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抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T36982 CXCR3 Antagonist 6c

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

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

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

VUF10132 is a full inverse CXCR3 N3.35A agonist.
T29147 VUF5834

VUF-5834,VUF 5834

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

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

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

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。

化合物

CXCR3 Antagonist 6c
Cat.No: T36982
Synonym:
Target:
AMG 487
Cat.No: T10297L
Synonym:
Target: CXCR
rac-NBI-74330
Cat.No: T26035
Synonym: rac NBI 74330,racNBI74330
Target: CXCR
TAK-779
Cat.No: T7499
Synonym: Takeda 779
Target: HIV Protease, CXCR, CCR
ZK 756326
Cat.No: T3360
Synonym: ZK756326 2HCl
Target: CCR
SCH 546738
Cat.No: T16863
Synonym:
Target: Others
ACT-672125
Cat.No: T70616
Synonym:
Target:
PS372424
Cat.No: T12567
Synonym:
Target: Others
PS372424 HCl
Cat.No: T70411
Synonym:
Target:
VUF10132
Cat.No: T24949
Synonym: VUF-10132,VUF 10132
Target:
VUF5834
Cat.No: T29147
Synonym: VUF-5834,VUF 5834
Target:
(±)-AMG 487
Cat.No: T22477
Synonym:
Target: Others
AMG 487 (S-enantiomer)
Cat.No: T10297
Synonym:
Target: Others
VUF-11222
Cat.No: T35085
Synonym: VUF 11222
Target:
ACT-660602
Cat.No: T63761
Synonym:
Target:
VUF11211
Cat.No: T23656
Synonym: VUF-11211,VUF 11211
Target:
ACT-777991
Cat.No: T73148
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。

天然产物

L-asarinin
Cat.No: T3765
Synonym: 細辛素,(-)-Episesamin
Target: Others
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