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Pamapimod

SKU: orb1225026

Description

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.

Images & Validation

Key Properties

CAS Number449811-01-2
MW406.3833
Purity>98% (HPLC)
FormulaC19H20F2N4O4
SMILESO=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
Targetp38 MAPK
SolubilityDMSO: ≥ 34 mg/mL

Bioactivity

In Vivo
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.
In Vitro
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Ro4402257 | R1503

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Pamapimod (orb1225026)

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Available Sizes

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5 mg
$ 400.00
10 mg
$ 670.00
25 mg
$ 1,040.00
50 mg
$ 1,470.00
100 mg
$ 1,970.00
500 mg
$ 3,810.00