Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[1][2][3].
Cergutuzumab amunaleukin (CEA-IL2v) is a monomeric carcinoembryonic antigen (CEA)-targeted IL-2 variant-based immunocytokine. Cergutuzumab amunaleukin has immunostimulating and antineoplastic activities[1].
N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier[1][2][3][4].
ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access[1][2].
SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, is a Salt-inducible kinases (SIKs) inhibitor. SIKs regulates the transformation of M1/M2 macrophages, involving in inflammation process. SIKs-IN-1 inhibits SIK activity, up-regulates anti-inflammatory cytokine IL-10, but down-regulates pro-inflammatory cytokine IL-12. SIKs-IN-1 shows excellent anti-inflammatory effects in a DSS-induced colitis model[1].
Promethazine Hcl(NSC-231688) is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium[1].
IL-4-inhibitor-1 (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 µM[1].
RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
STING agonist-28 (CF510) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
Palmitoylglycine, a novel endogenous lipid, acts as a modulator of calcium influx and nitric oxide production in sensory neurons. Palmitoylglycine induces transient influx of calcium followed by nitric oxide production via calcium-sensitive nitric-oxide synthase enzymes. Palmitoylglycine potently inhibits heat-evoked firing of nociceptive neurons in rat dorsal horn[1].
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions[1][2].
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity[1].
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research[1].
PD-1/PD-L1-IN-25 (compound D2) is an inhibitor of PD-1/PD-L1 interaction with an IC50 value of 16.17 nM. PD-1/PD-L1-IN-25 activates the antitumor immunity of T cells efficiently in PBMCs. PD-1/PD-L1-IN-25 can be used for the research of cancer[1].
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory[1][2].
ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6[1][2][3].
PF-3893787 hydrochloride is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research[1].
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
Hydroxyzine-d8 Dihydrochloride is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation[1].
S-MTC is a selective type I nitric oxide synthase (NOS) inhibitor.
Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission[1].
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms[1]. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
Vopikitug is an IgG1-kappa, anti-IL2RA (interleukin 2 receptor alpha subunit, IL-2RA, TAC, p55, CD25) homo sapiens monoclonal antibody. Vopikitug shows antineoplastic activity[1].
IX 207-887 is a novel antiarthritic agent which inhibits the release of interleukin-1 (IL-1).
Histamine diphosphate is a potent agonist of histamine receptors and vasodilator. It can activate nitric oxide synthetase.
Cetirizine Impurity C dihydrochloride is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
Rafutrombopag diolamine is the derivative of Rafutrombopag. Rafutrombopag is a thrombopoietin receptor agonist[1].