BAY 73-1449
目录号 : GC61581
BAY73-1449是一种选择性前列环素受体(prostacyclinreceptor,IP)的拮抗剂，在人HEL细胞和大鼠DRG的cAMP分析中具有很高的效价(IC50值小于0.1nM)。BAY73-1449可用于降血压的研究。
Cas No.:693790-96-4
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
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure[1].
BAY 73-1449 (0.1-1 mg/kg; i.v.) does not significantly reduce mesenteric inflow, but significantly reduces splenic shunt vessel outflow in rats[1].BAY 73-1449 (1-5 mg/kg, s.c. once daily for 7 d) has no effects on the degree of porto-systemic shunting in rats[1].BAY 73-1449 (1 mg/kg, s.c. once daily for 7 d), has no effects on portal pressures in rats[1]. Animal Model: Male Wistar rats (250-350 g) are ligated portal vein[1]
[1]. Bexis S, et, al. Vascular actions of the prostacyclin receptor antagonist BAY 73-1449 in the portal hypertensive rat. Eur J Pharmacol. 2008 Aug 20;590(1-3):322-6.
| Cas No. | 693790-96-4 | SDF | |
| Canonical SMILES | O=C(O)[C@@H](CC1=CC=CC=C1)NC2=NC=NC(C3=CC=C(OCC4=CC=CC=C4)C=C3)=C2 | ||
| 分子式 | C26H23N3O3 | 分子量 | 425.48 |
| 溶解度 | DMSO: 250 mg/mL (587.57 mM) | 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 | 2.3503 mL | 11.7514 mL | 23.5029 mL |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL |
| 10 mM | 0.235 mL | 1.1751 mL | 2.3503 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。
Vascular actions of the prostacyclin receptor antagonist BAY 73-1449 in the portal hypertensive rat
Eur J Pharmacol 2008 Aug 20;590(1-3):322-6.PMID:18603238DOI:10.1016/j.ejphar.2008.06.006
We have investigated the actions of the postacyclin receptor antagonist BAY 73-1449 on shunt vessel development and shunt flow in the portal vein ligated portal hypertensive Wistar rat in vivo. BAY 73-1449 (0.1-1 mg/kg), given intravenously, did not significantly reduce mesenteric inflow, but significantly reduced splenic shunt vessel outflow, compared to the effects of vehicle, in anaesthetized portal vein ligated rats as measured by shunt vessel conductance. There were no differences between portal vein ligated animals treated, beginning just before portal vein ligation, with vehicle for 7 days and animals treated for 7 days with BAY 73-1449 (1-5 mg/kg, s.c.) in the degree of porto-systemic shunting, as measured by the radioactive microsphere technique in anaesthetized rats. Portal pressure was similar in animals treated with vehicle or BAY 73-1449. It is concluded that the prostacyclin receptor antagonist BAY 73-1449 can acutely reduce shunt vessel blood flow in portal hypertensive rats.