BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
Thunalbene is a stilbene derivative isolated from Thunia alba. Thunalbene has a weak inhibitory effect on nitric oxide production and is not cytotoxic[1].
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Limonene is a monoterpene in citrus peel oil. A popular disinfectant and food preservative. Antimicrobial activities[1]. Anti-proliferative activities[2]. Antioxidant and anti-inflammatory effect[3].
Alintegimod (7HP349) is a potent and orally active integrin activator. Alintegimod can serve as a systemically administered adjuvant to enhance T cell-mediated immune responses to vaccines[1].
Asobamast is a potent, orally active antiallergic agent that inhibits ige mediated passive pulmonary allergic responses in rats (ED50=4.7 mg/kg) and inhibits antigen-induced mediator release from sensitized guinea pig lung fragments[1].
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
Oxyphenbutazone is a phenylbutazone derivative, with anti-inflammatory effect. Oxyphenbutazone is a non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis[1][2].
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Glycerol-2-13C is the 13C labeled Glycerol. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[1][2][3][4].
CDN-A is a cyclic di-nucleotide, it can be used to synthesis antibody-drug conjugate (ADC). Cyclic di-nucleotides are potent stimulators of innate and adaptive immune responses. In humans, cyclic di-nucleotide, which are either produced endogenously in response to foreign DNA or by invading bacterial pathogens, trigger the innate immune system by activating the expression of interferon genes[1][2][3].
α,β-Methylene ATP, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7[1][2].
AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury[1][2][3].
Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity[1][2].
Methyl nicotinate, the methyl ester of Niacin found in alcoholic beverages, that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain[1].
TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain[1].
SLC26A3-IN-3 (compound 4az) is a SLC26A3 inhibitor (IC50: 40 nM). SLC26A3-IN-3 can be used for research of constipation, cystic fibrosis[1].
12-OxoETE induces a rapid, dose dependent increase of cytoplasmic free calcium via leukotriene B4 receptor or a common activation sequence[1][2].
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders[1].
Mulberrofuran H is a 2-arylbenzofuran derivative from the cultivated mulberry tree (Morus lhou (ser.) Koidz.). Mulberrofuran H demonstrates potent inhibition against substrates L-tyrosine (IC50=4.45 µM) and L-DOPA (IC50=19.70 µM). Mulberrofuran H also shows potent anti-inflammatory and antioxidative activities[1][2][3].
αvβ6 integrin inhibitor 2 is a potent ανβ6 integrin inhibitor with an IC50 of 96.5 nM (WO2020081154A1, example 19)[1].
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
Lysophosphatidylcholines are a class of chemical compounds which are derived from phosphatidylcholines. Lysophosphatidylcholine is produced from phospholipids by the action of phospholipase A2 (PLA2). Lysophosphatidylcholine plays critical role in allergic airway disease manifestation[1].
GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].
Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
DMT1 blocker 2, Compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 of 0.83 μM, is expected to block iron uptake by enterocytes in vivo[1].