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  • ATI-2341 (trifluoroacetate salt)
ATI-2341 (trifluoroacetate salt)的可视化放大

ATI-2341 (trifluoroacetate salt)

A neuropeptide with diverse biological activities

原价
¥1837-11887
价格
1470-9510
ATI-2341 (trifluoroacetate salt)的二维码

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  • 库存: 现货
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  • 货号: ajcx21736
  • CAS: N/A
  • 别名:
  • 分子式: C104H178N26O25S2.XCF3COOH
  • 分子量: 2256.8
  • 纯度: >98%
  • 溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml
  • 储存: Store at -20°C
  • 库存: 现货

Background

ATI-2341 is a pepducin Gαi-signaling biased agonist of chemokine (C-X-C motif) receptor 4 (CXCR4).1 It induces dissociation of Gαi and Gγ2, indicating activation of Gαi-signaling, with an EC50 value of 0.21 µM in a bioluminescence resonance energy transfer (BRET) assay using HEK293T cells expressing CXCR4. ATI-2341 is selective for Gαi over Gα13 (EC50s = 0.53 and >1 µM, respectively, in BRET engagement assays) and is biased for Gαi engagement over β-arrestin-2, G protein-coupled receptor kinase 2 (GRK2), or GRK3 recruitment, exhibiting bias factor values of 24, 24.9, and 30, respectively. It induces chemotaxis of CCRF-CEM T cells, which endogenously express CXCR4, in a concentration-dependent manner. ATI-2341 (0.45 µmol/kg) increases peritoneal lavage fluid infiltration of polymorphonuclear leukocytes (PMNs) in mice.2



1.Quoyer, J., Janz, J.M., Luo, J., et al.Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G proteinProc. Natl. Acad. Sci. USA110(52)5088-5097(2013) 2.Tchernychev, B., Ren, Y., Sachdev, P., et al.Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cellsProc. Natl. Acad. Sci. USA107(51)22255-22259(2010)

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