RC-3095
RC-3095 Basic information
- Product Name:
- RC-3095
- Synonyms:
-
- (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methylpentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(3R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl]amino]pentanediamide
- bombesin (6-14), Tpi(6)-Leu(13)-psi(CH2NH)-Leu(14)-
- (3R)-2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-Ψ(CH2-NH)-L-Leucinamide triflouroacetate salt, (D-Tpi6, Leu13Ψ(CH2-NH)-Leu14)bombesin (6-14), D-Tpi-Gln-Trp-Ala-Val-Gly-His-Y(CH2-NH)-Leu-NH2 trifluoroacetate salt trifluoroacetate salt
- (D-Tpi6, Leu13 Ψ(CH2-NH)-Leu14)bombesin (6-14)
- D-Tpi-Gln
- [1(R),6[S-(R*,R*)]]-N2-[(2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indol-3-yl)carbonyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-N-[1-[[[1-(aminocarbonyl)-3-methylbutyl]amino]methyl]-3-methylbutyl]-L-histidinamide
- RC3095;RC 3095
- L-Leucinamide, (3R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-ψ(CH2-NH)-
- CAS:
- 138147-78-1
- MF:
- C56H79N15O9
- MW:
- 1106.32
- Mol File:
- 138147-78-1.mol
RC-3095 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
RC-3095 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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