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)
DMSO アルコール
A2040 Leronlimab (anti-CCR5) 146.7 KD mg/mL 0.2 μM filtered mg/mL
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
E0486 C-021 <1 mg/mL 94 mg/mL 23 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
S8361 PF-4136309 <1 mg/mL 100 mg/mL ''100 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
P1137 Thymulin 100 mg/mL <1 mg/mL <1 mg/mL

亜型選択性的な製品

CCR製品

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
A2040

Leronlimab (anti-CCR5)

Leronlimab (anti-CCR5)(PRO 140; Vyrologix) is a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy. It is being investigated as a potential therapy in the treatment of HIV infection.

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.

S2004

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.

S3479

R243

R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.

S7604

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.

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.

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.

S8220

INCB3344

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

E0395

Vercirnon

Vercirnon (GSK1605786A, CCX-282, Traficet-EN), an orally bioavailable, selective, and potent antagonist of CCR9, is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9.

E0486

C-021

C-021 is a potent CCR4 antagonist with IC50 values are 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.

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.

S8361

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.

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.

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.

P1137

Thymulin

Thymulin (FTS) is a neuroendocrine hormone with immunoregulatory actions, with anti-inflammatory potential by downregulating the release of inflammatory mediators, such as cytokines and chemokines, upregulating anti-inflammatory factors, such as interleukin (IL)-10, exerting molecular control via the regulation of transcription factors and mediators.

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
A2040

Leronlimab (anti-CCR5)

Leronlimab (anti-CCR5)(PRO 140; Vyrologix) is a humanized monoclonal antibody to CCR5, blocks breast cancer cellular metastasis and enhances cell death induced by DNA damaging chemotherapy. It is being investigated as a potential therapy in the treatment of HIV infection.

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.

S2004

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.

S3479

R243

R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis.

S7604

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.

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.

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.

2022, 41(1):81

2022, 289:115051

2022, 45(1):34-41

S8220

INCB3344

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

E0395

Vercirnon

Vercirnon (GSK1605786A, CCX-282, Traficet-EN), an orally bioavailable, selective, and potent antagonist of CCR9, is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9.

E0486

C-021

C-021 is a potent CCR4 antagonist with IC50 values are 0.14 μM and 39 nM for inhibition of chemotaxis in human and mouse respectively.

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.

2022, 13(5):478

S8361

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.

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.

2022, 13(5):478

2021, 118(9)e2017282118

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.

2022, 10.1007/s00262-022-03196-3

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
P1137

Thymulin

Thymulin (FTS) is a neuroendocrine hormone with immunoregulatory actions, with anti-inflammatory potential by downregulating the release of inflammatory mediators, such as cytokines and chemokines, upregulating anti-inflammatory factors, such as interleukin (IL)-10, exerting molecular control via the regulation of transcription factors and mediators.

Tags: CCR inhibitor|CCR agonist|CCR activator|CCR inducer|CCR antagonist|CCR signaling pathway|CCR assay kit