(R)-STU104

立即咨询

(R)-STU104

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2767124-77-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

(R)-STU104 是一种有效且具有口服活性的TAK1与MKK3蛋白质互作抑制剂，对TNF-α和 MKK3 磷酸化的IC₅₀分别为 0.58 μM 和 4.0 μM。(R)-STU104 通过与 MKK3 结合，阻断 TAK1 磷酸化 MKK3，抑制 TAK1/MKK3/p38/MnK1/MK2/elF4E 信号通路。(R)-STU104 可用于溃疡性结肠炎的研究。

生物活性

(R)-STU104 is a potent and orally activeTAK1-MKK3 interactioninhibitor withIC₅₀s of 0.58 μM and 4.0 μM forTNF-αand MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis^[1].

IC₅₀& Target

IC₅₀: 0.58 μM (TNF-α), 4.0 μM (MKK3 phosphorylation)^[1]

体外研究
(In Vitro)

(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production^[1].

体内研究
(In Vivo)

(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein^[1].
Pharmacokinetic Parameters of (R)-STU104 in male C57 mice^[1].

	IV (5 mg/kg)	PO (30 mg/kg)
T_max(h)		0.083
AUC_0-t(μg/L·h)	7249	9895
AUC_0-∞(μg/L·h)	8635	16991
MRT_0-∞(h)	7.32	12.52
C_max(ng/mL)	2920	2290
t_1/2(ng/mL)	9.29	8.67
V_Z(L/kg)	7.76	3.68
CL_Z(ng/mL)	0.58	0.29
F (%)	33%

Animal Model:	C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)^[1]
Dosage:	1, 3 and 10 mg/kg
Administration:	IG, for 7 days
Result:	Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.

分子量

298.33

Formula

C₁₈H₁₈O₄

CAS 号

2767124-77-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.