貨號	規格	價格	上海	北京	武漢	南京
S84980-1mg	≥98%	￥1500.00 S84980-1mg ￥1500.00 2-3天	0 貨期：2-3天	-	-	-
S84980-5mg	≥98%	￥3500.00 S84980-5mg ￥3500.00 2-3天	0 貨期：2-3天	-	-	-
S84980-10mg	≥98%	￥5000.00 S84980-10mg ￥5000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.

產品描述：

靶點：

MIP-1α-CCR5:1.4 nM (IC50, in CHO cells);RANTES-CCR5:3.5 nM (IC50, in CHO cells);HIV-1 (HHA):0.55 nM (EC50, in PBMCs);HIV-1 (CTV):0.72 nM (EC50, in PBMCs);HIV-1 (HTN):0.93 nM (EC50, in PBMCs);HIV-1 (KK):1.2 nM (EC50, in PBMCs);HIV-1 (HKW):1.7 nM (EC50, in PBMCs);HIV-1 (HNK):1.7 nM (EC50, in PBMCs);HIV-1 (HHA):4 nM (EC90, in PBMCs);HIV-1 (CTV):5 nM (EC90, in PBMCs);HIV-1 (KK):12 nM (EC90, in PBMCs);HIV-1 (HKW):12 nM (EC90, in PBMCs);HIV-1 (HTN):15 nM (EC90, in PBMCs);HIV-1 (HNK):28 nM (EC90, in PBMCs);HIVProt

體外研究：

TAK-220 is a selective CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5 in CHO cells, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion, with an IC50 value of 0.42 nM, but does not alter X4 HIV-1 (HXB2) envelope-mediated membrane fusion. TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs. TAK-220 shows potent inhibitory activity against the R5 isolates, with IC50s of 3.12 nM against HIV-1 R5-08, 13.47 nM against HIV-1 R5-06, and 2.26 nM against HIV-1 R5-18. TAK-220 (>100 nM) has no toxicity in uninfected PBMCs

參考文獻：

1. Takashima K, et al. Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist. Antimicrob Agents Chemother. 2005 Aug;49(8):3474-82. 2. Tremblay CL, et al. TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro. Antimicrob Agents Chemother. 2005 Aug;49(8):3483-5.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.808 ml	9.039 ml	18.079 ml
5 mM	0.362 ml	1.808 ml	3.616 ml
10 mM	0.181 ml	0.904 ml	1.808 ml
50 mM	0.036 ml	0.181 ml	0.362 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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