effects in 2 experimental models of arthritis, collagen-induced arthritis (CIA) and antigen-induced arthritis (AIA)^[2].
Arthritic mice treated with RC-3095 show a significant reduction in the concentrations of IL-17, IL-1 , and TNF, and showed a diminished expression of GRPR^[2].

Animal Model:	Male Balb/c wild-type mice (weighing 18-25 gm) with AIA model; Male DBA/1J inbred mice (weighing 18-25 gm) with CIA model^[2]
Dosage:	1 mg/kg for AIA studies; 0.3 mg/kg or 1 mg/kg for CIA studies
Administration:	Injected SC twice a day for a total of 2 or 10 days for AIA studies; Administered SC twice a day for 10 days after the onset of the disease for CIA studies
Result:	Reduced neutrophil migration, mechanical hy pernociception, and proteoglycan loss in mice with AIA; Led to a significant reduction in arthritis clinical scores and the severity of disease in the CIA model.

References

[1] Roesler R, et al. 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. DOI:10.1016/j.ejphar.2003.12.011
[2] Oliveira PG, et al. Protective effect of RC-3095, an antagonist of the gastrin-releasing peptide receptor, in experimental arthritis. 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

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