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) | ||
|---|---|---|---|---|
| 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 |
| S0777 | 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 |
| 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 |
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 |
|---|---|---|---|
| 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. |
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 MalateVicriviroc 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. |
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新 |
R243R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
||
| S3205新 |
PerillaldehydePerillaldehyde (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. |
||
| S0777 |
APX-115 free baseAPX-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. |
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.
|
|
| 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. |
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. |
|
| S7538新 |
RS-102895 HydrochlorideRS-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-813160BMS-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 |
AZD2098AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8. |
||
| S0129 |
SB-297006SB-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. |
||
| S8324 |
ZK756326 2HClZK756326 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. |
| 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. |
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 MalateVicriviroc 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. |
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新 |
R243R243 is an inhibitor of Chemokine (C-C motif) receptor 8 (CCR8) signaling and chemotaxis. |
||
| S3205新 |
PerillaldehydePerillaldehyde (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. |
||
| S0777 |
APX-115 free baseAPX-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. |
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.
|
|
| 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. |
2021, 10.1038/s41422-021-00528-3 2021, 23(1):11 2021, 35(4):e21402 |
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. |
| S7538新 |
RS-102895 HydrochlorideRS-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-813160BMS-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 |
AZD2098AZD2098 is a potent and bioavailable CCR4 receptor antagonist with pIC50 of 7.8. |
||
| S0129 |
SB-297006SB-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. |
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 2HClZK756326 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. |
2019, 216(12):2763-2777 |
