化合物 Ketorolac hemicalcium T60496

Product Introduction
Bioactivity


英文名: Ketorolac hemicalcium

描述: Ketorolac (RS37619) hemicalcium 是一种非选择性的 COX 抑制剂，对 COX-1 的 IC50 为 20 nM，对 COX-2 的 IC50 为 120 nM。 Ketorolac hemicalcium 是一种非甾体类抗炎药 (NSAID)，可用作 0.5% 滴眼液，用于研究过敏性结膜炎、黄斑囊样水肿、术中瞳孔缩小和术后眼部炎症和疼痛等。 Ketorolac hemicalcium 也是一种可用于癌症研究的 DDX3 抑制剂 [1] [4]。

体外活性: Ketorolac (RS37619) salt (0-30 μM, 48 h) effectively kills the oral cancer cells [4]. Ketorolac salt (0-5 μM, 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells [4]. Ketorolac salt (0-2.5 μM, 0-16 h) inhibits the proliferation of oral cancer cells [4]. Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity [4]. Cell Viability Assay [4] Cell Line: HOK, SCC4, SCC9 and H357 cells Concentration: 0-30 μM Incubation Time: 48 h Result: Showed inhibition with IC 50 s of 2.6, 7.1 and 8.1 μM against H357, SCC4 and SCC9 cells, respectively. And the normal HOK cell line did not show any cell death effect. Cell Proliferation Assay [4] Cell Line: H357 Concentration: 0.5, 1.0, 1.5, 2.0 and 2.5 μM Incubation Time: 0, 8 and 16 h Result: Inhibited the proliferation. Western Blot Analysis [4] Cell Line: H357 Concentration: 1, 2.5 and 5 μM Incubation Time: 48 h Result: Significantly reduced DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin. Apoptosis Analysis [4] Cell Line: H357 Concentration: 2.5 and 5 μM Incubation Time: 48 h Result: Induced apoptosis.

体内活性: Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits [1]. Ketorolac (4 mg/kg/day, p.o.; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats [2]. Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats [3]. Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice [4]. Animal Model: New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation [1] Dosage: 50 μL ketorolac tromethamine ophthalmic solution 0.4% Administration: In eyes, twice, 2 hours and 1 hour before LPS challenge Result: Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE 2 concentrations in the aqueous humor. Animal Model: Male Wistar rats (400–450 g), spinal cord ischemia model [3] Dosage: 30 and 60 μg Administration: Intrathecal injection, 1 h before the ischemia induction for once Result: Significantly reduced the motor disturbances and improved the survival rate at 60 μg. Animal Model: BALB/c mice, oral carcinogenesis model [4] Dosage: 20 mg/kg and 30 mg/kg Administration: IP injection, two times in a week for 3 weeks Result: Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途