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

R-130823 是一种具有口服活性的高选择性 p38α 抑制剂，其针对 p38α 的 IC50 为 22 nM，针对 p38β 的 IC50 为 820 nM，且对 p38γ、p38δ 无活性。R-130823 可下调下游软骨降解及炎症介质，抑制 MMP-13、MMP-1 和 PGE2 的释放。R-130823 可减轻后爪肿胀，改善痛觉过敏，阻断关节炎进展。\nR-130823 可用于骨关节炎和类风湿性关节炎的相关研究。

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R-130823

R-130823 Chemical Structure

CAS No. : 321344-32-5

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R-130823 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

查看 MMP 亚型特异性产品:

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.\nR-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

 

体外研究
(In Vitro)

R-130823 可强效抑制纯化的 p38α 激酶 (IC50 = 22 nM)，中度抑制纯化的 p38β 激酶 (IC50 = 820 nM)，且对 p38γ 或 p38δ 无活性[1]。
R-130823 (4-2500 nM; 1 h) 可抑制 IL-1β 诱导的人原代软骨细胞中 MMP-13 (IC50 = 20 nM)、MMP-1 (IC50 = 230 nM) 和 PGE2 (IC50 = 3.9 nM) 的释放[1]。
R-130823 (0.1-10 μM；孵育 3 周，每周补充化合物) 可抑制 IL-1α/抑瘤素 M 诱导的牛鼻软骨外植体中胶原蛋白的裂解，其 IC50 为 510 nM[1]。

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

R-130823 相关抗体:
体内研究
(In Vivo)

R-130823 (1-30 mg/kg/天；口服；每日 2 次；连续 7 天) 可剂量依赖性地减轻大鼠佐剂诱导性关节炎模型中已形成的足爪肿胀，在最高测试剂量 30 mg/kg/day 时肿胀抑制率达 55%[2]。
R-130823 (1-30 mg/kg；口服；单次) 可剂量依赖性地改善大鼠佐剂诱导的痛觉过敏，在最高测试剂量 30 mg/kg 时，其镇痛活性可持续长达 24 小时[2]。
R-130823 (3-30 mg/kg/天；口服；每日 1 次；连续 14 天) 可剂量依赖性地阻断小鼠胶原诱导性关节炎的进展，在最高测试剂量 30 mg/kg/天时，对关节炎指数的抑制具有统计学显著性 (P < 0.0001)，且可减轻关节组织炎症[2]。

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.
分子量

423.52

Formula

C28H26FN3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

R-130823 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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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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