2. MAPK/ERK Pathway
  3. p38 MAPK
  4. Org 48762-0

Org 48762-0 (UR13870) is a potent, orally active and selective p38 inhibitor with an EC50 of 0.1 μM for p38α kinase. Org 48762-0 shows a high degree of kinase selectivity for p38α and p38β over other kinases. Org 48762-0 reduces Lipopolysaccharides (HY-D1056) (LPS)-induced TNFα release. Org 48762-0 can be used for the study of rheumatoid arthritis (RA) and Werner syndrome.

For research use only. We do not sell to patients.

Org 48762-0 Chemical Structure

Org 48762-0 Chemical Structure

CAS No. : 755753-89-0

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Org 48762-0 Related Antibodies

Top Publications Citing Use of Products

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Org 48762-0 (UR13870) is a potent, orally active and selective p38 inhibitor with an EC50 of 0.1 μM for p38α kinase. Org 48762-0 shows a high degree of kinase selectivity for p38α and p38β over other kinases. Org 48762-0 reduces Lipopolysaccharides (HY-D1056) (LPS)-induced TNFα release. Org 48762-0 can be used for the study of rheumatoid arthritis (RA) and Werner syndrome[1][2].

IC50 & Target[1]

p38α

0.1 nM (EC50)

In Vitro

Org 48762-0 completely inhibits LPS-induced TNFα release from peripheral blood mononuclear cells (PBMC) with an EC50 value of 0.06 μM. Org 48762-0 dose-dependently inhibits stress-induced MK2 translocation, with an EC50 value of 0.69 μM[1].
Org 48762-0 (0.1-10 μM; pre-incubated for 30 min) is capable of inhibiting IL-1β-induced signalling cascades, consequently interfering with production of proinflammatory cytokines[1].

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

Org 48762-0 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells stimulated with IL-1β.
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: Pre-incubated for 30 min and subsequently stimulated with 10 ng/mL IL-1β.
Result: Inhibited IL-1β-induced phosphorylation of p38 kinase as well as of HSP27, a downstream marker of p38 kinase activity.
In Vivo

Org 48762-0 (0.3-3 mg/kg; p.o; once) inhibits LPS-induced cytokine production in mice[1].
In mice, Org 48762-0 shows an oral bioavailability of 85% and exhibits sustained systemic exposure (>1 μM) for 24 h after a dose of 4.0 mg/kg. When Org 48762-0 is administered intravenously (1.6 mg/kg), the compound shows a low volume of distribution in steady state (Vss: 50.0 mL/kg) and a low clearance (CL: 9.0 mL/h/kg), resulting in a mean residence time of 5.3 h[1].

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

Animal Model: Female Balb/c mice (7- to 8-week old) were intraperitoneally challenged with LPS (20 μg/mouse) dissolved in PBS to induce inflammatory responses[1].
Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: p.o; once
Result: Dose-dependently inhibited LPS-induced TNFα production.
Significantly reduced serum levels of IL-1β, IL-6, macrophage inflammatory protein-1α/β, RANTES and MCP-1 induced by LPS challenge.
Molecular Weight

398.41

Formula

C24H16F2N4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1N=C2C(C(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)C(C5=CC=C(F)C=C5)=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (251.00 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 2.5100 mL 12.5499 mL 25.0998 mL
5 mM 0.5020 mL 2.5100 mL 5.0200 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 2.5100 mL 12.5499 mL 25.0998 mL 62.7494 mL
5 mM 0.5020 mL 2.5100 mL 5.0200 mL 12.5499 mL
10 mM 0.2510 mL 1.2550 mL 2.5100 mL 6.2749 mL
15 mM 0.1673 mL 0.8367 mL 1.6733 mL 4.1833 mL
20 mM 0.1255 mL 0.6275 mL 1.2550 mL 3.1375 mL
25 mM 0.1004 mL 0.5020 mL 1.0040 mL 2.5100 mL
30 mM 0.0837 mL 0.4183 mL 0.8367 mL 2.0916 mL
40 mM 0.0627 mL 0.3137 mL 0.6275 mL 1.5687 mL
50 mM 0.0502 mL 0.2510 mL 0.5020 mL 1.2550 mL
60 mM 0.0418 mL 0.2092 mL 0.4183 mL 1.0458 mL
80 mM 0.0314 mL 0.1569 mL 0.3137 mL 0.7844 mL
100 mM 0.0251 mL 0.1255 mL 0.2510 mL 0.6275 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Org 48762-0 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Org 48762-0755753-89-0UR13870UR 13870UR-13870p38 MAPKorally activep38α kinaserheumatoid arthritis (RA)Werner syndromeInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Org 48762-0
Cat. No.:
HY-114221
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.