ONO-RS-082
Based on 1 Customer Validation
ONO-RS-082 is an inhibitor of phospholipase A (PLA). ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.31%
- CAS No.: 99754-06-0
- Formule: C21H22ClNO3
- Masse moléculaire:371.86
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Covalent Screening Library
HY-L036
-
Lipid Metabolism Compound Library
HY-L091
-
Metabolic Enzyme Compound Library
HY-L146
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Voir tous les produits spécifiques à Isoform Phospholipase
More
Activité biologique
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
3 μM
Compound: 8
|
Activation of human TREK1 expressed in CHO cells assessed as increase in channel currents at +50 mV relative to control
Activation of human TREK1 expressed in CHO cells assessed as increase in channel currents at +50 mV relative to control
|
[PMID: 26588045] |
ONO-RS-082 (10 μM) prevents P. aeruginosa strain PAO1-induced polymorphonumclear cells (PMNs) transepithelial migration, demonstrating that PLA2 activity is crucial to this process[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549 lung epithelial cell lines
-
Concentration:10 μM
-
Incubation Time:2-h pretreatment
-
Result:Completely blocked HXA3-mediated PAO1-induced PMN transepithelial migration. Largely prevented PAO1-induced PGE2 release.
In contrast, in vivo short-term KCNK3 activation by ONO-RS-082 (curative treatment) fails to reduce PH symptoms, which is attributed to the complete loss of KCNK3 expression in MCT-PH rats at days 14 to 21[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MCT- pulmonary hypertension (PH) rat model[4]
-
Dosage:50 mg/kg/day
-
Administration:
-
Result:Reduced the development of PH in the MCT-PH model for long-term.
Chemical Information
-
CAS No. 99754-06-0
-
Appearance Solid
-
Masse moléculaire 371.86
-
Formule C21H22ClNO3
-
Color White to off-white
-
SMILES
ClC1=CC(NC(/C=C/C2=CC=C(C=C2)CCCCC)=O)=C(C=C1)C(O)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (268.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.72 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Cremophor EL
Solubility: 25 mg/mL (67.23 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (272 KB)
-
SDS (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. H S Banga,et al. Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine. Proc Natl Acad Sci U S A.1986 Dec;83(23):9197-201. [Content Brief]
[2]. H Ohno, et al. Effect of phospholipase A2 inhibitors on mouse T lymphocytes. I. Phospholipase A2 inhibitors exert similar immunological activities as glycosylation inhibiting factor. Int Immunol. 1989;1(4):425-33. [Content Brief]
[3]. Bryan P Hurley, et al. Selective eicosanoid-generating capacity of cytoplasmic phospholipase A2 in Pseudomonas aeruginosa-infected epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2011 Feb;300(2):L286-94. [Content Brief]
[4]. Hélène Le Ribeuz, et al. Implication of Potassium Channels in the Pathophysiology of Pulmonary Arterial Hypertension. Biomolecules. 2020 Sep 1;10(9):1261. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL | 67.2296 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | 13.4459 mL | |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL | 6.7230 mL | |
| 15 mM | 0.1793 mL | 0.8964 mL | 1.7928 mL | 4.4820 mL | |
| 20 mM | 0.1345 mL | 0.6723 mL | 1.3446 mL | 3.3615 mL | |
| 25 mM | 0.1076 mL | 0.5378 mL | 1.0757 mL | 2.6892 mL | |
| 30 mM | 0.0896 mL | 0.4482 mL | 0.8964 mL | 2.2410 mL | |
| 40 mM | 0.0672 mL | 0.3361 mL | 0.6723 mL | 1.6807 mL | |
| 50 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3446 mL | |
| 60 mM | 0.0448 mL | 0.2241 mL | 0.4482 mL | 1.1205 mL | |
| 80 mM | 0.0336 mL | 0.1681 mL | 0.3361 mL | 0.8404 mL | |
| 100 mM | 0.0269 mL | 0.1345 mL | 0.2689 mL | 0.6723 mL |
ONO-RS-082 Related Classifications
HY-123070 Related Classifications
Powered by Bioz