BMY 45778
目录号 : GC11820
partial agonist at IP1 prostacyclin receptors
Cas No.:152575-66-1
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
BMY 45778 is a partial agonist of prostacyclin receptor [1].
Prostacyclin receptor (IP1) is a G-protein coupled receptor for prostacyclin. Prostacyclin inhibits platelet aggregation and elicits a potent vasodilation through binding to this receptor.
BMY 45778 is a partial agonist of prostacyclin receptor. BMY 45778 inhibited platelet aggregation with IC50 values of 35 nM, 136 nM and 1.3 μM in human, rabbit and rat, respectively. In human platelet membrane, BMY 45778 activated adenylyl cyclase with ED50 value of 6-10 nM and stimulated GTPase. Also, BMY 45778 completely inhibited the binding of Iloprost to platelet membranes with IC50 value of 7 nM. BMY 45778 inhibited iloprost-stimulated GTPase, which suggested that BMY 45778 is a partial agonist of prostacyclin receptor. In whole platelets, BMY 45778 increased cAMP levels and activated cAMP-dependent protein kinase [1]. BMY 45778 (1-10 μM) inhibited rat neutrophil aggregation induced by N-formyl-methionyl-leucylphenylalanine with IC50 value of 20 nM and inhibited the spontaneous activity of rat colon by 10-20%. Also, BMY 45778(10 μM) inhibited the inhibitory effect of cicaprost on rat colon [2].
References:
[1]. Seiler SM, Brassard CL, Federici ME, et al. [3-[4-(4,5-Diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid (BMY 45778) is a potent non-prostanoid prostacyclin partial agonist: effects on platelet aggregation, adenylyl cyclase, cAMP levels, protein kinase, and iloprost binding. Prostaglandins, 1997, 53(1): 21-35.
[2]. Wise H, Qian YM, Jones RL. A study of prostacyclin mimetics distinguishes neuronal from neutrophil IP receptors. Eur J Pharmacol, 1995, 278(3): 265-269.
| Cas No. | 152575-66-1 | SDF | |
| 化学名 | 2-(3-(4,5-diphenyl-[2,4'-bioxazol]-5'-yl)phenoxy)acetic acid | ||
| Canonical SMILES | OC(COC1=CC(C2=C(C3=NC(C4=CC=CC=C4)=C(C5=CC=CC=C5)O3)N=CO2)=CC=C1)=O | ||
| 分子式 | C26H18N2O5 | 分子量 | 438.44 |
| 溶解度 | <21.92mg/ml 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 | 2.2808 mL | 11.4041 mL | 22.8081 mL |
| 5 mM | 0.4562 mL | 2.2808 mL | 4.5616 mL |
| 10 mM | 0.2281 mL | 1.1404 mL | 2.2808 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。