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Cat. No. | Product Name | Target | Signaling Pathways |
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T36982 |
CXCR3 Antagonist 6c
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CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM). 1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva... | |||
T10297L |
AMG 487
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CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AMG 487 是可口服的选择性趋化因子受体3拮抗剂,对 I-IP-10、I-ITAC 和 MIG 的 IC50 值分别为 8、15 和 36nM。 | |||
T26035 |
rac-NBI-74330
rac NBI 74330,racNBI74330 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
rac-NBI-74330是一种有效的、选择性的 CXCR3拮抗剂。 | |||
T7499 |
TAK-779
Takeda 779 |
HIV Protease; CXCR; CCR | Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome |
TAK-779 (Takeda 779) 是一种非肽类CCR5和CXCR3 拮抗剂,对CCR5的Ki 值为 1.1 nM,并选择性抑制R5 HIV-1。 | |||
T3360 |
ZK 756326
ZK756326 2HCl |
CCR | Immunology/Inflammation; Microbiology/Virology |
ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂(IC50:1.8 μM,在人体内;2.6 μM,在小鼠体内)。对 CCR4/5 和 CXCR3/4 没有活性,比其他 26 种 GPCR 的选择性高 28 倍(对 α2A 和 5-HT 受体的选择性较低)。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。 | |||
T16863 |
SCH 546738
|
Others | Others |
SCH 546738 is an effective and non-competitive CXCR3 antagonist. SCH 546738 bindings to the human CXCR3 receptor is determined (Ki: 0.4 nM) in multiple experiments. | |||
T70616 |
ACT-672125
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ACT-672125 is a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases. ACT-672125 showed good physicochemical properties and safety profile. In a proof-of-mechanism model of lung inflammation, ACT-672125 inhibited the recruitment of CXCR3 expressing T cells into the inflamed lung in a dose-dependent manner. | |||
T12567 | PS372424 | Others | Others |
PS372424 is a specific agonist of human CXCR3, with anti-inflammatory activity. | |||
T70411 | PS372424 HCl | ||
PS372424 is a specific agonist of human CXCR3. It has been shown to induce phosphorylation of ERK and block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice. | |||
T24949 |
VUF10132
VUF-10132,VUF 10132 |
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VUF10132 is a full inverse CXCR3 N3.35A agonist. | |||
T29147 |
VUF5834
VUF-5834,VUF 5834 |
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VUF5834 is a full inverse agonist of CXCR3 N3.35A. | |||
T22477 |
(±)-AMG 487
|
Others | Others |
AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively). | |||
T10297 | AMG 487 (S-enantiomer) | Others | Others |
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an CXCR3 antagonist. | |||
T35085 |
VUF-11222
VUF 11222 |
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VUF-11222 is an agonist of high affinity non-peptide CXCR3 agonist (pKi = 7.2). | |||
T63761 | ACT-660602 | ||
ACT-660602 是口服具有活力的趋化因子受体 CXCR3 拮抗剂 (IC50: 204 nM)。ACT-660602 能够抑制 T 细胞迁移,并在体内急性肺损伤模型中显示出显著作用。ACT-660602 能够用于研究自身免疫性疾病。 | |||
T23656 |
VUF11211
VUF-11211,VUF 11211 |
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VUF11211 is an effective antagonist of CXCR3 that acts by extending from the minor pocket into the major pocket of the transmembrane domains. | |||
T73148 |
ACT-777991
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ACT-777991为一种选择性、口服生效的CXCR3拮抗剂,于动物模型中展现出微粒体及肝细胞稳定性,能抑制活化T细胞向CXCL11迁移。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T3765 |
L-asarinin
細辛素,(-)-Episesamin |
Others | Others |
L-asarinin ((-)-Episesamin) 降低外周血 IL-12 浓度并抑制 CXCR3 和 TLR4 的表达,这意味着 Asarinin 可能在 TLR4 通路中发挥作用,并延长同种异体心脏的存活时间。 |