Referencia número: HY-12383

Pelubiprofen

Revisión del cliente

Based on 1 Customer Validation

Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC₅₀ values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 98.46%
No. CAS: 69956-77-0
Fòrmula: C₁₆H₁₈O₃
Peso molecular:258.31

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pelubiprofen Chemical Structure

No. CAS: 69956-77-0

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Precio

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Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

COX-2

TAK1

Ver todos los productos específicos de isoformas COX :

Ver todos los productos específicos de isoformas NF-κB :

Ver todos los productos específicos de isoformas NO Synthase :

Ver todos los productos específicos de isoformas IKK :

Ver todos los productos específicos de isoformas MAP3K :

In Vitro

Pelubiprofen (0.01-60 μM, 24 h) inhibits COX in RAW 264.7 cells and suppresses LPS (HY-D1056)-induced PGE2 (IC₅₀ is 0.13 μM)^[1].
Pelubiprofen (15-60 μM, 24 h) inhibits the expression of iNOS and pro-inflammatory cytokines induced by LPS (HY-D1056) in RAW 264.7 cells^[1].
Pelubiprofen (15-60 μM, 24 h) suppresses the activation of NF-κB induced by LPS (HY-D1056) in RAW 264.7 cells^[1].
Pelubiprofen (15-60 μM, 24 h) inhibits IKK and TAK1 in RAW 264.7 cells induced by LPS (HY-D1056)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

RAW 264.7
Concentration:

0.01, 0.1, 1, 5, 15, 30, 60 μM
Incubation Time:

24h; 5 and 10 min
Result:

Inhibited the expression of COX-2 and PGE2, without affecting COX-1. Suppressed the expression of iNOS and reduced the levels of TNF-α, IL-1b, and IL-6.
Decreased the phosphorylation and degradation of IκB-α, inhibiting IKK and TAK1.

Real Time qPCR^[1]

Cell Line:

RAW 264.7
Concentration:

15, 30, 60 μM
Incubation Time:

24h
Result:

Inhibited the expression of iNOS and reduced the levels of TNF-α, IL-1b, and IL-6.

In Vivo

Pelubiprofen (25-100 mg/kg, oral, single dose) inhibits the anti-inflammatory effect of NF-κB in the carrageenan-induced paw edema model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Carrageenan-induced paw edema model ^[1]
Dosage:

25 and 100 mg/kg, single dose
Administration:

Oral gavage (p.o.)
Result:

Significantly reduced MPO activity, decreased production of PGE2, and notably inhibited the nuclear translocation of p65.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 69956-77-0
Appearance Solid
Peso molecular 258.31
Fòrmula C₁₆H₁₈O₃
Color White to off-white
SMILES

O=C(O)C(C)C1=CC=C(/C=C2C(CCCC/2)=O)C=C1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (387.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.8713 mL

19.3566 mL

38.7132 mL

5 mM

0.7743 mL

3.8713 mL

7.7426 mL

10 mM

0.3871 mL

1.9357 mL

3.8713 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Ji-Sun Shin, et al. Anti-inflammatory effect of pelubiprofen, 2-[4-(oxocyclohexylidenemethyl)-phenyl]propionic acid, mediated by dual suppression of COX activity and LPS-induced inflammatory gene expression via NF-κB inactivation. J Cell Biochem. 2011 Dec;112(12):3594-603. [Content Brief]

[2]. Choi IA, Baek HJ, et al. Comparison of the efficacy and safety profiles of a pelubiprofen versus celecoxib in patients with rheumatoid arthritis: a 6-week, multicenter, randomized, double-blind, phase III, non-inferiority clinical trial. BMC Musculoskelet Disord. 2014 Nov 18;15:375. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.8713 mL	19.3566 mL	38.7132 mL	96.7829 mL
	5 mM	0.7743 mL	3.8713 mL	7.7426 mL	19.3566 mL
	10 mM	0.3871 mL	1.9357 mL	3.8713 mL	9.6783 mL
	15 mM	0.2581 mL	1.2904 mL	2.5809 mL	6.4522 mL
	20 mM	0.1936 mL	0.9678 mL	1.9357 mL	4.8391 mL
	25 mM	0.1549 mL	0.7743 mL	1.5485 mL	3.8713 mL
	30 mM	0.1290 mL	0.6452 mL	1.2904 mL	3.2261 mL
	40 mM	0.0968 mL	0.4839 mL	0.9678 mL	2.4196 mL
	50 mM	0.0774 mL	0.3871 mL	0.7743 mL	1.9357 mL
	60 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6130 mL
	80 mM	0.0484 mL	0.2420 mL	0.4839 mL	1.2098 mL
	100 mM	0.0387 mL	0.1936 mL	0.3871 mL	0.9678 mL

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Pelubiprofen

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

FDA-Approved Drug Library

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Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Lactylation Compound Library

Ver todos los productos específicos de isoformas COX

Ver todos los productos específicos de isoformas NF-κB

Ver todos los productos específicos de isoformas NO Synthase

Ver todos los productos específicos de isoformas IKK

Ver todos los productos específicos de isoformas MAP3K

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pelubiprofen Related Classifications

HY-12383 Related Classifications