ChemicalBook CAS DataBase List 1217463-61-0

1217463-61-0

Name	RC-3095 (TFA)
CAS	1217463-61-0
Molecular Formula	C58H80F3N15O11
MDL Number	MFCD32215352
Molecular Weight	1220.37
MOL File	1217463-61-0.mol

Chemical Properties

storage temp.	-20°C, away from moisture
form	Solid
color	White to off-white

Hazard Information

Uses

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

Biological Activity

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

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. [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.

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