| 生物活性 |
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].
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IC50 Target |
Bombesin receptor; GRPR[1]
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体内研究
(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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Sealed storage, away from moisture
| Powder |
-80deg;C |
2 years |
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-20deg;C |
1 year |
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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| Solvent Solubility |
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
| ; |
Contents |
Assign value |
| Acidic amino acid |
Asp (D), Glu (E), and the C-terminal -COOH. |
-1 |
| Basic amino acid |
Arg (R), Lys (K), His (H), and the N-terminal -NH2 |
+1 |
| Neutral amino acid |
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) |
0 |
3.;;Recommended solution:
| Overall charge of peptide |
Details |
| Negative (lt;0) |
1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (gt;0) |
1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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| 参考文献 |
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[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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