Tulopafant (RP 59227)
(Synonyms: 妥洛帕泛; RP 59227) 目录号 : GC32541
Tulopafant (RP 59227) 是一种血小板活化因子 (PAF) 拮抗剂。
Cas No.:116289-53-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tulopafant is a platelet activating factor (PAF) antagonist.
Preincubation of neutrophils with Tulopafant (RP 59227) results in a concentration-dependent decrease in chemiluminescence produced by PAF primed cells[1].
Tulopafant (RP 59227) effectively reduces myocardial infarct size and reduces the incidence of ischemia and reperfusion-induced arrhythmias in barbital-anesthetized dogs[1].Histological examination reveals marked diminution of both interstitial hemorrhage and deposition of platelet and granulocytes in capillaries of cardiac xenografts when recipient animals are pretreated with Tulopafant[2].
[1]. Auchampach JA, et al. Effect of the platelet-activating factor antagonist RP 59227 (Tulopafant) on myocardial ischemia/reperfusion injury and neutrophil function. Basic Res Cardiol. 1998 Oct;93(5):361-71. [2]. O'Hair DP, et al. Tulopafant, a PAF receptor antagonist, increases capillary patency and prolongs survival in discordant cardiac xenotransplants. J Lipid Mediat. 1993 May;7(1):79-84.
| Cas No. | 116289-53-3 | SDF | |
| 别名 | 妥洛帕泛; RP 59227 | ||
| Canonical SMILES | O=C(C(C=C1)=C2N1C(C3=CC=CN=C3)SC2)NC4=CC=CC(C(C5=CC=CC=C5)=O)=C4 | ||
| 分子式 | C25H19N3O2S | 分子量 | 425.5 |
| 溶解度 | Soluble in DMSO | 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 | 2.3502 mL | 11.7509 mL | 23.5018 mL |
| 5 mM | 0.47 mL | 2.3502 mL | 4.7004 mL |
| 10 mM | 0.235 mL | 1.1751 mL | 2.3502 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。
Effect of the platelet-activating factor antagonist RP 59227 (Tulopafant) on myocardial ischemia/reperfusion injury and neutrophil function
Basic Res Cardiol 1998 Oct;93(5):361-71.PMID:9833148DOI:10.1007/s003950050104.
The effect of the platelet activating factor antagonist RP 59227 (Tulopafant) on myocardial infarct size was compared to that of a vehicle-treated control group in barbital-anesthetized dogs subjected to 90 min of left circumflex coronary artery occlusion and 5 h of reperfusion. The myocardial region at risk and infarct size were determined by the triphenyltetrazolium histochemical technique and regional myocardial blood flow by radioactive microspheres. Myeloperoxidase (MPO) activity was used as an index of neutrophil infiltration into the ischemic-reperfused area. Vehicle (n = 11) or RP 59227 (n = 12, 2.5 mg/kg i.v.) were administered 15 min prior to occlusion. Hemodynamics and regional myocardial blood flow in the ischemic-reperfused areas did not differ between the two groups throughout the experiment. In contrast, the number of dogs which developed ventricular fibrillation during occlusion and reperfusion was significantly less in RP 59227-treated dogs (8 of 11 in the control group vs. 3 of 12 in the RP 59227-treated group, p < 0.05). Myocardial infarct size expressed as a percent of the area at risk (control, 39.0 +/- 5.0; RP 59227, 24.8 +/- 3.4%) or as a percent of the left ventricle (control, 15.3 +/- 1.9; RP 59227, 9.0 +/- 1.3%) was significantly smaller in the RP 59227-treated group. Infarct size was inversely related to the collateral blood flow in the inner two thirds of the left ventricular wall of the infarct area, and this relationship was shifted downward in the RP 59227-treated group (p < 0.05). MPO activity in the border zone immediately adjacent to infarcted tissue was reduced in the RP 59227-treated dogs (control, 7.4 +/- 0.5 U/g; RP 59227, 4.1 +/- 0.4 U/g). In additional in vitro studies, the addition of PAF was found to elicit a concentration-dependent potentiation in chemiluminescence produced by purified canine neutrophils, a measure of oxygen-derived free radicals, which was stimulated with a low concentration of opsonized zymosan. Preincubation of neutrophils with RP 59227 resulted in a concentration-dependent decrease in chemiluminescence produced by PAF primed cells. Taken together, these data demonstrate that RP 59227 effectively reduces myocardial infarct size and reduces the incidence of ischemia and reperfusion-induced arrhythmias in barbital-anesthetized dogs, and support the concept that PAF plays an important role in the pathogenesis of acute myocardial infarction.
Tulopafant, a PAF receptor antagonist, increases capillary patency and prolongs survival in discordant cardiac xenotransplants
J Lipid Mediat 1993 May;7(1):79-84.PMID:8395256doi
Hyperacute rejection is a serious complication of xenogeneic organ transplantation. It is believed that platelets play a pivotal role in this phenomenon. In this study, we provide the first known evidence of the efficacy of the PAF receptor antagonist, Tulopafant, in improvement in graft function and histology of discordant cardiac xenografts. Transplantation of guinea pig hearts into recipient rats resulted in hyperacute rejection. Pretreatment of recipient animals with Tulopafant (but not indomethacin) extended rejection time by 4-5-fold. Histological examination revealed marked diminution of both interstitial hemorrhage and deposition of platelet and granulocytes in capillaries of cardiac xenografts when recipient animals were pretreated with Tulopafant.