chemotaxis

C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.

ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 binding to CCR8 on circulating T-cells.

Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki: 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophi

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

BMS-986235 (LAR-1219) is a selective and orally active agonist of formyl peptide receptor 2 (FPR2) with EC50s of 0.41 nM for hFPR2 and 3.4 nM for mFPR2. BMS-986235 can be used in studies on the prevention of heart failure.

Andrograpanin (19-HYDROXY-8(17),13-LABDADIEN-16,15-OLIDE) is a bioactive compound from Andrographis paniculata. Andrograpanin has anti-inflammatory and anti-infectious properties.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

BMS-817399 is an orally active antagonist of CCR1 with IC50s of binding affinity and chemotaxis inhibition potencies and can be used in studies about rheumatoid arthritis.

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

Olsalazine disodium (Dipentum) is bioconverted to 5-aminosalicylic acid (5-ASA) in the colon and has anti-inflammatory activity in ulcerative colitis.

Qingyangshengenin B (Otophylloside B) is a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic and anti-aging effects, it can extend lifespan, increase heat stress-resistance, delay body paralysis, and increase the chemotaxis response in C. elegans models of Alzheimer's disease. Otophylloside B can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist 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 at 40 nM and 70 nM, respectively.

LMD-009 is a non-peptide, selective CCR8 agonist that mediates chemotaxis, inositol phosphate accumulation, and calcium release, with an EC50 of 11–87 nM.

BMS CCR2 22 is a potent and selective antagonist of CCR2 with calcium flux IC50 of 18 nM, chemotaxis IC50 of 1 nM, and binding IC50 of 5.1 nM.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.