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36

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T11481 GSK2239633A

CCR Immunology/Inflammation; Microbiology/Virology
GSK2239633A 是趋化因子受体 CCR4 的变构拮抗剂,将 [125I]-TARC 与人 CCR4 结合的 pIC50 为 7.96。
T5384 RS 504393

CCR Immunology/Inflammation; Microbiology/Virology
RS 504393 是一种高度选择性的 CCR2 趋化因子受体拮抗剂,作用于人重组 CCR2 和 CCR1 受体,IC50值分别为 89 nM 和大于 100 μM。
TQ0283 RS102895

CCR Immunology/Inflammation; Microbiology/Virology
RS102895 是一种CCR2拮抗剂,IC50值为 360 nM。
T4300 AZD2098

CCR Immunology/Inflammation; Microbiology/Virology
AZD2098 是选择性CCR4抑制剂,可用于哮喘研究,对人类、大鼠、小鼠和狗的 CCR4 pIC50 值分别为 7.8、8.0、8.0和7.6。
T4674 SB297006

SB 297006

CCR Immunology/Inflammation; Microbiology/Virology
SB297006 是一种CCR3拮抗剂,IC50为39 nM。它能够显著抑制 CCL11 处理的神经祖细胞的增殖和神经球形成。
TQ0103 INCB3344

CCR Immunology/Inflammation; Microbiology/Virology
INCB3344 是一种有效、特异性和口服生物可利用的 CCR2 拮抗剂,结合拮抗作用的 IC50 值为 9.5 nM (mCCR2) 和 5.1 nM (hCCR2),趋化活性拮抗作用的 IC50 值为 7.8 nM (mCCR2) 和 3.8 nM (hCCR2)。
T30258 AZD-4818

CCR1 antagonist

CCR Immunology/Inflammation; Microbiology/Virology
AZD-4818 (CCR1 antagonist) 是趋化因子CCR1的一种拮抗剂,可用于研究慢性阻塞性肺病。
T24700 R243

R 243,R-243

CCR Immunology/Inflammation; Microbiology/Virology
R243 是选择性的CCR8拮抗剂,可抑制CCL1/CCR8的相互作用,以及CCR8信号传导和趋化性,具有抗伤害感受和抗炎作用。
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。
T10425 AZ084

CCR Immunology/Inflammation; Microbiology/Virology
AZ084 是可口服的选择性 CCR8变构拮抗剂,其Ki 值为 0.9 nM,可研究哮喘。
T16111 ML604086

CCR Immunology/Inflammation; Microbiology/Virology
ML604086 是选择性CCR8抑制剂,抑制循环T 细胞上 CCL1 与 CCR8 结合,还抑制 CCL1 介导的趋化性并提高细胞内 Ca2 浓度。
T16091 MK-0812 Succinate

Others; CCR Immunology/Inflammation; Microbiology/Virology; Others
MK-0812 Succinate 是一种选择性CCR2拮抗剂。
T11699 J-113863

CCR Immunology/Inflammation; Microbiology/Virology
J-113863 是选择性的 CCR1 (CD18)拮抗剂,有抗炎作用,对人和小鼠 CCR1受体的 IC50值分别为 0.9 和 5.8 nM。它是人 CCR3的强效拮抗剂,还是小鼠 CCR3的弱效拮抗剂,IC50分别为 0.58 和 460 nM。
T4584 BMS-813160

BMS 813160

CCR Immunology/Inflammation; Microbiology/Virology
BMS-813160 是CCR2/CCR5双重拮抗剂。有用于心血管的研究潜力。
T12773 RS102895 hydrochloride

RS102895盐酸盐

Others; 5-HT Receptor; CCR GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Others
RS102895 hydrochloride 是一种CCR2拮抗剂,IC50值为 360 nM。
T3430 PF-4136309

INCB8761,PF 4136309

CCR Immunology/Inflammation; Microbiology/Virology
PF-4136309 (INCB8761) 是一种高效选择性和可口服的 CCR2拮抗剂,能够抑制人、小鼠和大鼠 CCR2,IC50值分别为 5.2、17 和 13 nM。
T2375 BX471

BX 471,BX-471,ZK-811752

CCR Immunology/Inflammation; Microbiology/Virology
BX471 (BX 471) 是可口服的非多肽 CCR1选择性拮抗剂,Ki 值为 1 nM,对其选择性是对 CCR2、CCR5 和 CXCR4 的 250 倍。
T17225 Vercirnon

CCX282-B,维塞诺,GSK-1605786,Traficet-EN

CCR Immunology/Inflammation; Microbiology/Virology
Vercirnon (Traficet-EN) 是可口服的选择性 CCR9拮抗剂,可抑制 CCR9 介导的 Molt-4 细胞上 Ca2+移动和趋化性,用于炎症性肠病的研究。
T10639 C-021 dihydrochloride

CCR Immunology/Inflammation; Microbiology/Virology
C-021 dihydrochloride 是一种有效的 CCR4 拮抗剂。 它有效抑制人和小鼠的功能趋化性,IC50 为 140 nM 和 39 nM。
T6016 Maraviroc

Celsentri,马拉维若,UK-427857,Selzentry

HIV Protease; CCR Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Maraviroc (Selzentry) 是一种 C-C 趋化因子受体 5 拮抗剂,具有抑制HIV 的活性。
T7624 DAPTA

DAPTA(TFA),D-Ala-peptide T-amide,Adaptavir

HIV Protease; CCR Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
DAPTA (Adaptavir) 是一种合成肽,是 CCR5抑制剂,有抗 HIV 的活性。
TQ0297 Cenicriviroc

TAK-652,TBR-652

HIV Protease; CCR Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Cenicriviroc (TAK-652) 是一种可口服的CCR2/CCR5拮抗剂,可抑制 HIV-1 和 HIV-2,具有抗炎、抗感染作用。
T13114 CCR2 antagonist 4

Teijin compound 1

CCR Immunology/Inflammation; Microbiology/Virology
CCR2 antagonist 4 (Teijin compound 1) 是高效的、特异性的CCR2拮抗剂,对 CCR2b 的IC50为 180 nM,抑制 MCP-1 诱导的趋化作用的 IC50为 24 nM。
T21870 C-021

4-​Quinazolinamine, 2-​[1,​4'-​bipiperidin]​-​1'-​yl-​N-​cycloheptyl-​6,​7-​dimethoxy-

CCR Immunology/Inflammation; Microbiology/Virology
C 021 dihydrochloride 是一种 CC 趋化因子受体 4 (CCR4) 拮抗剂,抑制人和小鼠的功能趋化性,IC50分别为 140 和 39 nM。C-021 (4-​Quinazolinamine, 2-​[1,​4'-​bipiperidin]​-​1'-​yl-​N-​cycloheptyl-​6,​7-​dimethoxy-) 可有效阻止人 CCL22 衍生的 [35S]GTPγS 与受体结合,IC50为 18 nM。
T14900 CCR2-RA-[R]

(5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮

CCR Immunology/Inflammation; Microbiology/Virology
CCR2-RA-[R] 是一种 C-C 趋化因子受体 2 型 (CCR2) 变构拮抗剂,IC50值为103 nM。
T3435 Vicriviroc maleate

维立韦罗马来酸盐,SCH-D (maleate),SCH-417690 (maleate)

HIV Protease; CCR Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Vicriviroc maleate (SCH-417690 (maleate)) 是一种可口服,可透过血脑屏障的 CCR5选择性拮抗剂,同时抑制外周血单核细胞中的 HIV-1 的活性。
T2386 Pirfenidone

S-7701,AMR-69,S-7701,AMR69,吡非尼酮

CCR; TGF-beta/Smad Immunology/Inflammation; Microbiology/Virology; Stem Cells
Pirfenidone (AMR69) 是一种抗纤维化剂,可减弱纤维细胞中CCL2和CCL12的产生。它可抑制细胞生长,并能降低人胶质瘤细胞系中的TGF-β2蛋白水平,具有抗炎活性。
T76782 Mogamulizumab

KW-0761

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
Mogamulizumab (KW-0761) 是一种针对 T 细胞 CC 趋化因子受体 4 的 单克隆抗体。Mogamulizumab 具有抗癌活性,通过抗体依赖性细胞毒性 (ADCC) 消除肿瘤细胞,可用于研究癌症、成人T细胞白血病/淋巴瘤 (ATLL)、皮肤T细胞淋巴瘤(CTCL)。
T68984 AF-399/42018025

AF-399/42018025 is a CC chemokine receptor 4 (CCR4) antagonist.
T29181 YM-355179

YM 355179

YM-355179 is a novel, selective antagonist of CC chemokine receptor 3 with oral activity.
T69830 GSK2239633

GSK2239633 is a potent CC-chemokine receptor 4 antagonist with pIC50 of 7.9. The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for anti-inflammatory therapy.
T26642 Aplaviroc hydrochloride

AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl

Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc
T10716 CCR7 Ligand 1

CCR7-Cmp2105

Others Others
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM
T10713 CCR4 antagonist 2

Calcium Channel Membrane transporter/Ion channel; Metabolism
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
T69523 BMS-681

BMS-681 is an orthosteric antagonist of chemokine receptor 2 (CCR2) that forms a ternary complex with CCR2 and its allosteric antagonist, CCR2-RA-[R]. Together, the complex inhibits chemokine binding with BVMS-681 in the orthosteric pocket and CCR2-RA-[R] in the intracellular allosteric G-protein binding site. When chemokine binding is inhibited, modulation responses implicated in several inflammatory and neurodegenerative diseases, including atherosclerosis, multiple sclerosis, asthma, neuropat...
T69081 KRH-1636

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 chem...

化合物

GSK2239633A
Cat.No: T11481
Synonym:
Target: CCR
RS 504393
Cat.No: T5384
Synonym:
Target: CCR
RS102895
Cat.No: TQ0283
Synonym:
Target: CCR
AZD2098
Cat.No: T4300
Synonym:
Target: CCR
SB297006
Cat.No: T4674
Synonym: SB 297006
Target: CCR
INCB3344
Cat.No: TQ0103
Synonym:
Target: CCR
AZD-4818
Cat.No: T30258
Synonym: CCR1 antagonist
Target: CCR
R243
Cat.No: T24700
Synonym: R 243,R-243
Target: CCR
TAK-779
Cat.No: T7499
Synonym: Takeda 779
Target: HIV Protease, CXCR, CCR
AZ084
Cat.No: T10425
Synonym:
Target: CCR
ML604086
Cat.No: T16111
Synonym:
Target: CCR
MK-0812 Succinate
Cat.No: T16091
Synonym:
Target: Others, CCR
J-113863
Cat.No: T11699
Synonym:
Target: CCR
BMS-813160
Cat.No: T4584
Synonym: BMS 813160
Target: CCR
RS102895 hydrochloride
Cat.No: T12773
Synonym: RS102895盐酸盐
Target: Others, 5-HT Receptor, CCR
PF-4136309
Cat.No: T3430
Synonym: INCB8761,PF 4136309
Target: CCR
BX471
Cat.No: T2375
Synonym: BX 471,BX-471,ZK-811752
Target: CCR
Vercirnon
Cat.No: T17225
Synonym: CCX282-B,维塞诺,GSK-1605786,Traficet-EN
Target: CCR
C-021 dihydrochloride
Cat.No: T10639
Synonym:
Target: CCR
Maraviroc
Cat.No: T6016
Synonym: Celsentri,马拉维若,UK-427857,Selzentry
Target: HIV Protease, CCR
DAPTA
Cat.No: T7624
Synonym: DAPTA(TFA),D-Ala-peptide T-amide,Adaptavir
Target: HIV Protease, CCR
Cenicriviroc
Cat.No: TQ0297
Synonym: TAK-652,TBR-652
Target: HIV Protease, CCR
CCR2 antagonist 4
Cat.No: T13114
Synonym: Teijin compound 1
Target: CCR
C-021
Cat.No: T21870
Synonym: 4-​Quinazolinamine, 2-​[1,​4'-​bipiperidin]​-​1'-​yl-​N-​cycloheptyl-​6,​7-​dimethoxy-
Target: CCR
CCR2-RA-[R]
Cat.No: T14900
Synonym: (5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮
Target: CCR
Vicriviroc maleate
Cat.No: T3435
Synonym: 维立韦罗马来酸盐,SCH-D (maleate),SCH-417690 (maleate)
Target: HIV Protease, CCR
Pirfenidone
Cat.No: T2386
Synonym: S-7701,AMR-69,S-7701,AMR69,吡非尼酮
Target: CCR, TGF-beta/Smad
Mogamulizumab
Cat.No: T76782
Synonym: KW-0761
Target: CXCR
AF-399/42018025
Cat.No: T68984
Synonym:
Target:
YM-355179
Cat.No: T29181
Synonym: YM 355179
Target:
GSK2239633
Cat.No: T69830
Synonym:
Target:
Aplaviroc hydrochloride
Cat.No: T26642
Synonym: AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl
Target:
CCR7 Ligand 1
Cat.No: T10716
Synonym: CCR7-Cmp2105
Target: Others
CCR4 antagonist 2
Cat.No: T10713
Synonym:
Target: Calcium Channel
BMS-681
Cat.No: T69523
Synonym:
Target:
KRH-1636
Cat.No: T69081
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6413 Bindarit

宾达利,AF2838

CCR Immunology/Inflammation; Microbiology/Virology
Bindarit (AF2838) 是单核细胞趋化蛋白MCP-1/CCL2,MCP-3/CCL7和MCP-2/CCL8的选择性抑制剂,具有抗炎作用。
TN1273 7,4'-Dihydroxyflavone

4',7-Dihydroxyflavone,7,4'-二羟基黄酮

NF-κB; COX; HDAC; CCR; NOD Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB
7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) 是从甘草中分离的类黄酮,是 eotaxin/CCL11抑制剂,抑制嗜酸性粒细胞趋化因子产生。它通过调节 NF-κB、STAT6 和 HDAC2,抑制 MUC5A 基因表达和粘液产生。

天然产物

Bindarit
Cat.No: T6413
Synonym: 宾达利,AF2838
Target: CCR
7,4'-Dihydroxyflavone
Cat.No: TN1273
Synonym: 4',7-Dihydroxyflavone,7,4'-二羟基黄酮
Target: NF-κB, COX, HDAC, CCR, NOD
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