Ketorolac tromethamine salt
(Synonyms: 酮咯酸氨丁三醇; Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt) 目录号 : GC16594
An NSAID and COX inhibitor
Cas No.:74103-07-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
HEL, Mono Mac 6 and RAW 264.7 cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.025 ~ 300 μM |
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Applications |
In HEL cells (COX-1) and LPS-induced Mono Mac 6 cells (COX-2), Ketorolac tromethamine salt inhibited eicosanoid formation with the IC50 value of 0.025 μM and 0.039 μM, respectively. However, in supernatants of LPS-induced RAW 264.7 cells, it did not significantly inhibit NO accumulation at the dose up to 300 μM. |
| Animal experiment [2]: | |
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Animal models |
Male Wistar rats |
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Dosage form |
0.3 ~ 30 mg/kg; p.o. |
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Applications |
At all doses, Ketorolac tromethamine salt significantly inhibited COX-1 activity and gastric PG synthesis. At the doses ≥ 1 mg/kg, Ketorolac tromethamine salt inhibited COX-1 activity by 95% and gastric PG synthesis by > 88%, without causing obvious gastric damage. At the dose ≤ 3 mg/kg, Ketorolac tromethamine salt did not significantly affect COX-2 activity, but at the doses of 10 and 30 mg/kg, it inhibited COX-2 activity by 75% and 91%, respectively. Meanwhile, it caused significant gastric damage as well. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Berg J, Fellier H, Christoph T, Grarup J, Stimmeder D. The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro. Inflamm Res. 1999 Jul;48(7):369-79. [2]. Wallace JL, McKnight W, Reuter BK, Vergnolle N. NSAID-induced gastric damage in rats: requirement for inhibition of both cyclooxygenase 1 and 2. Gastroenterology. 2000 Sep;119(3):706-14. | |
Ketorolac tromethamine salt (RS37619 tromethamine salt) is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1].
Ketorolac tromethamine (0.4%) causes nearly complete inhibition on LPS endotoxin-induced increases in FITC-dextran in the anterior chamber, and increases in aqueous PGE2 concentrations in the aqueous humor in rabbits[1].Ketorolac (30 mg/kg, i.v.) rapidly reverses hyperalgesia in rats. Ketorolac also reduces carrageenan-induced hyperalgesia and paw PG production, and causes reduction in PGE2 levels in rats[1]. Ketorolac (4 mg/kg/day, p.o.) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats[2]. Ketorolac (60 μg/10 μL) reduces the histological changes such as ischemic cell death, including cytoplasmic eosinophilia with disintegration of cytoarchitecture and nuclear pyknosis in rats. Ketorolac also effectively reduces neuronal death and improves hindlimb motor function, and the long-term survival is similar to that in the control group[3].
References:
[1]. Waterbury LD, et al. Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40.
[2]. Fracon RN, et al. Treatment with paracetamol, ketorolac or etoricoxib did not hinder alveolar bone healing: a histometric study in rats. J Appl Oral Sci. 2010 Dec;18(6):630-4.
[3]. Hsieh YC, et al. Intrathecal ketorolac pretreatment reduced spinal cord ischemic injury in rats. Anesth Analg. 2005 Apr;100(4):1134-9.
| Cas No. | 74103-07-4 | SDF | |
| 别名 | 酮咯酸氨丁三醇; Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt | ||
| 化学名 | 2-amino-2-(hydroxymethyl)propane-1,3-diol;5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid | ||
| Canonical SMILES | C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O | ||
| 分子式 | C19H24N2O6 | 分子量 | 376.4 |
| 溶解度 | ≥ 13.1mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6567 mL | 13.2837 mL | 26.5675 mL |
| 5 mM | 0.5313 mL | 2.6567 mL | 5.3135 mL |
| 10 mM | 0.2657 mL | 1.3284 mL | 2.6567 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。