BMY 45778 |
| رقم الكتالوجGC11820 |
partial agonist at IP1 prostacyclin receptors
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 152575-66-1
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 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 | ||
| Formula | C26H18N2O5 | M.Wt | 438.44 |
| الذوبان | <21.92mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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