Tak-715

Bezeichnung:Tak-715

CAS-Nr303162-79-0

Englisch Name:Tak-715

CBNumberCB71017172

SummenformelC24H21N3OS

Molgewicht399.51

MOL-Datei303162-79-0.mol

Tak-715 physikalisch-chemischer Eigenschaften

storage temp.	Sealed in dry,2-8°C
Löslichkeit	DMSO: >15mg/mL
Aggregatzustand	powder
Farbe	faint yellow to dark yellow
InChI	InChI=1S/C24H21N3OS/c1-3-21-27-22(18-11-7-8-16(2)14-18)23(29-21)19-12-13-25-20(15-19)26-24(28)17-9-5-4-6-10-17/h4-15H,3H2,1-2H3,(H,25,26,28)
InChIKey	HEKAIDKUDLCBRU-UHFFFAOYSA-N
SMILES	C(NC1=NC=CC(C2SC(CC)=NC=2C2=CC=CC(C)=C2)=C1)(=O)C1=CC=CC=C1

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36
S-Sätze:	26
WGK Germany	3
HS Code	2934999090
Speicherklasse	11 - Combustible Solids
Hazard Classifications	Acute Tox. 4 Oral Eye Irrit. 2

Gefahreninformationscode (GHS)

Tak-715 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
TAK 715 is a p38 MAPK inhibitor for p38α and p38β but not for p38γ and p38δ.
Definition
ChEBI: N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]benzamide is a member of benzamides.
Biologische Aktivität
tak-715 is a selective inhibitor of p38 mapk with ic50 value of 7.1 nm [1].p38 mitogen-activated protein (map) kinases (p38 mapks) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. four p38 mapks contain members, p38-α (mapk14), p38-β (mapk11), p38-γ (mapk12/erk6), and p38-δ (mapk13/sapk4), have been identified. abnormal expression of p38 mapks are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].tak-715 is a potent p38 mapk inhibitor and has a different selectivity with the reported p38 mapk inhibitor vx-745. when tested with human monocytic thp-1 cells, administration of tak-715 exhibited inhibition on p38mapkα with ic50 value of 7.1 nm [1]. in hek293t, u2os, and f9 cells, tak-715 was used to inhibit p38 mapk activity and concluded that p38 mapk had no function in wnt/β-catenin signaling pathway [2].in adjuvant-induced rheumatoid arthritis rat model, administration of tak-715 at dose of 10 mg/kg significantly decreased lps-induced stimulated release of tnf-α (87.6%) by inhibiting p38 mapk activity [1].
in vivo

TAK-715 (compound 8h; 3-30 mg/kg; PO) significantly reduces the secondary paw volume^[1].
TAK-715 (10 mg/kg; PO) has a C_max of 0.19 μg/mL and an AUC of 1.16 μg h/mL.
Animal Model: 7-week-old male Lewis rats with arthritis^[1]
Dosage: 3, 10, 30 mg/kg
Administration: PO; single dose
Result: Significantly reduced the secondary paw volume (25% inhibition)
Animal Model: Rat^[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: PO
Result: Had a C_max of 0.19 μg/mL and an AUC of 1.16 μgh/mL.
IC 50
p38α: 7.1 nM (IC₅₀); p38β: 200 nM (IC₅₀); p38δ: >10 μM (IC₅₀); p38γ: >10 μM (IC₅₀); CK1δ; CK1ε
Lager
+4°C
Einzelnachweise
[1]. miwatashi, s., et al., novel inhibitor of p38 map kinase as an anti-tnf-alpha drug: discovery of n-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (tak-715) as a potent and orally active anti-rheumatoid arthritis agent. j med chem, 2005. 48(19): p. 5966-79.
[2]. verkaar, f., et al., inhibition of wnt/beta-catenin signaling by p38 map kinase inhibitors is explained by cross-reactivity with casein kinase idelta/varepsilon. chem biol, 2011. 18(4): p. 485-94.

Tak-715 Upstream-Materialien And Downstream Produkte

Tak-715 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

303162-79-0, Tak-715 Verwandte Suche:

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Animal Model:	7-week-old male Lewis rats with arthritis^[1]
Dosage:	3, 10, 30 mg/kg
Administration:	PO; single dose
Result:	Significantly reduced the secondary paw volume (25% inhibition)

Animal Model:	Rat^[1]
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	PO
Result:	Had a C_max of 0.19 μg/mL and an AUC of 1.16 μgh/mL.