Org 48762-0
Based on 1 Customer Validation
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.
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- Purity: 99.99%
- CAS No.: 755753-89-0
- 화학식: C24H16F2N4
- 분자량:398.41
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보관:Powder -20°C, 3 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]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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p38α 0.1 nM (EC50) |
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.
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Cell Line:THP-1 cells stimulated with IL-1β.
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:Pre-incubated for 30 min and subsequently stimulated with 10 ng/mL IL-1β.
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Result:Inhibited IL-1β-induced phosphorylation of p38 kinase as well as of HSP27, a downstream marker of p38 kinase activity.
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.
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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].
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Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:p.o; once
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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.
Chemical Information
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CAS No. 755753-89-0
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Appearance Solid
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분자량 398.41
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화학식 C24H16F2N4
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Color White to off-white
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SMILES
CN1N=C2C(C(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)C(C5=CC=C(F)C=C5)=N2)=C1
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Synonyms
UR13870
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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)
순도&문서
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. K Mihara, et al. A potent and selective p38 inhibitor protects against bone damage in murine collagen-induced arthritis: a comparison with neutralization of mouse TNFalpha. Br J Pharmacol. 2008 May;154(1):153-64. [Content Brief]
[2]. Bagley MC,et al. Synthesis of the highly selective p38 MAPK inhibitor UR-13756 for possible therapeutic use in Werner syndrome. Future Med Chem. 2010 Feb;2(2):193-201. [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 |
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| 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 |
Org 48762-0 Related Classifications
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