2. MAPK/ERK Pathway Metabolic Enzyme/Protease Immunology/Inflammation
  3. p38 MAPK MMP PGE synthase
  4. R-130823

R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression. R-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis.

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R-130823

R-130823 Chemical Structure

CAS No. : 321344-32-5

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R-130823 Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Description

R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression. R-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis[1][2].

IC50 & Target[1]

p38α

22 nM (IC50)

p38β

820 nM (IC50)

MMP13

 

MMP-1

 

In Vitro

R-130823 potently inhibits purified p38α kinase (IC50 = 22 nM), moderately inhibits purified p38β kinase (IC50 = 820 nM), and shows no activity against p38γ or p38δ[1].
R-130823 (4-2500 nM; 1 h) inhibits the release of MMP-13 (IC50 = 20 nM), MMP-1 (IC50 = 230 nM) and PGE2 (IC50 = 3.9 nM) induced by IL-1β in human primary chondrocytes[1].
R-130823 (0.1-10 μM; incubated for 3 weeks with weekly compound supplementation) inhibits IL-1α/oncostatin M-induced collagen cleavage in bovine nasal cartilage explants, with an IC50 of 510 nM[1].

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

R-130823 Related Antibodies
In Vivo

R-130823 (1-30 mg/kg/day; p.o.; twice daily; 7 days) dose-dependently reduces established hind paw swelling in rat adjuvant-induced arthritis, with a 55% reduction at the highest tested dose of 30 mg/kg/day[2].
R-130823 (1-30 mg/kg; p.o.; single dose) dose-dependently ameliorates adjuvant-induced hyperalgesia in rats, with sustained analgesic activity lasting up to 24 hours at the highest tested dose of 30 mg/kg[2].
R-130823 (3-30 mg/kg/day; p.o.; once daily; 14 days) dose-dependently blocks arthritis progression in murine collagen-induced arthritis, with statistically significant suppression of arthritis index (P < 0.0001) and reduced joint tissue inflammation at the highest tested dose of 30 mg/kg/day[2].

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

Animal Model: Lewis rats (female, 7 weeks old, adjuvant-induced arthritis model)[2]
Dosage: 1 mg/kg/day; 3 mg/kg/day; 10 mg/kg/day; 30 mg/kg/day
Administration: p.o.; twice daily; 7 days
Result: Reduced hind paw swelling volume by 18% at 1 mg/kg/day on Day 25.
Reduced hind paw swelling volume by 31% at 3 mg/kg/day on Day 25.
Reduced hind paw swelling volume by 45% at 10 mg/kg/day on Day 25.
Reduced hind paw swelling volume by 55% at 30 mg/kg/day on Day 25.
Animal Model: Lewis rats (male, 5 weeks old, adjuvant-induced hyperalgesia model)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Produced dose-dependent reductions in pain score, with effects observed within 1 hour, maximum effect at 2 hours post-administration, and sustained analgesic activity up to 24 hours post-administration.
Decreased pain score by 74% at 30 mg/kg at 24 hours post-administration, with statistical significance relative to controls between 1 and 24 hours.
Animal Model: DBA1/J mice (male, 5 weeks old, collagen-induced arthritis model)[2]
Dosage: 3 mg/kg/day; 10 mg/kg/day; 30 mg/kg/day
Administration: p.o.; once daily; 14 days
Result: Dose-dependently suppressed arthritis progression.
Showed no increase in arthritis index over the treatment period at 30 mg/kg/day, with a statistically significant lower index relative to vehicle controls (P < 0.0001).
Reduced severity of synovial neutrophil infiltration, fibrin deposition, synoviocyte proliferation, fibroblast proliferation, joint cavity debris, and cartilage cell desquamation in knee joints at 30 mg/kg/day relative to vehicle controls.
Molecular Weight

423.52

Formula

C28H26FN3
CAS No.
SMILES

FC1=CC=C(C=C1)C2=C(C(C3=CCN(CC3)CCC4=CC=CC=C4)=CN2)C5=CC=NC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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R-130823 Related Classifications

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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:

R-130823321344-32-5R130823R 130823p38 MAPKMMPPGE synthaseMatrix metalloproteinasesProstaglandin E synthasep38δinterleukin-1βextracellular signal-regulated kinase 1/2p38α mitogen-activated protein kinasematrix metalloproteinase-13p38βp38γc-Jun N-terminal kinase 1α1matrix metalloproteinase-1cyclooxygenase-2Inhibitorinhibitorinhibit

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