N- [2-({(3R,4R)-1- [4-(1,3-苯并间二氧杂环戊烯-5-基)-4-羟基环己

更新时间：2024-01-09 11:04:45

N- [2-({(3R,4R)-1- [4-(1,3-苯并间二氧杂环戊烯-5-基)-4-羟基环己结构式	常用名	N- [2-({(3R,4R)-1- [4-(1,3-苯并间二氧杂环戊烯-5-基)-4-羟基环己	英文名	Benzamide, N-[2-[[(3R,4R)-1-[cis-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, rel-
	CAS号	1285539-85-6	分子量	577.59
	密度	N/A	沸点	N/A
	分子式	C₂₉H₃₄F₃N₃O₆	熔点	N/A
	MSDS	N/A	闪点	N/A

用途

本网站展示的所有产品仅用作科学研究，不可食用，不可用于人体或动物的临床诊断和治疗。

cis-INCB3344 是 INCB3344 (HY-50674) 的非活性异构体,可作为实验中的对照化合物。INCB3344 是一种有效的 CCR2 拮抗剂,拮抗结合活性时,IC50 为 5.1 nM (hCCR2) 和 9.5 nM (mCCR2),拮抗趋化活性时,IC50 为 3.8 nM (hCCR2) 和 7.8 nM (mCCR2)。

中文名	N- [2-({(3R,4R)-1- [4-(1,3-苯并间二氧杂环戊烯-5-基)-4-羟基环己
英文名	N-[2-({(3R,4R)-1-[4-(1,3-Benzodioxol-5-yl)-4-hydroxycyclohexyl]-4 -ethoxy-3-pyrrolidinyl}amino)-2-oxoethyl]-3-(trifluoromethyl)benz amide

描述	cis-INCB3344 是 INCB3344 (HY-50674) 的非活性异构体,可作为实验中的对照化合物。INCB3344 是一种有效的 CCR2 拮抗剂,拮抗结合活性时,IC50 为 5.1 nM (hCCR2) 和 9.5 nM (mCCR2),拮抗趋化活性时,IC50 为 3.8 nM (hCCR2) 和 7.8 nM (mCCR2)。
相关类别	研究领域 >> 内分泌信号通路 >> 其他 >> 其他研究领域 >> 炎症/免疫
参考文献	[1]. Xue CB, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8 [2]. Zhao W, et al. Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882. [3]. Aye-Mon A, et al. CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. Mol Pain. 2018 Jan-Dec;14:1744806917751322. [4]. Chan CT, et al. Reversal of vascular macrophage accumulation and hypertension by a CCR2 antagonist in deoxycorticosterone/salt-treated mice. Hypertension. 2012 Nov;60(5):1207-12. [5]. Brodmerkel CM, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344. J Immunol. 2005 Oct 15;175(8):5370-8. [6]. Cassini MF, et al. Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. J Am Soc Nephrol. 2018 Oct;29(10):2471-2481. [7]. Dansereau MA, et al. Spinal CCL2 pronociceptive action is no longer effective in CCR2 receptor antagonist-treated rats. J Neurochem. 2008 Jul;106(2):757-69.

描述

相关类别

研究领域 >> 内分泌

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

参考文献

[1]. Xue CB, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8

[2]. Zhao W, et al. Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882.

[3]. Aye-Mon A, et al. CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. Mol Pain. 2018 Jan-Dec;14:1744806917751322.

[4]. Chan CT, et al. Reversal of vascular macrophage accumulation and hypertension by a CCR2 antagonist in deoxycorticosterone/salt-treated mice. Hypertension. 2012 Nov;60(5):1207-12.

[5]. Brodmerkel CM, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344. J Immunol. 2005 Oct 15;175(8):5370-8.

[6]. Cassini MF, et al. Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. J Am Soc Nephrol. 2018 Oct;29(10):2471-2481.