1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. ONO-RS-082

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.

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ONO-RS-082

ONO-RS-082 構造式

CAS 番号 : 99754-06-0

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 在庫あり
Solution
10 mM * 1 mL in DMSO USD 77 在庫あり
Solid
5 mg $70 在庫あり
10 mg $115 在庫あり
25 mg $216 在庫あり
50 mg $360 在庫あり
100 mg $540 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

ONO-RS-082 is an inhibitor of phospholipase A (PLA)[1]. ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM[2].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
3 3
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]
CHO EC50
3 3
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]
体外実験

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 Viability Assay[3]

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.
体内実験

In vivo long-term activation of KCNK3 by ONO-RS-082 (50 mg/kg/day; preventive treatment, day 0 to day 21) reduces the development of PH in the MCT-PH model[4].
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.
分子量

371.86

分子式

C21H22ClNO3

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(NC(/C=C/C2=CC=C(C=C2)CCCCC)=O)=C(C=C1)C(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6892 mL 13.4459 mL 26.8918 mL
5 mM 0.5378 mL 2.6892 mL 5.3784 mL
10 mM 0.2689 mL 1.3446 mL 2.6892 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    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 Corn oil, and mix evenly.

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.

  • Protocol 1

    Add each solvent one by one:  0.5% CMC-Na/0.1% Tween-80 in Saline water

    Solubility: 10 mg/mL (26.89 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  Cremophor EL

    Solubility: 25 mg/mL (67.23 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.31%

参考文献

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
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
ONO-RS-082
製品番号:
HY-123070
数量:
MCE 日本正規代理店: