貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S84448-1mg	99.8%	￥192.00 S84448-1mg ￥192.00 現(xiàn)貨	4 4	-	-	-
S84448-2mg	99.8%	￥300.00 S84448-2mg ￥300.00 現(xiàn)貨	5 5	-	-	-
S84448-5mg	99.8%	￥360.00 S84448-5mg ￥360.00 現(xiàn)貨	4 4	-	-	-
S84448-10mg	99.8%	￥590.00 S84448-10mg ￥590.00 現(xiàn)貨	4 4	-	-	-
S84448-25mg	99.8%	￥1300.00 S84448-25mg ￥1300.00 現(xiàn)貨	4 4	-	-	-
S84448-50mg	99.8%	￥2400.00 S84448-50mg ￥2400.00 現(xiàn)貨	4 4	-	-	-
S84448-100mg	99.8%	￥4300.00 S84448-100mg ￥4300.00 現(xiàn)貨	3 3	-	-	-

產(chǎn)品介紹

BX471 (ZK811752, BAY 865047, SH T 04268H) 是一種有效的非肽 CC 趨化因子受體-1 (CCR1) 拮抗劑，在 MIP-1α 和 MCP-3 與 CCR1 轉(zhuǎn)染的 HEK23 細(xì)胞結(jié)合中，Ki 值分別為 1 nM 和 5.5 nM

產(chǎn)品描述：

靶點(diǎn)：

CCR1(in MIP-1α binding assay):1 nM(ki); CCR1(in MCP-3 binding assay):5.5 nM(ki);CCR

體外研究：

By displacing the ligand binding to CC chemokine receptor-1 (CCR1), BX 471, a potent antagonist, can inhibit the effects medicated by CCR1. In addition, BX-471 exhibits anti-allergic effect by increasing Treg cell population

體內(nèi)研究：

For fasted dogs, the half-life for BX 471 was approximately 3 h, with an oral bioavailability of approximately 60%. In rats of EAE model, CCR1 antagonist, BX 471, dose-dependently decreased the severity of the disease

細(xì)胞實(shí)驗(yàn)：

Cell lines: THP-1- or CCR1-transfected HEK293 cells Concentrations: 10 μM Incubation Time: 24 h Method: Binding assays were performed by filtration. Radiolabeled chemokines at a final concentration of approximately 0.1–0.2 nM were used as ligand. HEK293 cells expressing human CCR1 at 8,000 or 300,000 cells per assay point were used as the receptor source. Nonspecific binding was determined in the presence of 100 nM unlabeled chemokine. The binding data were curve-fitted with the computer program IGOR (Wavemetrics) to determine the affinity and number of sites. To demonstrate that CCR1 antagonism by BX 471 was not due to the cellular toxicity of the compound, THP-1- or CCR1-transfected HEK293 cells were treated with BX 471 at concentrations up to 10 μM for 24 h, and cellular toxicity was monitored by measuring WST-1 staining. No significant toxicity was observed

動(dòng)物實(shí)驗(yàn)：

Animal Models: Fasted male beagle dogs; Male Lewis Rats of EAE model Dosages: 4 mg/kg (for fasted male beagle dogs); 20 and 50 mg/kg (for Male Lewis Rats) Administration: p.o.

參考文獻(xiàn)：

1. M Liang, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. 2. Feng S, et al. Therapeutic Effect of C-C Chemokine Receptor Type 1 (CCR1) Antagonist BX471 on Allergic Rhinitis. J Inflamm Res. 2020 Jul 21;13:343-356.

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	2.299 ml	11.497 ml	22.994 ml
5 mM	0.46 ml	2.299 ml	4.599 ml
10 mM	0.23 ml	1.15 ml	2.299 ml
50 mM	0.046 ml	0.23 ml	0.46 ml

注意：

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

參考文獻(xiàn)

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