RC-3095 TFA

发表于由

RC-3095 TFA; 纯度: 97.18%

RC-3095 TFA 是一种选择性蛙皮素 (bombesin)/胃泌素 (gastrin) 释放肽受体拮抗剂。RC-3095 TFA 作用于关节炎小鼠，通过减少胃氧化损伤来发挥保护作用。

RC-3095 TFAamp;;

RC-3095 TFA Chemical Structure

CAS No. : 1217463-61-0

规格 价格 是否有货 数量
1 mg ￥4400 In-stock
5 mg ￥9800 In-stock
10 mg ￥15500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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RC-3095 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

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].

IC50 Target

Bombesin receptor; GRPR[1]
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.

分子量

1220.34

Formula

C58H80F3N15O11
CAS 号

1217463-61-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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.
参考文献

  • [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.