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 相关产品 (35):

Cat. No. Product Name Effect Purity
  • HY-10046
    Plerixafor Antagonist >98.0%
    Plerixafor 是一种选择性的 CXCR4 拮抗剂,IC50 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 是一种有效的 CXCL8 受体 CXCR1/2 变构抑制剂,微弱抑制 CXCR2- 调节的细胞迁移 (IC50=100 nM),但强抑制 CXCR1- 调节的细胞趋化 (IC50=1 nM)。
  • HY-10198
    SCH 527123 Antagonist 99.06%
    SCH 527123 是一种有效的 CXCR1CXCR2 的别构拮抗剂,IC50 分别为 1000 nM 和 3-6 nM。
  • HY-15252
    Reparixin L-lysine salt Inhibitor 98.44%
    Reparixin L-lysine salt 是一种有效的 CXCL8 受体 CXCR1/2 变构抑制剂,微弱抑制 CXCR2- 调节的细胞迁移 (IC50=100 nM),但强抑制 CXCR1- 调节的细胞趋化 (IC50=1 nM)。
  • HY-P7061A
    ALX 40-4C Trifluoroacetate Inhibitor 98.15%
    ALX 40-4C Trifluoroacetate 是一种趋化因子受体 (chemokine receptor CXCR4) 抑制剂,ALX 40-4C Trifluoroacetate 具有抗 HIV-1 作用;同时为 APJ 受体拮抗剂,IC50 值为 2.9 μM。
  • HY-112154
    CXCR7 modulator 2 Modulator
    CXCR7 modulator 2 是 CXCR7 的调节剂,其 Ki 值为 13 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-15319
    AMG 487 Inhibitor 99.65%
    AMG 487 是一种有效的趋化因子受体 CXCR3 拮抗剂,能够抑制 125I-IP-10 和 125I-ITAC 与 CXCR3 结合,IC50 值分别为 8.0 和 8.2 nM。
  • 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-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-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-19768
    Danirixin Antagonist 98.23%
    Danirixin 是一种选择性的,可逆的 CXCR2 拮抗剂,也可抑制 CXCL8,其 IC50 值为 12.5 nM。
  • HY-P0171
    BKT140 4-fluorobenzoyl Antagonist 99.19%
    BKT140是一种新型的CXCR4拮抗剂, IC50约为1 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 2 和 26 nM。
  • HY-13848
    AZD8797 Antagonist 98.22%
    AZD8797是人类CX3CR1受体的变构非竞争性调节剂; 在B淋巴细胞细胞系和人全血中拮抗CX3CL1的IC50值分别为6和300 nM。
  • 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。
  • HY-10011
    SCH 563705 Antagonist
    SCH 563705 是一种有效的,可口服的 CCR2CCR1 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。
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