1. Signaling Pathways
  2. GPCR/G Protein
    Immunology/Inflammation
  3. CXCR

CXCR

CXCRs (CXC chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CXC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins, since they span thecell membrane seven times. There are currently seven known CXC chemokine receptors in mammals, named CXCR1 through CXCR7. CXCR1 and CXCR2 are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif. CXCR3 is expressed predominantly on T lymphocytes. CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1) and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectively expressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6 was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on its chromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originally called RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response to CXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.

CXCR 相关产品 (55):

Cat. No. Product Name Effect Purity
  • HY-10046
    Plerixafor Antagonist >98.0%
    Plerixafor (AMD 3100) 是选择性的 CXCR4 拮抗剂,IC50值为44 nM。
  • HY-16711
    SB225002 Antagonist 99.78%
    SB225002 是一种有效的选择性 CXCR2 非肽拮抗剂,抑制 125I-IL-8 和 CXCR2 结合的 IC50 为 22 nM。
  • HY-15319
    AMG 487 Inhibitor 99.65%
    AMG 487 是一种有效的、具有口服活性的、选择性的趋化因子受体3 (CXCR3) 拮抗剂,抑制 CXCL10和 CXCL11与 CXCR3 结合的 IC50 值分别为 8.0 和 8.2 nM。
  • HY-10198
    Navarixin Antagonist 98.62%
    Navarixin 是一种有效的 CXCR1CXCR2 的别构拮抗剂,对猕猴 CXCR1 的 Kd 值为 41 nM,对小鼠,大鼠和猕猴 CXCR2 的 Kd 值分别为 0.20 nM,0.20 nM,0.08 nM。
  • HY-19855
    AZD-5069 Antagonist 99.92%
    AZD-5069 是有效的 CXCR2 chemokine 受体拮抗剂,用于癌症治疗。
  • HY-119339
    SX-682 Inhibitor 98.52%
    SX-682 是口服有效的 CXCR1CXCR2 变构抑制剂。SX-682 可以阻断肿瘤髓系抑制细胞 (MDSCs) 募集并增强 T 细胞活化和抗肿瘤免疫。
  • HY-P0172A
    ATI-2341 TFA Agonist 99.91%
    ATI-2341 是一种有效的 C-X-C 趋化因子受体 4 型 (CXCR4) 功能选择性变构激动剂,其作为偏向配体起作用,有利于 Gα1激活而不是 Gα13。ATI-2341 激活抑制性异源三聚体 G 蛋白 (Gi) 以促进 cAMP 产生的抑制并诱导钙动员。ATI-2341 是一种有效骨髓多形核中性粒细胞 (PMNs) 和造血干细胞和祖细胞 (HSPCs) 动员剂。
  • HY-50688
    SB-265610 Antagonist
    SB-265610 是一种选择性的竞争性非肽变构 CXCR2 拮抗剂。SB-265610 阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50 分别为 3.7 nM 和 70 nM。
  • HY-50912
    Plerixafor octahydrochloride Antagonist >98.0%
    Plerixafor octahydrochloride (AMD3100 octahydrochloride) 是一种选择性的 CXCR4 拮抗剂, IC50 为 44 nM。
  • HY-15251
    Reparixin Inhibitor 99.98%
    Reparixin是趋化因子受体 CXCR1CXCR2 激活的非竞争性变构抑制剂,IC50 分别为1 和 100 nM。
  • HY-13848
    AZD8797 Antagonist 98.65%
    AZD8797 是非竞争性、可口服的人 CX3CR1 变构调节剂,拮抗 CX3CR1 和 CXCR2,Ki 分别为 3.9 和 2800 nM。
  • HY-50101A
    Mavorixafor trihydrochloride Antagonist 99.14%
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 是一种有效的,选择性的,可口服的 CXCR4 拮抗剂,能够拮抗 125I-SDF 与 CXCR4 结合,IC50 值为 13 nM;Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 能够抑制 HIV-1 (NL4.3 strain) 的复制,在 MT-4 和 PBMCs 细胞中,IC50 值分别为 1 和 9 nM。
  • HY-P0171
    Motixafortide Antagonist 99.19%
    Motixafortide (BKT140 4-fluorobenzoyl) 是一种新型的CXCR4拮抗剂,IC50约为1 nM。
  • HY-12488
    LY2510924 Inhibitor 99.91%
    LY2510924是有效,选择性的 CXCR4 拮抗剂;阻止SDF-1结合CXCR4,IC50值为0.079 nM。
  • HY-15252
    Reparixin L-lysine salt Inhibitor 99.97%
    Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。
  • HY-10017
    SCH 546738 Antagonist 99.23%
    SCH 546738 是一种有效、可口服的非竞争性 CXCR3 拮抗剂,结合到人 CXCR3 受体的亲和常数 (Ki) 为 0.4 nM。
  • HY-13406
    TAK-779 Antagonist 99.73%
    TAK-779 是一种有效的,选择性的,非肽类 CCR5CXCR3 拮抗剂,对 CCR5Ki 值为 1.1 nM,同时可以有效地,选择性地抑制 R5 HIV-1,在 MAGI-CCR5 细胞中,EC50EC90 值分别为 1.2 nM 和 5.7 nM。
  • HY-101458A
    IT1t dihydrochloride Antagonist 99.97%
    IT1t dihydrochloride是高效的CXCR4拮抗剂;抑制CXCL12/CXCR4相互作用的IC50值为2.1 nM。
  • HY-N0011
    Baohuoside I Inhibitor 99.70%
    Baohuoside I 是从朝鲜淫羊藿中得到的黄酮类化合物,作为 CXCR4 的抑制剂,能够抑制 CXCR4 的表达,诱导凋亡,具有抗肿瘤活性。
  • HY-19768
    Danirixin Antagonist 98.21%
    Danirixin 是选择性,可逆的 CXCR2 拮抗剂。抑制 CXCL8的 IC50 值为 12.5 nM。
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