nkt

human tachykinin NK1 receptor antagonist

α-Galactosylceramide (KRN7000) is a synthetic glycolipid with antitumorial and immunostimulatory and is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide and CD1d can bind to the T cell antigen receptor of NKT cells.

Gusperimus trihydrochloride is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.

Senktide TFA is a potent and selective neurokinin 3 (NK3) receptor agonist with an EC50 of 0.5-3 nM, while showing significantly weaker activity on NK1 receptors (EC50=35 µM). It is a promising candidate for research in neurological disorders.

Naloxegol (NKTR-118; AZ-13337019) is an opioid receptor antagonist[1].

Senktide is an agonist of tachykinin NK3 receptor.

Senktide acetate (Senktide acetate(106128-89-6 free base)) is a selective tachykinin NK3 receptor agonist that promotes the consolidation or expression of ELM for the study of Alzheimer's disease.

Anti-TCR Antibody (NKTT320) is a CHO-expressed humanized antibody that targets TCR. It features a huIgG4 heavy chain and a huκ light chain, with an estimated molecular weight (MW) of 150 kDa. For its isotype control, refer to HumanIgG4kappa, Isotype Control.

A2G2S2-KVANKTglycopeptide is a multifunctional fluorescent linker, classified as a polyglycan N-glycoprotein. The resulting conjugates exhibit high sensitivity and specificity by mimicking the antennae components of N-glycans.

GPEP FA2-KVANKT glycopeptide (F(3)A2 glycan-KVANKT & F(6)A2 glycan-KVANKT) is a type of N-glycoprotein that serves as a multifunctional fluorescent linker. The resulting conjugates demonstrate high sensitivity and specificity by simulating the antenna elements of N-glycans.

Naloxegol oxalate (NKTR-118) is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.

Vadaclidine is an orally acting antinociceptive muscarinic agonist.

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

Dendrotoxin K TFA, a Kv1.1 channel blocker, modulates glutamate release in CA3 neurons by time-dependently regulating the presynaptic spike waveform [1].

GCS-12-6 is a potent Th2-selective NKT cell agonist that targets the CD1d protein. It holds potential for research in autoimmune diseases, such as inflammatory bowel disease and multiple sclerosis.

α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide. [1] It increases IL-2 secretion by DN32.D3 NKT hybridoma cells when co-cultured with CD1d-transfected RBL cells pre-loaded with α-GalCer analog 8 at a concentration of 32 ng/ml. α-GalCer analog 8 (32 ng/ml) induces IL-4 secretion to a greater extent than the synthetic α-GalCer KRN 7000 in mouse splenocytes in vitro and in mouse serum following administration of a 1 µg per animal dose, indicating a Th2 response.

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection.

ABX196 is an NKT agonist and an analog of the parental compound -GalCer [1].

GCS-12, a Th1/2-balanced sulfonamide glycolipid, enhances its interaction with CD1d. It acts as an agonist for Natural Killer T cells (NKT cells), inducing the secretion of cytokines IFN-γ and IL-4. In mice, it has demonstrated immunoregulatory and antitumor activities.

GCS-11 is an effective activator of natural killer T (NKT) cells. It specifically promotes the production of IFN-γ and IL-4, with a particular selectivity for IFN-γ. As a compound, GCS-11 exhibits anticancer activity and holds potential as a promising adjuvant in cancer immunotherapy or vaccine development.

Nanrilkefusp alfa (SO-C101; SOT101), a fusion protein, serves as a powerful and selective agonist of the IL-15 and IL-15Rα sushi + domain. It promotes the proliferation and activation of memory CD8 + T cells, natural killer (NK) cells, γ/δ T cells, and NKT cells to inhibit tumor growth. Nanrilkefusp alfa demonstrates remarkable anti-metastatic effects in melanoma and effectively suppresses tumor progression in various mouse tumor models [1] [2].