CCR
CCR产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S2907 |
PirfenidonePirfenidone (S-7701, AMR-69) 抑制TGF-β产生和TGF-β刺激的胶原蛋白产生,且降低TNF-α和IL-1β产生,具有抗纤维化和抗炎特性。Pirfenidone可减弱 chemokine (CC motif) ligand-2 (CCL2) 和 CCL12的生成,并具有抗纤维化的活性。Phase 3。 |
![]() ![]() Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
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S2004New |
Vicriviroc MalateVicriviroc (SCH-417690, SCH-D)是一种有效的CCR5拮抗剂,IC50为0.91 nM,对遗传多样性的HIV-1分离株具有广谱活性,对具有RTI, PRI,和MDR表型的病毒也具有耐药性。Phase 3。 |
![]() ![]() Effect of CCR5 receptor antagonists/ligands on LukED cytotoxicity and HIV infection. (a) Viability of Jurkat-R5 cells pre-incubated with CCR5 small molecule antagonists maraviroc (MVC), vicriviroc (VVC), or TAK-779 (TAK) (1μg/mL to 2.5 pg/mL) followed by incubation with LukED (5 μg/mL) and quantification of cell viability via FACS scatter. (b) HIV infection of Hut-R5 cells after incubation with the same CCR5 antago-nists as in (a) (1μg/mL to 64 pg/mL) and subsequent incubation with CCR5-tropic HIV-1 virus encoding the mouse heat-stable antigen (HSA) as a reporter (HIV-R5) for 2.5 days. Infection success was determined by FACS analysis after staining cells for the HSA protein encoded by the virus. Mean and s.e.m. of infected cells from duplicate experiments is shown. |
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S3479New |
R243R243 是一种 Chemokine (C-C motif) receptor 8 (CCR8) 信号转导和趋化性的抑制剂。 |
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S3205New |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens(一种传统的抗氧化剂)的主要成分,可抑制BaP诱导的 AHR 的活化和 ROS 的产生,抑制 BaP/AHR 介导的 CCL2 chemokine 的释放,并激活 NRF2/HO1 抗氧化剂途径。 |
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S8512New |
CenicrivirocCenicriviroc (CVC, TAK-652, TBR-652) 是一种有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的双效抑制剂。Cenicriviroc 还可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性。 |
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S0777New |
APX-115 free baseAPX-115 free base (Ewha-18278 free base) 是一种有效的、口服活性的 pan NADPH oxidase (pan-Nox) 的抑制剂,对Nox1、Nox2和Nox4的Ki值分别为1.08 μM、0.57 μM 和 0.63 μM。APX-115 free base (Ewha-18278 free base) 可在糖尿病性肾中显著地抑制 MCP-1/CCL2、IL-6 和 TNFα。 |
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S3032 |
BindaritBindarit (AF 2838) 是天然化合物,具有特定抗炎活性,因为选择性抑制炎症趋化因子亚家族,包括单核细胞趋化蛋白MCP-1/CCL2, MCP-3/CCL7, 和 MCP-2/CCL8。 |
![]() ![]() Differential participation of ATRs or MCP-1/CCR2 signaling in RVLM in pressor response and tachycardia after stroke. Changes in mean diastolic (ΔDBP) blood pressure or heart rate (ΔHR) relative to baseline in rats that received pretreatment by microinjection bilaterally into the RVLM of bindarit (Bin; 10 nmol, MCP-1 synthesis inhibitor), BMS CCR2 22 (BMS; 10 pmol, CCR2 antagonist), propagermanium (Prop; 10 pmol, CCR2 antagonist) or vehicle control (Veh).Values are mean ± SEM, n = 5-7 animals per experimental group. *P < 0.05 versus SC group, and +P < 0.05 versus Veh (Saline) + MCAO group in the post hoc Scheffe multiple-range test.
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S2003 |
MaravirocMaraviroc (UK-427857)是一种CCR5拮抗剂,作用于MIP-1α,MIP-1β和RANTES,无细胞试验中IC50分别为3.3 nM,7.2 nM和5.2 nM。Maraviroc可应用于治疗HIV感染。 |
![]() ![]() CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D. |
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S0129New |
SB-297006SB-297006 是一种 C-C chemokine receptor 3 (CCR3) 的拮抗剂,可抑制抗原诱导的T(h)2和嗜酸性粒细胞在肺中的累积。SB-297006 可抑制CCL11诱导的Th2趋化性,其IC50值为2.5 μM。 |
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S0085New |
BMS-813160BMS-813160 是一种有效的、吸收良好的 CCR2 和 CCR5 趋化因子的双重拮抗剂。BMS-813160 可抑制炎症过程、血管生成、肿瘤细胞迁移、肿瘤细胞的增殖和侵袭。 |
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S6555 |
AZD2098AZD2098是有效的CCR4 receptor拮抗剂,pIC50为7.8。 |
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S8501 |
Adaptavir (DAPTA)Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) 是一种水溶性的、有效的、选择性CCR5拮抗剂,有效地抑制特异性依赖于CD4的CCR5与gp120 Bal和CM235的结合,IC50分别为0.06 nM和0.32 nM。 |
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S8324 |
ZK756326 2HClZK756326是CCR8(趋化因子受体8)的完全激动剂。IC50为1.8 μM。它可剂量依赖性地引起胞内钙含量的增加以及CCL1与受体的交叉脱敏。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S2907 |
PirfenidonePirfenidone (S-7701, AMR-69) 抑制TGF-β产生和TGF-β刺激的胶原蛋白产生,且降低TNF-α和IL-1β产生,具有抗纤维化和抗炎特性。Pirfenidone可减弱 chemokine (CC motif) ligand-2 (CCL2) 和 CCL12的生成,并具有抗纤维化的活性。Phase 3。 |
![]() ![]() Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
|
|
S2004New |
Vicriviroc MalateVicriviroc (SCH-417690, SCH-D)是一种有效的CCR5拮抗剂,IC50为0.91 nM,对遗传多样性的HIV-1分离株具有广谱活性,对具有RTI, PRI,和MDR表型的病毒也具有耐药性。Phase 3。 |
![]() ![]() Effect of CCR5 receptor antagonists/ligands on LukED cytotoxicity and HIV infection. (a) Viability of Jurkat-R5 cells pre-incubated with CCR5 small molecule antagonists maraviroc (MVC), vicriviroc (VVC), or TAK-779 (TAK) (1μg/mL to 2.5 pg/mL) followed by incubation with LukED (5 μg/mL) and quantification of cell viability via FACS scatter. (b) HIV infection of Hut-R5 cells after incubation with the same CCR5 antago-nists as in (a) (1μg/mL to 64 pg/mL) and subsequent incubation with CCR5-tropic HIV-1 virus encoding the mouse heat-stable antigen (HSA) as a reporter (HIV-R5) for 2.5 days. Infection success was determined by FACS analysis after staining cells for the HSA protein encoded by the virus. Mean and s.e.m. of infected cells from duplicate experiments is shown. |
|
S3479New |
R243R243 是一种 Chemokine (C-C motif) receptor 8 (CCR8) 信号转导和趋化性的抑制剂。 |
||
S3205New |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens(一种传统的抗氧化剂)的主要成分,可抑制BaP诱导的 AHR 的活化和 ROS 的产生,抑制 BaP/AHR 介导的 CCL2 chemokine 的释放,并激活 NRF2/HO1 抗氧化剂途径。 |
||
S8512New |
CenicrivirocCenicriviroc (CVC, TAK-652, TBR-652) 是一种有效的、口服活性的 CC chemokine receptor 2 (CCR2) 和 CCR5 的双效抑制剂。Cenicriviroc 还可抑制 HIV-1 和 HIV-2 并具有有效的抗炎和抗感染活性。 |
||
S0777New |
APX-115 free baseAPX-115 free base (Ewha-18278 free base) 是一种有效的、口服活性的 pan NADPH oxidase (pan-Nox) 的抑制剂,对Nox1、Nox2和Nox4的Ki值分别为1.08 μM、0.57 μM 和 0.63 μM。APX-115 free base (Ewha-18278 free base) 可在糖尿病性肾中显著地抑制 MCP-1/CCL2、IL-6 和 TNFα。 |
||
S3032 |
BindaritBindarit (AF 2838) 是天然化合物,具有特定抗炎活性,因为选择性抑制炎症趋化因子亚家族,包括单核细胞趋化蛋白MCP-1/CCL2, MCP-3/CCL7, 和 MCP-2/CCL8。 |
![]() ![]() Differential participation of ATRs or MCP-1/CCR2 signaling in RVLM in pressor response and tachycardia after stroke. Changes in mean diastolic (ΔDBP) blood pressure or heart rate (ΔHR) relative to baseline in rats that received pretreatment by microinjection bilaterally into the RVLM of bindarit (Bin; 10 nmol, MCP-1 synthesis inhibitor), BMS CCR2 22 (BMS; 10 pmol, CCR2 antagonist), propagermanium (Prop; 10 pmol, CCR2 antagonist) or vehicle control (Veh).Values are mean ± SEM, n = 5-7 animals per experimental group. *P < 0.05 versus SC group, and +P < 0.05 versus Veh (Saline) + MCAO group in the post hoc Scheffe multiple-range test.
|
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S2003 |
MaravirocMaraviroc (UK-427857)是一种CCR5拮抗剂,作用于MIP-1α,MIP-1β和RANTES,无细胞试验中IC50分别为3.3 nM,7.2 nM和5.2 nM。Maraviroc可应用于治疗HIV感染。 |
![]() ![]() CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D. |
|
S0129New |
SB-297006SB-297006 是一种 C-C chemokine receptor 3 (CCR3) 的拮抗剂,可抑制抗原诱导的T(h)2和嗜酸性粒细胞在肺中的累积。SB-297006 可抑制CCL11诱导的Th2趋化性,其IC50值为2.5 μM。 |
||
S0085New |
BMS-813160BMS-813160 是一种有效的、吸收良好的 CCR2 和 CCR5 趋化因子的双重拮抗剂。BMS-813160 可抑制炎症过程、血管生成、肿瘤细胞迁移、肿瘤细胞的增殖和侵袭。 |
||
S6555 |
AZD2098AZD2098是有效的CCR4 receptor拮抗剂,pIC50为7.8。 |
||
S8501 |
Adaptavir (DAPTA)Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) 是一种水溶性的、有效的、选择性CCR5拮抗剂,有效地抑制特异性依赖于CD4的CCR5与gp120 Bal和CM235的结合,IC50分别为0.06 nM和0.32 nM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8324 |
ZK756326 2HClZK756326是CCR8(趋化因子受体8)的完全激动剂。IC50为1.8 μM。它可剂量依赖性地引起胞内钙含量的增加以及CCL1与受体的交叉脱敏。 |