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。
| 生物活性 | RC-3095 TFA is a selectivebombesin/gastrinreleasing 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].
| 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 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(40.97 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.8194 mL | 4.0972 mL | 8.1944 mL | | 5 mM | 0.1639 mL | 0.8194 mL | 1.6389 mL | | 10 mM | 0.0819 mL | 0.4097 mL | 0.8194 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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