A-940894 is a potent histamine H4 receptor antagonist, with Ki values of 7.6 nM (rat H4) and 71 nM (human H4). A-940894 exhibits with anti-inflammatory properties[1].
Tripelennamine Hcl, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.IC50 Value:Target: Histamine H1 receptorTripelennamine can be used in the treatment of asthma, hay fever, rhinitus and urticaria.in vitro: Arterial and mixed venous blood-gas and pH measurements were made at rest before and after saline or drug administration and during incremental exercise leading to maximal exertion at 14 m/s on 3.5% uphill grade for 120 s. Galloping at this workload elicited maximal heart rate and induced exercise-induced pulmonary hemorrhage in all horses in both treatments, thereby indicating that capillary stress failure-related pulmonary injury had occurred [1].in vivo: The data obtained (median and range in brackets) in camels and horses, respectively, were as follows: the terminal elimination half-lives were 2.39 (1.91-6.54) and 2.08 (1.31-5.65) h, total body clearances were 0.97 (0.82-1.42) and 0.84 (0.64-1.17)L/h/kg. The volumes of distribution at steady state were 2.87 (1.59-6.67) and 1.69 (1.18-3.50) L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model were 1.75 (0.68-2.27) and 1.06 (0.91-2.20) L/kg [2]. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively [3].
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia[1].
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects[1][2][3].
CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM[1].
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly[1].
Alcaftadine-D3 (R89674-D3) is a deuterium labeled Alcaftadine. Alcaftadine (HY-17039) is a H1 histamine receptor antagonist[1].
TLR8 agonist 5 is a potent TLR8 agonist with an EC50 value of 20 nM for HEK-Blue hTLR8. TLR8 agonist 5 activates the immune response[1].
Met-RANTES (human) is a partial antagonist of CCR5. Met-RANTES (human) reduces the infiltration of blood monocytes into the liver[1].
(S)-ZLc002 is a S-enantiomer of ZLc-002. ZLc-002 is a selective inhibitor of nNOS-Capon coupling. ZLc-002 suppresses inflammatory nociception and chemotherapy-induced neuropathic pain[1].
Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.IC50 value:Target: DHODH inhibitorin vitro: 4SC-101 is a potent inhibitor of human DHODH, inhibits lymphocyte proliferation, and uniquely blocks phytohemagglutinin-stimulated IL-17 production by lymphocytes [2].in vivo: In vivo Vido treatment alone most effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells. In contrast, similarly reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels were observed from animals treated with Vido alone and Vido + Uri. Vido improves TNBS-induced colonic inflammation by a unique dual mode of action [1]. Oral administration of 4SC-101 effectively improved both chronic DSS and acute TNBS colitis in mice. In these colitis models the overall efficacy profile of 4SC-101 was similar to that of dexamethasone [2].
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists 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 are 40 nM and 70 nM, respectively[1].
Resatorvid (TAK-242) is a potent TLR4 signaling inhibitor which selectively inhibits the TLR4-mediated production of cytokines and nitric oxide.
IL-1β-IN-1, cannabidiol derivative, is a potent IL-1β inhibitor. IL-1β-IN-1 has anti-inflammatory and pain-resolving properties[1].
Erepdekinra is an interleukin-17A (IL-17A) receptor antagonist[1].
NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively[1].
Lokivetmab (Anti-Canine IL31 Recombinant Antibody) is an anti-canine IL-31 monoclonal antibody that can be used for the research of atopic dermatitis (AD) in dogs[1].
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties[1][2]. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca2+, and markedly decreases iNOS protein expression[3].
Ppc-1 is a mitochondrial uncoupler. Ppc-1 enhances mitochondrial oxygen consumption without adverse effects on ATP production. Ppc-1 is a cell-permeate interleukin-2 (IL-2) inhibitor. Ppc-1 inhibits the Gram-negative periodontopathogen Porphyromonas gingivalis. Ppc-1 has anti-obesity, antibacterial and anti-inflammatory activities[1][2][3][4].
DB0614 (Example 21) is a bifunctional compound targeted protein degradation of kinases. DB0614 degrades AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
Withangulatin A is a selective cyclooxygenase-2 (COX-2) inhibitor. Withangulatin A can be isolated from Physalis angulata L. Withangulatin A has anti-tumor, trypanocidal activity and anti-inflammatory function[1].
AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma[1].
Longiferone B is a daucane sesquiterpene, that can be isolated from Boesenbergia longiflora rhizomes. Longiferone B shows anti-inflammatory activity against NO release with an IC50 of 21.0 μM. Longiferone B also suppresses the iNOS and COX-2 mRNA expression[1].
C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation[1].
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively[1][2]. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats[2].
Zeluvalimab (AMG-404) is a monoclonal antibody targeting the PD-1 receptor that can be used for the research of cancer[1].
IFN-γ Antagonist 1 (AYCRDGKIGPPKLDIRKEEKQI) is an antagonist of interferon γ (IFN γ). IFN-γ Antagonist 1 inhibits IFN-γ induced HLR/DR antigen expression in Colon 205 cells with an IC50 value of approximately 35 μM. IFN-γ Antagonist 1 has potential applications in immune regulation[1].
BKT140 4-fluorobenzoyl is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM. Sequence: 4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2(Disulfide bridge: Cys4-Cys13).