Pamapimod

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服生物可利用的 p38α MAPK 抑制剂，Kd 为 0.2 nM。

A potent, selective, orally bioavailable p38α MAPK inhibitor with Kd of 0.2 nM; displays >100 fold selectivity over p38β (Kd=29 nM), and no affinity against p38γ, p38δ and a broad panel of kianses; inhibits LPS-stimulated TNF-alpha production by monocytes, IL-1beta production in human whole blood; exhibits the ability to inhibit the signs and symptoms of RA and other autoimmune diseases.Rheumatoid Arthritis Phase 2 Discontinued.

Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively. After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively.

Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis. Animal Model:DBA/1J female mice (8-10 weeks of age) induced murine collagen Dosage:0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg Administration:Oral gavage; once daily Result:Reduced inflammation and bone loss.

Ro4402257 | R1503

MAPK/ERK Signaling

p38 MAPK

p38α|p38β

Inflammation/Immunology

Rheumatoid Arthritis

449811-01-2

406.3833

C19H20F2N4O4

>98% (HPLC)

DMSO: ≥ 34 mg/mL

O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-

(-20℃)

With Ice Pack

≥ 2 years