- 貨號 Cat. No.
- S2928
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
TAK-715
Catalog No.S2928
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.
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10mM/1mLIn DMSO |
USD 239 |
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10mg |
USD 185 |
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50mg |
USD 592 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2. |
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Targets |
p38α |
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IC50 |
7.1 nM [1] |
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In vitro |
TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. [1] TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. [2] The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop. [3] |
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In vivo |
TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model. [1] |
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Features |
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Protocol(Only for Reference)
Kinase Assay: [1]
p38 MAP Kinase Assay |
Kinase reactions of purified human p38 MAP kinase α are performed at 30 °C for 1 h in kinase reaction buffer (25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol) containing 0.1 μCi [γ-32P]ATP, 500 nM ATP, and myelin basic protein (MBP). The kinase reactions are terminated by the addition of 10% trichloroacetic acid. Phosphorylated proteins are filtrated through GF/C filter plates with a Cell harvester, washing out free [γ-32P]ATP with 250 mM phosphoric acid. The plates are then incubated for 60 min at 45 °C, followed by the addition of 40 μL of MicroScint-O. Radioactivity is counted using a Top-count scintillation counter. |
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Animal Study: [1]
Animal Models |
Adjuvant-induced arthritis (AA) rat model |
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Dosages |
30 mg/kg |
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Administration |
Orally |
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Solubility |
30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL |
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1
References
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number |
Recruitment |
Conditions |
Sponsor
/Collaborators |
Start Date |
Phases |
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NCT00760864 |
Completed |
Arthritis, Rheumatoid |
Takeda |
2004-08 |
Phase 2 |
NCT00931970 |
Recruiting |
End-Stage Renal Disease |
Clinical Research Center for End Stage Renal Disease, Korea|Ministry of Health & Welfare, Korea|Kyungpook National University|Daegu Metropolitan City, Korea|National Clinical Research Coordination Center, Seoul, Korea|Medical Research Collaborating Center, Seoul, Korea |
2009-07 |
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NCT01220596 |
Recruiting |
Hepatitis B, Chronic |
Hanyang University|Roche Pharma AG |
2010-06 |
Phase 3 |
Download TAK-715 SDF
Molecular Weight (MW) |
399.51 |
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Formula |
C24H21N3OS
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CAS No. |
303162-79-0 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
80 mg/mL (200 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
16 mg/mL (40 mM) |
In vivo |
30% propylene glycol, 5% Tween 80, 65% D5W, |
30 mg/mL |
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name |
Benzamide, N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]- |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.39951 |
3.9951 |
7.9902 |
11.9853 |
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