>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

Aprepitant 阿瑞匹坦；阿瑞吡坦；阿瑞比坦

Aprepitant是一种有效的选择性 neurokinin-1 receptor 拮抗剂，IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平，包括 G-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。

货号：
TK0447
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	170729-80-3
生物活性	Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
分子式	C23H21F7N4O3
分子量	534.43
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, protect from light,*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据	DMSO : ≥ 100 mg/mL (187.12 mM)
体内研究	Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. In contrast, aprepitant significantly enhances the expression of CPP produced by morphine while significantly suppressing the locomotor activity of the mice conditioned with morphine. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls.
体外研究	Aprepitant decreases the metabolic activity with an estimated IC50 value of 20 µM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 µM) induces p53 accumulation and expression of pro-apoptotic p53 target genes. Aprepitant (1, 5, 10 µM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC90 value of aprepitant is equivalent to 10 μM, and the IC50 value is about 5 μM.
纯度及产品资料	98%

推荐产品