AMG 487

CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses³. AMG 487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle⁴. AMG487 treatment in collagen-induced arthritis(CIA) mice decreased mRNA and protein expression levels of CXCR3, IL-17A, RORγt, and STAT3. Therefore, it can be concluded that the anti-arthritic effect of AMG487 is caused by the inhibitory action on IL-17A and by downregulating RORγt/STAT3 expression in CIA the model⁵. Pharmacological blockade of CXCR3 using local injection of its inhibitor, AMG487, into the anterior cingulate cortex (ACC) significantly attenuated hyperalgesia induced by chronic constriction injury and suppressed the phosphorylation of extracellular signal-regulated kinase (ERK)⁶. AMG487 application might alleviate PDGFR-β and occludin loss, and decreased the residual content of retinal albumin in the streptozocin-induced DR mouse model via the inhibition of oxidative and endoplasmic reticulum stress, in which p38 activation was also involved⁷. AMG487 significantly alleviated joint inflammation by decreasing GITR+CD25+, GITR+CD45+, GITR+IL-9+, GITR+NF-κB+ CD45+CD4+, CD45+CCR6+, CD45+IL-6+ cells, CD45+IL-17A+, and CD45+IL-21+, and increasing GITR+Foxp3+ and GITR+STAT6+ cells⁸.

溶解方案(细胞实验)

DMSO 中的溶解度 : ≥ 41 mg/mL (67.93 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|* "≥" means soluble, but saturation unknown.

溶解方案(动物实验)

"方案一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (4.14 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: 2.5 mg/mL (4.14 mM); 悬浊液; 超声助溶 此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (4.14 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"

"方案一": "请依序添加每种溶剂：20% HP-β-CD in SalineSolubility: 5 mg/mL (8.28 mM); Suspened solution; 超声助溶"