貨號	規格	價格	上海	北京	武漢	南京
S81046-2mg	99.9%	￥280.00 S81046-2mg ￥280.00 現貨	10 10	-	-	-
S81046-5mg	99.9%	￥472.00 S81046-5mg ￥472.00 現貨	8 8	-	-	-
S81046-10mg	99.9%	￥800.00 S81046-10mg ￥800.00 現貨	8 8	-	-	-
S81046-25mg	99.9%	￥1600.00 S81046-25mg ￥1600.00 現貨	4 4	-	-	-
S81046-50mg	≥99%	￥3040.00 S81046-50mg ￥3040.00 2-3天	0 貨期：2-3天	-	-	-
S81046-100mg	≥99%	￥5520.00 S81046-100mg ￥5520.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

產品描述：

IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

靶點：

IκB/IKK;LRRK2;IκB/IKK;?LRRK2

體內研究：

IKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.

細胞實驗：

IKK 16 is prepared in DMSO and stored, and then diluted with appropriate medium before use. Human umbilical vein vascular endothelial cells line (HUVECs) are cultured in DMEM supplemented with 10% fetal bovine serum, streptomycin, and penicillin. The cells is grown at 37°C in a humidified 5% CO2 atmosphere. Cells are pretreated with IKK 16 (10 μmol/mL) for 1 hr. The cells are then cultured with TGF-β1 (20 ng/mL) and AT-RvD1 (20 ng/mL). After incubation, the gene expressions of Nrf2 and Smad7 are determined by RT-PCR. The protein expression of Nrf2 and IκBα are determined by Western blot

動物實驗：

IKK 16 is prepared in DMSO and diluted with saline or PBS.Rats and MiceIKK 16 is tested in two animal models. First, its efficacy to inhibit TNFα release into plasma upon LPS-challenge in the rat is determined. IKK 16 is dosed sc (30 mg/kg) or orally (30 mg/kg) 1 h prior to the LPS-challenge. Four hours after the challenge, plasma is collected and the systemic TNFα levels are analyzed using a commercially available ELISA kit. Both routes of administration of IKK 16 at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). In a second experiment, IKK 16 is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50% at a dose of 10 mg/kg sc. MiceTwo-month-old male C57BL/6 mice receive LPS (9 mg/kg body weight) and PepG (3 mg/kg body weight) in 0.9% saline (5 mL/kg body weight) intraperitoneally. Sham mice are not subjected to LPS/PepG, but are otherwise treated the same way. At 1 hour after LP

參考文獻：

1.Waelchli R, et al. Bioorg Med Chem Lett, 2006, 16(1), 108-112.

溶解性：

DMSO:90 mg/mL (186.1 mM) Ethanol:<1 mg/mL H2O:<1 mg/mL

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.068 ml	10.338 ml	20.677 ml
5 mM	0.414 ml	2.068 ml	4.135 ml
10 mM	0.207 ml	1.034 ml	2.068 ml
50 mM	0.041 ml	0.207 ml	0.414 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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