nk 1

NK-1 Antagonist 1 is a NK-1 receptor antagonist.

NK1 Receptor Antagonist 2, a compound targeting the NK1 receptor, holds potential for tinnitus and hearing loss research.

NK3R-IN-1 (compound 16x), an orally active imidazolepiperazine derivative, functions as a Neurokinin Receptor NK3R inhibitor and has been demonstrated to reduce blood luteinizing hormone concentrations in an ovariectomy (OVX) model [1].

Cefazolin sodium (cephazolin sodium) salt binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cefazolin sodium salt is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

Cefazolin is a semi-synthetic cephalosporin that has a broad spectrum of antibacterial activity and inhibits the synthesis of bacterial cell walls.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

[Sar9]-Substance P acetate is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.

Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.

NKP608 is a selective and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50: 2.6 nM) and in vivo.

Lanepitant (LY303870) is a nonpeptide neurokinin-1 (NK-1) antagonist with analgesic activity that inhibits neurogenic dura mater inflammation and is used for the prevention of migraine.

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

Euphoheliosnoid A (Compound 24), a diterpenoid, significantly enhances natural killer (NK) cell-mediated cytotoxicity against H1299-luci cells and A549-luci cells at a concentration of 2.5 μM [1].

Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

YM44781 is a non-peptide tachykinin receptor antagonist. YM44781 exhibits high binding affinities at NK(1) (pK(i) = 9.09 +/- 0.02) and NK(2) (pK(i) = 9.94 +/- 0.03) receptors, respectively.

Biotin-Neurokinin A, a biotinylated form of Neurokinin A (Substance K), functions as a peptide neurotransmitter within the tachykinin family, primarily engaging the NK-2 receptor. It serves as a significant mediator in the physiological processes of human airway and gastrointestinal tissues [1].

Acasunlimab (GEN1046), a bispecific antibody (bsAb) designed to target PD-L1 and 4-1BB, functions by enhancing both T-cell and NK-cell response via conditional 4-1BB stimulation and continuously inhibiting the PD-1/PD-L1 axis. This compound is applicable in cancer research [1] [2].

[Sar9]-Substance P is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

Lorukafusp alfa (14.18 mAb; hu14.18-IL2) is an immunocytokine composed of a humanized 14.18 anti-GD2 monoclonal antibody (mAb) linked to interleukin-2 (IL2). It exerts anti-tumor effects [1] by inducing antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity, targeting GD2-expressing tumor cells, and stimulating NK and T cells via IL2 receptors.

[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), a Neurokinin A analogue, is a selective and potent NK2 receptor (NK2R) agonist with prokinetic activity, making it valuable for researching smooth muscle contractions across various tissues through NK-2 receptor engagement [1][2][3].

Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist [1].

Euphoscopin C, a diterpenoid isolated from Euphorbia helioscopia, significantly enhances the cytotoxic activity of natural killer (NK) cells against H1299-luci and A549-luci cells [1].

Fingolimod-d4 HCl is a deuterated compound of Fingolimod HCl. Fingolimod HCl has a CAS number of 162359-56-0. Fingolimod, a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Pitavastatin-d4 Sodium Salt is a deuterated compound of Pitavastatin Sodium Salt. Pitavastatin Sodium Salt has a CAS number of 574705-92-3. Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC 50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects [1] [2] [3] [8].

ODN D-SL03, a class C CpG oligonucleotide, effectively stimulates peripheral blood mononuclear cells (PBMCs) to produce high levels of IFN-α. It activates human B cells, NK cells, and mononuclear cells, elevating the expression of CD80, CD86, and HLA-DR on PBMC subsets' surface. Additionally, ODN D-SL03 impedes tumor growth. Its sequence: 5'-tcgcgaacgttcgccgcgttcgaacgcgg-3' [1].

GR 94800 TFA is a potent, selective antagonist of the NK 2 receptor peptide, demonstrating pK B values of 9.6 for NK 2, 6.4 for NK 1, and 6.0 for NK 3 receptors, respectively [1] [2].

[MePhe7]-Neurokinin B is a neurokinin NK-3 receptor (NK3R) agonist, exhibiting a potent agonistic activity with an IC50 value of 3 nM. It acts as a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion through the activation of NK3R [1].

Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen

Neurokinin A TFA (Substance K TFA), a peptide neurotransmitter of the tachykinin family, functions via the NK-2 receptor and acts as a key mediator in human airway and gastrointestinal tissues [1].

Substance P (5-11), the C-terminal heptapeptide derived from Substance P, functions as a neuropeptide that specifically interacts with the NK-1 tachykinin receptor [1].

[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with inhibitory affinities (K_i values) of 1 μM for NK-1, 1.3 μM for NK-2, and approximately 9 μM for NK-3 receptors [1].

[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK 1 receptor selective agonist.

MDL-105212A HCl is a nonpeptide NK-1 and NK-2 receptor antagonist.

Inbakicept (ALT-803) is an IL-15 superagonist complex, consisting of IL-15 mutant and IL-15Rα-Fc fusion. Inbakicept magnifies anti-CD20 mAb-mediated NK-cell responses and antibody-dependent cellular cytotoxicity (ADCC). Inbakicept also increases degranulation, IFNγ production in cells [1] .

Tuparstobart (Incagn-02385) is an IgG1κ monoclonal antibody targeting the immune checkpoint receptor protein LAG-3, predominantly expressed on activated T cells, NK cells, B cells, and plasmacytoid dendritic cells [1].

GR 83074 is a potent and selective antagonist of the NK-2 (Neurokinin Receptor) with a 340-fold selectivity over NK-1 and a pK_B value of 8.23. It does not act as an antagonist for NK-3, affirming its specificity [1].

Substance P(1-4) acts as a potent antagonist of neurokinin receptors (NK-R) and regulates normal hematopoiesis, additionally inhibiting the formation of endogenous erythroid colonies (EEC) [1].

Vestipitant mesylate is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

Serlopitant is a selective antagonist of Neurokinin-1 (NK-1) receptor.

SCH 206272 is a potent, orally active antagonist of tachykinin NK(1), NK(2), and NK(3) receptor.

1. (20R)-Protopanaxadiol ((20R)-Protopanaxdiol) has the effect of anti-tumor through increasing the activity of body immunity, inhibiting tumor interstitial microvascular density and its proliferation activity, improving the lymphocyte transformation, the activity of NK cells and the contents of IL-2 significantly. 2. (20R)-Protopanaxadiol prevents and heals obesity, fatty liver and hypertriglyceridemia in mice fed with a high-fat diet.

HPK1-IN-22 (compound ZYF0033) is a haematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of less than 10 nM for MBP protein-based phosphorylation inhibition. HPK1-IN-22 reduces phosphorylation of SLP76 (serine 376) and promotes anti-cancer immune responses. HPK1-IN-22 inhibits tumor growth and increases intra-tumor infiltration of DCs, NK cells and CD107a+CD8+ T cells, but decreases infiltration of T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells and LAG3+CD8+ T cells in a 4T-1 homozygous mouse model.

Dargistotug (M-6223) is a fully human IgG1 monoclonal antibody that targets TIGIT (T cell immune receptor with Ig domain and ITIM), an inhibitory immune checkpoint that depletes NK cells and reduces cytokine secretion via interaction with CD155. It also modulates effector T cell activity and enhances regulatory T cell (Tregs) function, contributing to immunosuppression [1].

[Pro9]-Substance P is a highly effective, reversible, and selective NK-1 tachykinin receptor agonist with an EC50 value of 0.93 nM [1].

(D-Arg1, D-Pro2, D-Phe7, D-His9)-Substance P is a selective NK1 receptor antagonist [1].

Nemvaleukin alfa (ALKS 4230), an IL-2 fusion protein, selectively targets intermediate-affinity IL-2R to activate NK and effector T cells, and is used in cancer research [1] [2] [3].

YM49598 is a tachykinin receptor antagonist. YM49598 exhibited high binding affinities at NK(1) (pK(i) = 9.09 +/- 0.02) and NK(2) (pK(i) = 9.94 +/- 0.03) receptors, respectively. YM49598 was almost inactive but produced a potent inhibition (IC(50) = 11 +/