ccr1 antagonist j 113863  (MedChemExpress)

Journal: Frontiers in Molecular Biosciences

Article Title: Multitargeted biological actions of polydatin in preventing pseudogout acute attack

doi: 10.3389/fmolb.2025.1553912

Figure Lengend Snippet: Effect of IL-1β signal inhibition on PD treatment. Monocytes were pretreated with PD (100 µM) for 2 h and then stimulated for 24 h with CPP (0.025 mg/mL). Where indicated, anakinra (anak, 0.1 µg/mL) was added 30 min before the PD treatment. (A) IL-1β, (B) IL-18, (C) IL-6, (D) TNFα, (E) IL-8, (F) CCL-23 and (G) VEGF levels in supernatants were quantified by ELISA. Data are expressed as mean of four independent experiments ±SD. p calculated according to the One Way Anova, Bonferroni’s multiple comparisons test: *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001. p calculated according to t-test, PD + CPP vs anak + PD + CPP: °p < 0.05, °°p < 0.01. CPP, calcium pyrophosphate crystals; PD, polydatin; anak, anakinra.

Article Snippet: Where indicated, polydatin (100 µM) was added 2 h before the stimulation with crystals and anakinra (0.1 µg/mL), J113863 (Medchemexpress, Monmouth Junction, USA, 10 µM) and EX527 (Selleckchem, Cologne, 10 µM) were added 30 min before the use of polydatin.

Techniques: Inhibition, Enzyme-linked Immunosorbent Assay

Journal: Frontiers in Molecular Biosciences

Article Title: Multitargeted biological actions of polydatin in preventing pseudogout acute attack

doi: 10.3389/fmolb.2025.1553912

Figure Lengend Snippet: Effect of CCR1 inhibition on PD treatment. Monocytes were pretreated with PD (100 µM) for 2 h and then stimulated for 24 h with CPP (0.025 mg/mL). Where indicated, J113863 (10 µM) was added 30 min before the PD treatment. (A) IL-1β, (B) IL-18, (C) IL-6, (D) TNFα, (E) IL-8, (F) VEGF levels in supernatants were quantified by ELISA. Data are expressed as mean of four independent experiments ±SD. p calculated according to the One Way Anova, Bonferroni’s multiple comparisons test:*p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001. p calculated according to t-test, PD + CPP vs J + PD + CPP: °°p < 0.01. CPP, calcium pyrophosphate crystals; PD, polydatin.

Article Snippet: Where indicated, polydatin (100 µM) was added 2 h before the stimulation with crystals and anakinra (0.1 µg/mL), J113863 (Medchemexpress, Monmouth Junction, USA, 10 µM) and EX527 (Selleckchem, Cologne, 10 µM) were added 30 min before the use of polydatin.

Techniques: Inhibition, Enzyme-linked Immunosorbent Assay

Journal: Frontiers in Molecular Biosciences

Article Title: Multitargeted biological actions of polydatin in preventing pseudogout acute attack

doi: 10.3389/fmolb.2025.1553912

Figure Lengend Snippet: Migration of PBMCs exposed to SFs from patients with CPP induced arthritis in the presence or absence of PD (100–200 µM) or J113866 (10 µM) for 1.30 h. Medium RMPI supplemented with 5% plasma was used as a positive control (C+), while medium RPMI supplemented with 1% FBS was used as a negative control (C-). Left panel : Representative image of migrated cells on the bottom of a filter membrane of a modified 48-well Boyden chamber. Right panel : Effect of 100–200 μM PD on PBMCs migration induced by (A) 5% plasma (n = 3) (B) inflammatory SFs from CIA patients (n = 4). (C) Effect of 10 μM J113863 on PBMCs migration induced by inflammatory SFs from CIA patients (n = 4). Cell migration is shown as optical density values (O.D). Each sample was tested in sextuplicate. Data are expressed as mean of three to four independent experiments ±SD. p calculated according to the One Way Anova, Bonferroni’s multiple comparisons test: *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001. CPP, calcium pyrophosphate crystals; PD, polydatin; SF, synovial fluid; PBMCs, peripheral blood mononuclear cells.

Article Snippet: Where indicated, polydatin (100 µM) was added 2 h before the stimulation with crystals and anakinra (0.1 µg/mL), J113863 (Medchemexpress, Monmouth Junction, USA, 10 µM) and EX527 (Selleckchem, Cologne, 10 µM) were added 30 min before the use of polydatin.

Techniques: Migration, Positive Control, Negative Control, Membrane, Modification

Journal: Brain sciences

Article Title: Pharmacological Modulation of the MIP-1 Family and Their Receptors Reduces Neuropathic Pain Symptoms and Influences Morphine Analgesia: Evidence from a Mouse Model.

doi: 10.3390/brainsci13040579

Figure Lengend Snippet: Figure 6. The effects of a CCR1 antagonist (J113863) administered intrathecally (i.t.) according to timeline (A), at doses of 1, 15, 30, and 60 µg/5 µL on mechanical (B) and thermal (C) hypersensitivity and the influence of J113863 at a dose of 15 µg/5 µL plus morphine 2.5 µg/5 µL on mechanical (E) and thermal (F) hypersensitivity, administered according to timeline (D), 7 days after CCI in mice. The data are presented as the mean ± SEM (naive n = 5; CCI n = 5–8). The results were evaluated using one-way ANOVA followed by Bonferroni’s post hoc test for comparisons of selected pairs. * p < 0.05, ** p < 0.01, and *** p < 0.001 indicate significant differences vs. V-treated group at each of the investigated time points: 1, 4, and 24 h for (B,C) graphs; * p < 0.05 and *** p < 0.001 indicate significant differences vs. V + W-treated group for (E,F) graphs; ## p < 0.01 indicates significant differences between the V + M- and J11 + M-treated groups for (E,F) graphs; and & p < 0.05 indicates significant differences between the J11 + W- and J11 + M-treated groups. Abbreviations: V: vehicle (DMSO); W: vehicle (aqua pro injectione); M: morphine, J11: J113863; CCI: chronic constriction injury of the sciatic nerve.

Article Snippet: Administration of CCR1 and CCR5 Antagonists A single i.t. administration of J113863 (CCR1 antagonist, at doses of 1, 15, 30, and 60 μg/5; μL cat. #2595, Tocris, Bristol, UK), TAK-220 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5; μL cat. #HY-19974/CS-5579, MedChemExpress, Monmouth Junction, NJ, USA), or AZD-5672 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5 μL cat. #HY119101/CS-0068004, MedChemExpress) were administered once to CCI-exposed mice on Day 7, when mechanical and thermal hypersensitivity were fully developed.

Techniques:

Journal: Brain sciences

Article Title: Pharmacological Modulation of the MIP-1 Family and Their Receptors Reduces Neuropathic Pain Symptoms and Influences Morphine Analgesia: Evidence from a Mouse Model.

doi: 10.3390/brainsci13040579

Figure Lengend Snippet: Figure 9. Comparison of the effects of intrathecal (i.t.) administration of substances targeting CCR1 (J113863), CCR5 (TAK-220 or AZD-5672), and their combination (J11 + TAK-220 or J11 + AZD-5672) at a dose of 15 µg/5 µL (timeline (A)) on mechanical and thermal hypersensitivity measured after 1 h (B,C) and after 4 h (D,E), 7 days after chronic CCI in mice. The data are presented as the mean ± SEM (naive n = 5; CCI n = 7–8). The results were evaluated using one-way ANOVA followed by Bonferroni’s post hoc test for comparisons of selected pairs. • p < 0.05, •• p < 0.01, and ••• p < 0.001 indicate significant differences vs. J11-treated group; ♦p < 0.05 and ♦♦♦p < 0.001 indicate significant differences vs. TAK-treated group; ■p < 0.05 indicates significant differences vs. AZD-treated group; and ▲p < 0.05 indicates significant differences vs. J11 + TAK-treated group. Abbreviations: N: naive; V: vehicle (DMSO); J11: J113863; TAK: TAK-220; AZD: AZD -5672; CCI: chronic constriction injury of the sciatic nerve.

Article Snippet: Administration of CCR1 and CCR5 Antagonists A single i.t. administration of J113863 (CCR1 antagonist, at doses of 1, 15, 30, and 60 μg/5; μL cat. #2595, Tocris, Bristol, UK), TAK-220 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5; μL cat. #HY-19974/CS-5579, MedChemExpress, Monmouth Junction, NJ, USA), or AZD-5672 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5 μL cat. #HY119101/CS-0068004, MedChemExpress) were administered once to CCI-exposed mice on Day 7, when mechanical and thermal hypersensitivity were fully developed.

Techniques: Comparison

Journal: Brain sciences

Article Title: Pharmacological Modulation of the MIP-1 Family and Their Receptors Reduces Neuropathic Pain Symptoms and Influences Morphine Analgesia: Evidence from a Mouse Model.

doi: 10.3390/brainsci13040579

Figure Lengend Snippet: Scheme 1. Pharmacological modulation of chemokines from MIP-1 family (CCL3 and CCL9) via neutralizing antibodies and their receptors (CCR1 by J113863, CCR5 by TAK-220 or AZD -5672) reduces neuropathic pain symptoms and influences morphine analgesia—evidence from mice model evoked by chronic constriction injury of the sciatic nerve.

Article Snippet: Administration of CCR1 and CCR5 Antagonists A single i.t. administration of J113863 (CCR1 antagonist, at doses of 1, 15, 30, and 60 μg/5; μL cat. #2595, Tocris, Bristol, UK), TAK-220 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5; μL cat. #HY-19974/CS-5579, MedChemExpress, Monmouth Junction, NJ, USA), or AZD-5672 (CCR5 antagonist, at doses of 0.5, 2, 4, and 15 μg/5 μL cat. #HY119101/CS-0068004, MedChemExpress) were administered once to CCI-exposed mice on Day 7, when mechanical and thermal hypersensitivity were fully developed.

Techniques: