cxcr4 antagonist 4

CXCR4 antagonist 4 是口服具有活力的、有效的CXCR4拮抗剂，IC50 值为 24 nM。CXCR4 antagonist 4能够抑制 CYP 2D6 的活性，增加 PAMPA 的通透性，有效阻碍人类免疫缺陷病毒的进入 (IC50=7 nM)。

CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM.

CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor, with notable anti-HIV activity.

CXCR4 antagonist10（compound 21）作为一种CXCR4拮抗剂，具有7.8 nM的IC50， 在癌症研究领域显示出其重要性。

CXCR4 antagonist 7 (Compound PARA-B) 是可用于研究HIV 感染、炎症性疾病、癌症和 WHIM 综合症的CXCR4拮抗剂 (IC50 = 9.3 nM)。

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4. It demonstrates an IC50 value of 57 nM in CXCR4 antagonism. In addition, it effectively inhibits the increase in cytosolic calcium induced by CXCL12 with an IC50 value of 0.24 nM. Furthermore, Compound 3 shows efficacy in the inhibition of CXCL12 CXCR4-mediated cell migration [1].

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].

CXCR4 antagonist 5 (compound 23), a potent CXCR4 antagonist, exhibits high inhibition efficacy against CXCR4 with an IC50 value of 8.8 nM. It effectively suppresses CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and hinders CXCR4 CXCL12-mediated chemotaxis. Moreover, Compound 23 demonstrates favorable physicochemical properties and in vitro safety profiles, exhibiting only marginal to moderate inhibition of CYP isozymes and hERG [1].

CXCR4 antagonist 6 (compound 46) is a highly potent inhibitor of CXCR4 with an IC50 value of 79 nM. It effectively inhibits the cytosolic calcium flux induced by CXCL12, achieving an IC50 of 0.25 nM. Moreover, CXCR4 antagonist 6 demonstrates significant mitigation of cell migration mediated by the CXCL12 CXCR4 interaction. Notably, this compound exhibits remarkable efficacy in a mouse model of cancer metastasis [1].

CXCR4 antagonist 9 (Compound 2) is a potent CXCR4 antagonist displaying an IC50 of 15 nM. It effectively inhibits the cytosolic calcium increase induced by CXCL12, with an IC50 value of 1.3 nM [1].

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM).

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM). BMS-1166 hydrochloride is an inhibitor of PD-1 PD-L1 interaction (IC50: 1.4 nM). BMS-1166 rivalries the inhibitory effect of PD-1 PD-L1 immune checkpoint on T cell activation.

KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.

EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段，是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内，EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中，EPI-X4（16µmol kg）在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高，并与肾小球滤过率(GFR)成反比。

TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。

EPI-X4（hSA408–423 peptide），一种C-X-C 基序趋化因子受体 4（CXCR4）的拮抗剂，其 IC50 值为 8.6 μM。该化合物能够阻断 CXCL12 介导的信号传导，并有效抑制趋化因子引起的白血病细胞迁移与侵袭。此外，EPI-X4 在小鼠模型中展现了抗炎作用，并对 CXCR4 嗜性 HIV 具有抗病毒活性，同样的 IC50 为 8.6 μM。

Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂，对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。