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) represents a highly specialized humanized agonistic monoclonal antibody specifically engineered to target the invariant T-cell receptor of iNKT cells with exceptional binding affinity and selectivity, effectively facilitating the measurable activation and expansion of this unique lymphocyte subset across various preclinical experimental models to evaluate the induction of immunomodulatory cytokines during strictly monitored laboratory observation periods.

NKTT120 is a humanized monoclonal antibody that targets iNKT cells. It shows potential for research in sickle cell disease (SCD).

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.

Inbakicept is a dimer of IL-15 receptor alpha sushi domain and immunoglobulin G1 (human Fc fragment) fusion protein, which is an IL-15 super agonist protein complex. Inbakicept binds to IL-15 antibody Nogapendekin alfa to form the complex Nogapendekin alfa inbakicept (ALT-803) in a 1:2 ratio. ALT-803 has potential anticancer and anti-tumor activities, which can be used to study breast cancer.

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

Bempegaldesleukin (NKTR-214) is a PEGylated interleukin-2 (IL-2) that functions as an immunostimulatory IL-2 proagent, acting as a CD122-preferential agonist of the IL-2 pathway. It can stimulate an antitumor immune response [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.