nk-3

DNK 333 is a dual antagonist targeting the neurokinin NK1 NK2 receptors.

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

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)

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

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

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

NK 1971 is a bioactive chemical.

Stevastelin B3 is a depsipeptide isolated from Penicillium.

D-Lysine lactam is a chiral building block.1,2It has been used in the synthesis of a chiral antibiotic synthetic intermediate, as well as in the stereoselective synthesis of neurokinin (NK) receptor antagonists. 1.Kumar, A., Bhashkar, B., Bhavsar, J., et al.Catalytic reduction: Efficient synthesis of chiral key intermediate of besifloxacin hydrochlorideDer Pharma Chemica7(9)297-3000(2015) 2.Gerspacher, M., Lewis, C., Ball, H.A., et al.Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonistJ. Med. Chem.46(16)3508-3513(2003)

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

Pitavastatin (NK-104) is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, effectively inhibiting cholesterol synthesis from acetic acid in HepG2 cells with an IC50 of 5.8 nM. It also induces hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptors and exhibits therapeutic activities such as anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective, and reno-protective effects.

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].

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

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].

[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].

[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].

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].

[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].

HCV Peptide (35-44), a core protein of Hepatitis C Virus at positions 35 to 44, functions as an HLA-A2-restricted CTL epitope and inhibits NK cell activity through the KIR2DL2 3 receptor and synergistically through the CD94:NKG2A receptor [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].

ML-T7, a powerful inhibitor of Tim-3, effectively disrupts its interactions with PtdSer and CEACAM1. This compound enhances the antitumor activity of adoptive transfer therapy involving cytotoxic T lymphocytes (CTLs) and CAR T cells, while also boosting T cell effector functions. Additionally, ML-T7 augments the killing activity of NK cells against tumor cells and improves the antigen-presenting capacity of dendritic cells (DCs). Demonstrating antitumor efficacy in preclinical models, ML-T7 shows potential either as a standalone treatment or in combination with Nivolumab for tumor immunotherapy research [1].