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

CXCR (CXC趋化因子受体)

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 亚型特异性产品:

  • CXCR

  • CXCR1

  • CXCR2

  • CXCR3

  • CXCR4

  • CXCR7

  • CXCR6

CXCR 相关产品 (68):

目录号 产品名 作用方式 纯度
  • HY-10046
    Plerixafor Antagonist ≥98.0%
    Plerixafor (AMD 3100) 是选择性的 CXCR4 拮抗剂,IC50 为 44 nM。Plerixafor 是一种免疫刺激剂和造血干细胞动员剂,也是 CXCR7 的变构激动剂。Plerixafor 抑制 HIV-1HIV-2 的复制,EC50 为 1-10 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 99.13%
    Navarixin (SCH 527123) 是一种有效的,具有口服活性的变构的 CXCR1CXCR2 拮抗剂,对猕猴 CXCR1Kd 值为 41 nM,对小鼠,大鼠和猕猴 CXCR2Kd 值分别为 0.20 nM,0.20 nM 和 0.08 nM。
  • HY-19855
    AZD-5069 Antagonist 99.63%
    AZD-5069 是有效的 CXCR2 chemokine 受体拮抗剂,用于癌症的研究。
  • HY-19519
    Ladarixin Antagonist 99.71%
    Ladarixin (DF 2156A free base) 是一种具有口服活性的,非竞争性的 CXCR1CXCR2 的变构抑制剂。Ladarixin 可用于 COPD 和哮喘的研究。
  • HY-19519A
    Ladarixin sodium Antagonist 99.86%
    Ladarixin sodium (DF 2156A) 是一种具有口服活性的,非竞争性的 CXCR1CXCR2 的变构抑制剂。Ladarixin sodium 可用于 COPD 和哮喘的研究。
  • HY-120878A
    (R,R)-CXCR2-IN-2 Antagonist 99.37%
    (R,R)-CXCR2-IN-2 是 CXCR2-IN-2 (compound 68) 的非对映异构体,是一种可透过血脑屏障的 CXCR2 拮抗剂,在 TANGO 试验中 pIC50 为 9,在 HWB Gro-α 诱导 CD11b 表达实验中 pIC50 为6.8。
  • 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-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-P0171
    Motixafortide Antagonist 99.03%
    Motixafortide (BKT140 4-fluorobenzoyl) 是一种新型的CXCR4拮抗剂,IC50约为1 nM。
  • HY-50101A
    Mavorixafor trihydrochloride Antagonist ≥98.0%
    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-13406
    TAK-779 Antagonist ≥98.0%
    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 99.23%
    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-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-111793A
    NUCC-390 dihydrochloride Agonist 99.59%
    NUCC-390 dihydrochloride 是新型的选择性小分子 CXCR4 receptor 受体激动剂。NUCC-390 dihydrochloride 可以诱导 CXCR4 受体的内化,作用方式与 AMD3100 (HY-10046) 相反。NUCC-390 dihydrochloride 在动物模型中,有助于神经退行性变后神经功能恢复。
  • 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-15320
    NBI-74330 Antagonist 99.23%
    NBI-74330 是一种有效的 CXCR3 拮抗剂,能够抑制 (125I)CXCL10 和 (125I)CXCL11 的特异性结合,Ki 值分别为 1.5 和 3.2 nM。
  • HY-19867A
    Burixafor hydrobromide Antagonist ≥98.0%
    Burixafor hydrobromide (TG-0054 hydrobromide) 是具有口服活性的、有效的 CXC 族趋化因子受体 4 (CXCR4) 的拮抗剂,是一种具有潜在研究脉络膜新生血管的抗血管生成剂。Burixafor hydrobromide (TG-0054 hydrobromide) 能够在猪心肌梗死模型中,动员间充质干细胞,减轻炎症反应,维持心脏的收缩功能。
  • HY-15252
    Reparixin L-lysine salt Inhibitor 99.93%
    Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。
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