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

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.

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

RPR-200765A methanesulfonate

RPR-200765A methanesulfonate Chemical Structure

CAS No. : 218162-38-0

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RPR-200765A methanesulfonate Related Antibodies

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Description

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].

In Vitro

RPR-200765A methanesulfonate potently inhibits p38 kinase with an IC50 of 0.050 μM, and exhibits weak or no inhibition of ERK, ZAP70, SYK, and Lck kinases[1].
RPR-200765A methanesulfonate is non-mutagenic in the Ames test and CHO cell micronucleus test, and does not induce CYP1A1 in rat hepatocytes[1].

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

RPR-200765A methanesulfonate Related Antibodies
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 % / / /
In Vivo

RPR-200765A methanesulfonate (6 mg/kg; p.o.; single administration) inhibits LPS (HY-D1056)-induced TNFα release in mice, with an oral ED50 of 6 mg/kg[1].
RPR-200765A methanesulfonate (3-30 mg/kg; p.o.; twice daily for 28 days) reduces paw swelling in adjuvant-induced arthritis rats in a dose-dependent manner[1].

MedChemExpress (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.
Molecular Weight

548.58

Formula

C25H29FN4O7S
CAS No.
SMILES

O=C([C@@]1(C)CO[C@@H](C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)OC1)N5CCOCC5.CS(=O)(O)=O
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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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RPR-200765A methanesulfonate 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:

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

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