UC-1728 (t-TUCB)
(Synonyms: t-TUCB) 目录号 : GC33883
UC-1728 (t-TUCB) 是一种有效的兔可溶性环氧化物水解酶 (sEH) 抑制剂，对兔肝脏的 IC50 为 2 nM。
Cas No.:948304-40-3
Sample solution is provided at 25 µL, 10mM.
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UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver.
Miotic, fixed pupils are observed in the treated eyes of both groups receiving LPS injections but the difference in pupillary light reflex scores is only significantly increased in the UC-1728/LPS treated group relative to the PBS group at 6 h post-injection[1]. Pretreatment with UC-1728 (t-TUCB) at 10 and 30 mg/kg, p.o., significantly prevents ISO induced increase in heart weight and elevation of CK-MB and LDH levels (p<0.05), indicating its cardioprotective effect against ISO induced cardiac injury. At 3 mg/kg, p.o. UC-1728 only shows significant protection against heart weight changes. Pretreatment with UC-1728 at 3, 10 and 30 mg/kg, p.o., significantly reduces the ISO induced infarct size (p<0.05) when compared to control. The calculated percentage reductions for these doses are found to by 15.90, 46.60 and 40.44%, respectively[2]. Inhibition of sEH with UC-1728 is associated with a significant improvement in pain scores in one horse with laminitis whose pain is refractory to the standard of care therapy. No adverse effects are noticed[3].
[1]. McLellan GJ, et al. Effect of a Soluble Epoxide Hydrolase Inhibitor, UC1728, on LPS-Induced Uveitis in the Rabbit. J Ocul Biol. 2016 Jan;4(1). [2]. Shrestha A, et al. Soluble epoxide hydrolase inhibitor, t-TUCB, protects against myocardial ischaemic injury in rats. J Pharm Pharmacol. 2014 Sep;66(9):1251-8. [3]. Guedes AG, et al. Use of a soluble epoxide hydrolase inhibitor as an adjunctive analgesic in a horse with laminitis. Vet Anaesth Analg. 2013 Jul;40(4):440-8.
Animal experiment: | Mice[1]Eighteen male SPF New Zealand White Rabbits (2.6-3.2 Kg) are randomly assigned to 3 groups of 6 rabbits each. Rabbits in group 1 have 20 μL sterile PBS intracamerally injected in the right eye (negative control) and all other rabbits receive 100 ng LPS in 20 μL of PBS. Groups 2 and 3 are treated with anti-inflammatory drug or vehicle once daily on the following schedule: 24 h prior to intra-cameral LPS or PBS injection, the day of injection and 24 h post-injection. Group 2 receive UC-1728 (3 mg/kg, SC) and Group 3 receive PEG400 vehicle only (0.9 mL, subcutaneously, (SC)). To limit post-procedural discomfort, systemic buprenorphine (0.03 mg/kg SC) is administered immediately prior to returning rabbits to their cages upon recovery from anesthesia, then every 6-12 h for the first 24 h and as needed for the duration of the study[1]. |
References: [1]. McLellan GJ, et al. Effect of a Soluble Epoxide Hydrolase Inhibitor, UC1728, on LPS-Induced Uveitis in the Rabbit. J Ocul Biol. 2016 Jan;4(1). | |
| Cas No. | 948304-40-3 | SDF | |
| 别名 | t-TUCB | ||
| Canonical SMILES | O=C(O)C1=CC=C(O[C@H]2CC[C@H](NC(NC3=CC=C(OC(F)(F)F)C=C3)=O)CC2)C=C1 | ||
| 分子式 | C21H21F3N2O5 | 分子量 | 438.4 |
| 溶解度 | DMSO : 50 mg/mL (114.05 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.281 mL | 11.4051 mL | 22.8102 mL |
| 5 mM | 0.4562 mL | 2.281 mL | 4.562 mL |
| 10 mM | 0.2281 mL | 1.1405 mL | 2.281 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet