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Cat. No.: HY-123670

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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.

CAS No.: 218162-38-0
Formula: C₂₅H₂₉FN₄O₇S
Molecular Weight:548.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

RPR-200765A methanesulfonate Chemical Structure

CAS No.: 218162-38-0

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Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All p38 MAPK Isoforms :

All TNF Receptor Isoforms :

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.

Parmacokinetics

Species	Dose	Route	V_d	CL	T_1/2	Bioavailability	C_max	AUC	T_max
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.

Chemical Information

CAS No. 218162-38-0
Molecular Weight 548.58
Formula C₂₅H₂₉FN₄O₇S
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
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

Handling Instructions (2659 KB)

References

[1]. Mclay LM, et al. The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg Med Chem. 2001 Feb;9(2):537-54.
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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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RPR-200765A methanesulfonate

All p38 MAPK Isoforms

All TNF Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RPR-200765A methanesulfonate Related Classifications

HY-123670 Related Classifications