貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
Y31549-1mg	≥99%	￥467.00 Y31549-1mg ￥467.00 現(xiàn)貨	10 10	-	-	-
Y31549-5mg	≥99%	￥765.00 Y31549-5mg ￥765.00 現(xiàn)貨	6 6	-	-	-
Y31549-10mg	≥99%	￥1275.00 Y31549-10mg ￥1275.00 現(xiàn)貨	6 6	-	-	-
Y31549-25mg	≥99%	￥2380.00 Y31549-25mg ￥2380.00 現(xiàn)貨	6 6	-	-	-
Y31549-100mg	≥99%	￥6800.00 Y31549-100mg ￥6800.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

產(chǎn)品描述：

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

靶點(diǎn)：

Cathepsin L2:6.7(pIC50), Cathepsin B:5.2(pIC50), Cathepsin S:6(pIC50), cathepsin K:5.5(pIC50), Cathepsin L:7.9(pIC50);CysteineProtease

體外研究：

The CatL pIC50 value of Cathepsin Inhibitor 1 was found to exceed that of its analog by 1.6 units. Moreover, CatS (ΔpIC50 = -0.1) and CatL2 (ΔpIC50 = 0.5) were much less sensitive to the structural change of Cathepsin Inhibitor 1, leading to an improved selectivity profile relative to its analog. Cathepsin Inhibitor 1 was as least as selective with respect to CatB and CatS as previously described CatL inhibitors. The crystal structure of its another analog bound to CatL provided the rationale for the SAR observed for Cathepsin Inhibitor 1. The 1-methyl group of the pyrazole made some contact with Leu69 and appeared to force the pyrazole ring out of co-planarity with the amide, likely functioning as a conformational lock

體內(nèi)研究：

Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats.

參考文獻(xiàn)：

1. Asaad N, et al. Dipeptidyl nitrile inhibitors of Cathepsin L. Bioorg Med Chem Lett, 2009, 19(15), 4280-4283.

溶解性：

Soluble in DMSO、Ethanol

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.488 ml	12.441 ml	24.882 ml
5 mM	0.498 ml	2.488 ml	4.976 ml
10 mM	0.249 ml	1.244 ml	2.488 ml
50 mM	0.05 ml	0.249 ml	0.498 ml