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ATI-2341 是 C-X-C 趋化因子受体 4 型功能选择性变构激动剂,作为偏向配体有利于 Gα1 激活。它是一种变构激动剂,可激活抑制性异源三聚体 G 蛋白 (Gi) 以促进抑制 cAMP 产生并诱导钙动员。

ATI-2341 是 C-X-C 趋化因子受体 4 型功能选择性变构激动剂,作为偏向配体有利于 Gα1 激活。它是一种变构激动剂,可激活抑制性异源三聚体 G 蛋白 (Gi) 以促进抑制 cAMP 产生并诱导钙动员。
| 规格 | 价格 | 库存 | 数量 | 
|---|---|---|---|
| 100 mg |  待询   | 5日内发货 | 
ATI-2341 相关产品
| 产品描述 | ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.  | 
| 靶点活性 |  CXCR4:194 nM(EC50)  | 
| 体外活性 | ATI-2341能够在表达CXCR4的细胞中引发与CXCR4及G蛋白依赖的信号传导、受体内化和趋化性。它是亲和力较高的激动剂,具有194 ± 16 nM的EC50值和81 ± 4%的内在活性。ATI-2341是一种高效的骨髓PMNs(多形核白细胞)和HSPCs(造血干细胞和前体细胞)动员剂,为HSPCs招募至ABMT(自体骨髓移植)前的治疗方法提供了新的策略。同时,ATI-2341能引起CCRF-CEM细胞的趋化性,产生典型的趋化剂所观察到的钟形曲线[1]。  | 
| 体内活性 | 腹腔内给予BALB/c小鼠ATI-2341(i.p.注射)会引起剂量依赖性的PMNs向腹膜的招募,最大效应出现在405 nmol/kg时。ATI-2341的更高浓度会导致招募减少,这种现象与化学趋化剂通常见到的钟形曲线相似。ATI-2341通过静脉(i.v.)给药后,小鼠外周血液中PMNs的数量呈剂量依赖性增加,在给药后90分钟测量达到最大效应,此时ATI-2341的浓度为0.66 μMol/kg。在所有测试剂量下,ATI-2341对淋巴细胞的动员均无影响[1]。  | 
| 细胞实验 | Receptors(CXCR4-eGFP) are transiently transfected into HEK-293 cells and are plated 24 h after transfection on glass coverslips coated with poly-D-lysine. The next day, cells are treated with either vehicle alone or with varying concentrations of ATI-2341 for 30 min at 37 °C followed by fixation with methanol for 5 min at −20 °C. GFP fluorescence is visualized directly using a Zeiss Axiovert inverted microscope. Images are processed using Adobe Photoshop and Adobe Illustrator. (Only for Reference)  | 
| 别名 | ATI2341 | 
| 分子量 | 2256.82 | 
| 分子式 | C104H178N26O25S2 | 
| CAS No. | 1337878-62-2 | 
| 密度 | 1.36 g/cm3 (Predicted) | 
| Sequence Short | 1-Oxohexadecyl-MGYQKKLRSMTDKYRL | 
| 存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | 
| 溶解度信息 | Ethanol: 2 mg/mL (0.89 mM), Sonication is recommended.  DMSO: 93 mg/mL (41.21 mM), Sonication is recommended.  H2O: <1 mg/mL   | 
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