2. MAPK/ERK Pathway Apoptosis
  3. p38 MAPK TNF Receptor
  4. RPR-200765A methanesulfonate

RPR-200765A methanesulfonate 是一种口服有效的 p38 MAPK 抑制剂，其 IC50 为 0.050 μM。RPR-200765A methanesulfonate 对 Lck 的活性较弱，对 ERK、ZAP70 或 SYK 无显著活性。RPR-200765A methanesulfonate 可抑制 TNFα 的产生，可用于炎症疾病的研究。

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RPR-200765A methanesulfonate

RPR-200765A methanesulfonate Chemical Structure

CAS No. : 218162-38-0

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RPR-200765A methanesulfonate 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 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RPR-200765A methanesulfonate is an orally active p38 MAPK inhibitor with an IC50 of 0.050 μM. RPR-200765A methanesulfonate shows weak activity against Lck, and exhibits no significant activity against ERK, ZAP70 or SYK. It inhibits the production of TNFα and can be used in the research of inflammatory diseases[1].

体外研究
(In Vitro)

RPR-200765A methanesulfonate 可强效抑制 p38 激酶，其 IC50 为 0.050 μM，且对 ERK、ZAP70、SYK 和 Lck 激酶仅表现出弱抑制活性或无抑制活性[1]。
RPR-200765A methanesulfonate 在 Ames 试验和 CHO 细胞微核试验中无致突变性，且不会在大鼠肝细胞中诱导 CYP1A1 的表达[1]。

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

RPR-200765A methanesulfonate 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Vd CL T1/2 Bioavailability Cmax AUC Tmax
Rat[1] 10 mg/kg p.o. / / 2.8 h 50 % 5154 ng/mL 11111 ng·h/mL 0.25-0.5 h
Rat[1] 1 mg/kg i.v. 0.7 L/kg 1 L/h/kg 1.6 h 50 % / / /
体内研究
(In Vivo)

RPR-200765A methanesulfonate (6 mg/kg；口服；单次给药) 可抑制 LPS (HY-D1056) 诱导的小鼠体内 TNFα 释放，口服后的 ED50 为 6 mg/kg[1]。
RPR-200765A methanesulfonate (3-30 mg/kg；口服；每天两次共 28 天) 以剂量依赖的方式减轻佐剂诱导的关节炎大鼠的足肿胀[1]。

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

Animal Model: balb/c mice[1]
Dosage: 6 mg/kg
Administration: p.o.; single dose
Result: Achieved 50% inhibition of LPS-induced TNFα release (ED50 = 6 mg/kg).
Animal Model: balb/c mice
[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; twice daily for 28 consecutive days
Result: Significantly reduced paw swelling in adjuvant-induced arthritic rats.
分子量

548.58

Formula

C25H29FN4O7S
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

RPR-200765A methanesulfonate 相关分类

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  • 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:

RPR-200765A218162-38-0p38 MAPKTNF ReceptorTumor Necrosis Factor ReceptorTNFRp38 mitogen-activated protein kinasetumor necrosis factor alphaCYP 1A1SYKlipopolysaccharideERKCHO cellZAP70Lckrat hepatocytesInhibitorinhibitorinhibit

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