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TAK-715

SKU: orb1225375

Description

A potent, selective, orally active p38α MAPK inhibitor with IC50 of 7.1 nM; displays >20-fold selectvity over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1; inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM; exerts significant efficacy in rat adjuvant-induced arthritis model.Rheumatoid Arthritis Phase 2 Discontinued.

Images & Validation

Key Properties

CAS Number303162-79-0
MW399.508
Purity>98% (HPLC)
FormulaC24H21N3OS
SMILESO=C(NC1=NC=CC(C2=C(C3=CC=CC(C)=C3)N=C(CC)S2)=C1)C4=CC=CC=C4
Targetp38 MAPK
Solubility10 mM in DMSO

Bioactivity

In Vivo
Animal model: 7-week-old male Lewis rats with arthritis. Dosage: 3, 10, 30 mg/kg. Administration: PO; single dose. Result: Significantly reduced the secondary paw volume (25% inhibition). Animal model: Rat. Dosage: 10 mg/kg (Pharmacokinetic Analysis). Administration: PO. Result: Had a Cmax of 0.19 μg/mL and an AUC of 1.16 μg h/mL.

Storage & Handling

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

Alternative Names

TAK 715 | TAK715

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TAK-715 (orb1225375)

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Available Sizes

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2 mg
$ 90.00
5 mg
$ 130.00
10 mg
$ 160.00
25 mg
$ 260.00
50 mg
$ 470.00
100 mg
$ 710.00
500 mg
$ 1,550.00