1. GPCR/G Protein
  2. 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 Isoform Specific Products:

  • CXCR

  • CXCR1

  • CXCR2

  • CXCR3

  • CXCR4

  • CXCR7

  • CX3CR1

CXCR 相关产品 (34):

Cat. No. Product Name Effect Purity
  • HY-10046
    Plerixafor Antagonist >98.0%
    Plerixafor是选择性的 CXCR4 拮抗剂,IC50值为44 nM。
  • HY-50912
    Plerixafor octahydrochloride Antagonist 98.90%
    Plerixafor octahydrochloride是一种选择性的 CXCR4 拮抗剂, IC50 为 44 nM。
  • HY-15251
    Reparixin Inhibitor 99.88%
    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-15319
    AMG 487 Inhibitor 99.65%
    AMG 487 是一种有效的趋化因子受体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 99.06%
    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-107456
    E6130 Modulator
    E6130 是一种可口服的,高度选择性的 CX3CR1 调节剂,有治疗炎症性肠病的潜力。
  • HY-112154
    CXCR7 modulator 2 Modulator
    CXCR7 modulator 2 是 CXCR7 的调节剂,其 Ki 值为 13 nM。
  • HY-15252
    Reparixin L-lysine salt Inhibitor 98.44%
    Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。
  • HY-12488
    LY2510924 Inhibitor >98.0%
    LY2510924是有效,选择性的CXCR4拮抗剂;阻止SDF-1结合CXCR4的IC50值为0.079 nM。
  • HY-16711
    SB225002 Antagonist 99.58%
    SB225002 是一种有效的选择性 CXCR2 拮抗剂,IC50 为 22 nM。
  • HY-19855
    AZD-5069 Antagonist 98.97%
    AZD-5069 是有效的 CXCR2 chemokine 受体拮抗剂,用于癌症治疗。
  • HY-10017
    SCH 546738 Antagonist 99.20%
    SCH 546738 是一种有效的非竞争性 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-19768
    Danirixin Antagonist 98.23%
    Danirixin 是选择性,可逆的 CXCR2 拮抗剂。抑制 CXCL8的 IC50 值为 12.5 nM。
  • HY-P0171
    BKT140 4-fluorobenzoyl Antagonist 99.19%
    BKT140 4-fluorobenzoyl 是一种新型的CXCR4拮抗剂,IC50约为1 nM.
  • HY-13848
    AZD8797 Antagonist 98.22%
    AZD8797是非竞争的人 CX3CR1 变构调节剂,Ki分别为3.9,2800 nM。
  • HY-50101A
    AMD-070 hydrochloride Antagonist >98.0%
    AMD-070 hydrochloride 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;AMD-070 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-10011
    SCH 563705 Antagonist
    SCH 563705 是一种有效的,可口服的 CXCR2CXCR1 拮抗剂,IC50 值分别为 1.3 nM 和 7.3 nM,Ki 值分别为 1 nM 和 3 nM。
  • HY-15971
    AMD 3465 hexahydrobromide Antagonist 98.79%
    AMD 3465 hexahydrobromide 是一种有效的 CXCR4 拮抗剂,在 SupT1 细胞中,能够抑制 2G5 mAb,CXCL12AF647CXCR4 的结合,IC50 值分别为 0.75 nM 和 18 nM;AMD 3465 同时可有效抑制 X4 HIV 的复制 (IC50,1-10 nM),但对 R5 HIV 病毒无作用。
  • HY-13696
    MSX-122 Antagonist 99.74%
    MSX-122 是一种 CXCR4 的部分拮抗剂,抑制 CXCR4/CXCL12 相互作用,IC50 值约为 10 nM;MSX-122 具有抗炎和抗转移的活性。
Isoform Specific Products

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