RC-3095 是一种蛙皮素 (bombesin)/胃泌素 (gastrin) 释放肽受体拮抗剂。RC-3095 作用于关节炎小鼠，通过减少胃氧化损伤来发挥保护作用。
| 生物活性 | RC-3095 is abombesin/gastrinreleasing peptide receptor (GRPR) antagonist[1]. RC-3095 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].
| 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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 (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>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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