CCR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2907	Pirfenidone (S-7701)	<1 mg/mL	37 mg/mL	'37 mg/mL
S2004	Vicriviroc Malate	38 mg/mL	134 mg/mL	'134 mg/mL
S3479	R243	<1 mg/mL	71 mg/mL	'''35 mg/mL
S7604	BX471	<1 mg/mL	87 mg/mL	22 mg/mL
S0777	Isuzinaxib (APX-115 free base)	<1 mg/mL	56 mg/mL	56 mg/mL
S3032	Bindarit (AF 2838)	<1 mg/mL	64 mg/mL	64 mg/mL
S8512	Cenicriviroc (TAK-652)	<1 mg/mL	100 mg/mL	'''100 mg/mL
S2003	Maraviroc (UK-427857)	<1 mg/mL	100 mg/mL	'''100 mg/mL
S8361	PF-4136309	<1 mg/mL	100 mg/mL	''100 mg/mL
S3383	RS102895	<1 mg/mL	85 mg/mL	'''25 mg/mL
S7538	RS-102895 Hydrochloride	<1 mg/mL	85 mg/mL	'''85 mg/mL
S0085	BMS-813160	<1 mg/mL	97 mg/mL	97 mg/mL
S6555	AZD2098	<1 mg/mL	67 mg/mL	5 mg/mL
S0129	SB-297006	<1 mg/mL	68 mg/mL	20 mg/mL
S8501	Adaptavir (DAPTA)	100 mg/mL	-1 mg/mL	-1 mg/mL
S8324	ZK756326 2HCl	78 mg/mL	39 mg/mL	4 mg/mL

亜型選択性的な製品

CCR製品

All (17) CCR阻害剤(8) CCR拮抗剤(8) CCR作動薬(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2907	Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Front Cell Dev Biol, 2021, 9:648201 Front Pharmacol, 2021, 12:631891 Biochem Biophys Res Commun, 2021, 553:172-179	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.
S2004^新	Vicriviroc Malate Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.	Nature, 2013, 493(7430):51-5 Cancer Res, 2012, 72(15):3839-50 J Antimicrob Chemot, 2011, 66(4):802-12	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.
S3479	R243 R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.
S7604^新	BX471 BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.
S0777	Isuzinaxib (APX-115 free base) APX-115 free base (Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
S3032	Bindarit (AF 2838) Bindarit (AF 2838) exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.	Hum Cell, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4 Cancer Cell Int, 2020, 19;20:58	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.
S3205	Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
S8512	Cenicriviroc (TAK-652) Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.	Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0
S2003	Maraviroc (UK-427857) Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.	Cell Res, 2021, 10.1038/s41422-021-00528-3 Nat Commun, 2021, 12(1):4474 J Exp Med, 2021, 218(11)e20200792	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.
S8361^新	PF-4136309 PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
S3383	RS102895 RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
S7538	RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S0085	BMS-813160 BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion.
S6555	AZD2098 AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8.
S0129	SB-297006 SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM.
S8501	Adaptavir (DAPTA) Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.	Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118 FEBS J, 2020, 287(11):2367-2385
S8324	ZK756326 2HCl ZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.	J Exp Med, 2019, 216(12):2763-2777

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2907	Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Front Cell Dev Biol, 2021, 9:648201 Front Pharmacol, 2021, 12:631891 Biochem Biophys Res Commun, 2021, 553:172-179	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.
S2004^新	Vicriviroc Malate Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.	Nature, 2013, 493(7430):51-5 Cancer Res, 2012, 72(15):3839-50 J Antimicrob Chemot, 2011, 66(4):802-12	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.
S3479	R243 R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.
S7604^新	BX471 BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.
S0777	Isuzinaxib (APX-115 free base) APX-115 free base (Ewha-18278 free base) is a potent, orally active inhibitor of pan NADPH oxidase (pan-Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base (Ewha-18278 free base) significantly suppresses the expression of inflammatory molecules including MCP-1/CCL2, IL-6, and TNFα in the diabetic kidney.
S3032	Bindarit (AF 2838) Bindarit (AF 2838) exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.	Hum Cell, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4 Cancer Cell Int, 2020, 19;20:58	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.
S3205	Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
S8512	Cenicriviroc (TAK-652) Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.	Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00191-0

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2003	Maraviroc (UK-427857) Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.	Cell Res, 2021, 10.1038/s41422-021-00528-3 Nat Commun, 2021, 12(1):4474 J Exp Med, 2021, 218(11)e20200792	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.
S8361^新	PF-4136309 PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
S3383	RS102895 RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
S7538	RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S0085	BMS-813160 BMS-813160 is a potent, well-absorbed dual CCR2 and CCR5 chemokine antagonist. BMS-813160 inhibits inflammatory processes, angiogenesis, tumor cell migration, tumor cell proliferation and invasion.
S6555	AZD2098 AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8.
S0129	SB-297006 SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. SB-297006 suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM.
S8501	Adaptavir (DAPTA) Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.	Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118 FEBS J, 2020, 287(11):2367-2385

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S8324	ZK756326 2HCl ZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.	J Exp Med, 2019, 216(12):2763-2777

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S8324

ZK756326 2HCl

ZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.

J Exp Med, 2019, 216(12):2763-2777

研究分野別

製品類型

CCR

シグナル伝達経路

研究分野

阻害剤の選択性比較

亜型選択性的な製品

CCR製品