Omtriptolide
(Synonyms: 昂曲托来) 目录号 : GC33857
Omtriptolide(PG490-88)是从中草药纯化的雷公藤内酯的水溶性衍生物前药。
Cas No.:195883-06-8
Sample solution is provided at 25 µL, 10mM.
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Omtriptolide (PG490-88) is a water soluble derivative prodrug of triptolide purified from the Chinese herb.
Triptolide, a traditional Chinese medicine, has anti-inflammatory, antiproliferative, and proapoptotic properties[1].
In a mouse model of cisplatin-induced AKI, omtriptolide results in a significant decrease in blood urea nitrogen (BUN), serum creatinine, and acute tubular necrosis (ATN) score, and a nonsignificant increase in tubular apoptosis score in AKI. The protection of omtriptolide against AKI is associated with a decrease in p-ERK and is independent of MKP-1 and proinflammatory cytokines[1]. In a mouse heterotopic tracheal allograft model of obliterative airway disease, omtriptolide attenuates airway obliteration and inhibits accumulation of inflammatory cells, and therefore may have preventive or therapeutic benefits for patients with obliterative airway disease following lung transplantation[2]. Omtriptolide inhibits fibrosis in the bleomycin group when given the same day or 5 days after bleomycin. Omtriptolide also markedly reduces the number of myofibroblasts in the bleomycin treatment group[3]. Omtriptolide inhibits in vivo both CD4+Vbeta3+ and CD8+Vbeta3+ T cell (alloreactive T cells in this model) expansion in the spleen by 64.09 and 34.02%, respectively, at the time when Vbeta3+ cell expansion is in the logarithmic phase (day 3 after transplantation)[4].
[1]. Kim HJ, et al. The water-soluble triptolide derivative PG490-88 protects against cisplatin-induced acute kidney injury. J Pharmacol Exp Ther. 2014 Jun;349(3):518-25. [2]. Leonard CT, et al. PG490-88, a derivative of triptolide, attenuates obliterative airway disease in a mouse heterotopic tracheal allograft model. J Heart Lung Transplant. 2002 Dec;21(12):1314-8. [3]. Krishna G, et al. PG490-88, a derivative of triptolide, blocks bleomycin-induced lung fibrosis. Am J Pathol. 2001 Mar;158(3):997-1004. [4]. Chen BJ, et al. Prevention of graft-versus-host disease by a novel immunosuppressant, PG490-88, through inhibition of alloreactive T cell expansion. Transplantation. 2000 Nov 27;70(10):1442-7.
Animal experiment: | Mice: Omtriptolide (0.25 mg/kg per day) is started immediately after the transplant and 10 control mice receive intraperitoneal injections of sterile water each day. The mice are then maintained for 28 days until killing, at which time the mice are administered CO2 inhalation, and cervical dislocation is performed. Trachea is divided for histologic staining and immunohistochemistry [2]. |
References: [1]. Kim HJ, et al. The water-soluble triptolide derivative PG490-88 protects against cisplatin-induced acute kidney injury. J Pharmacol Exp Ther. 2014 Jun;349(3):518-25. | |
| Cas No. | 195883-06-8 | SDF | |
| 别名 | 昂曲托来 | ||
| Canonical SMILES | C[C@@]([C@@]1([H])C[C@@H]2O3)(CCC4=C1COC4=O)[C@]5([C@H]([C@H]6[C@]7(C(C)C)O6)O5)[C@]23[C@@H]7OC(CCC(O)=O)=O | ||
| 分子式 | C24H28O9 | 分子量 | 460.47 |
| 溶解度 | H2O : 1.39 mg/mL (3.02 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 | 2.1717 mL | 10.8585 mL | 21.7169 mL |
| 5 mM | 0.4343 mL | 2.1717 mL | 4.3434 mL |
| 10 mM | 0.2172 mL | 1.0858 mL | 2.1717 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