nk1

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

Lanepitant 2HCl is a non-peptide neurokinin-1 receptor antagonist with analgesic and anti-inflammatory activity.Lanepitant 2HCl inhibits the binding of Substance P to the neurokinin-1 receptor, inhibits neurogenic inflammation and pain transmission, and can be used in the study of painful neuropathic disorders, such as migraines.

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

(R)-CJ 11974: non-peptide NK1 receptor antagonist, may relieve pain and prevent chemo-induced vomiting.

Ezlopitant (CJ-11974) is a small molecule neurokinin-1-receptor (NK1) antagonist used to treat nausea, vomiting and pain.

Substance P (Neurokinin P) (SP) is an undecapeptide (a peptide composed of a chain of 11 amino acid residues) member of the tachykinin neuropeptide family.

Neurokinin B acetate(86933-75-7 free base) is the acetate form of Neurokinin B, which belongs to the tachykinin family. Neurokinin binds to neurokinin receptor 1 (NK1R), nk2r and NK3R, and mediates its biological effects.

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

MNK1 2-IN-7 (compound 20j) serves as an orally administered inhibitor targeting MNK1 2, known for its anticancer properties and hERG safety. It also blocks the phosphorylation of eIF4E, thereby disrupting the MNK eIF4E signaling pathway and reducing cancer cell growth. Additionally, MNK1 2-IN-7 synergizes effectively with Ibrutinib. [15] [1]

Anti-Mouse NK1.1 Antibody (PK136) is an IgG2a class antibody of murine origin targeting NK1.1, which eliminates NK1.1 and NK1.1NKT cells and inhibits NK1.1 signaling in peripheral blood, spleen, and lung tissues, and can be used in the study of heart and lung failure.

MNK1 2-IN-8 (compound 15b) serves as an inhibitor of MNK1 2, exhibiting potent IC 50 values of 0.8 nM for Mnk1 and 1.5 nM for Mnk2. Additionally, this compound demonstrates anti-proliferative effects and induces cell cycle arrest.

MNK1 2-IN-5 is a potent and selective MNK1 2 inhibitor with anticancer activity and can be used to study solid tumors and hematological malignancies.

WNK1-IN-1, a selective inhibitor of WNK1, exhibits an IC50 value of 1.6 μM and also inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM, indicating its potential utility in the research of blood pressure regulation and cancer.

PROTAC JNK1-targeted-1 (PA2) is a JNK1 PROTAC degrader with a DC50 of 10 nM. It effectively reduces fibronectin levels and is useful in lung fibrosis research. [Pink: JNK1 inhibitor; Black: linker; Blue: CRBN Ligand]

MNK1 2-IN-6 is a potent and selective inhibitor of MNK1 (IC50: 2.3 nM) and MNK2 (IC50: 3.4 nM) that induces apoptosis in a concentration-dependent manner.

Befetupitant (Ro67-5930) is a potent and selective tachykinin 1 receptor (NK1R) antagonist for the study of corneal neovascularization.

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

MEN11467 is a novel, orally available, potent and selective peptidomimetic tachykinin NK 1 receptor antagonist for the study of acute colon cancer.

WIN 51,708 is a neurokinin receptor (NK1) antagonist.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

N-Acetyl-L-tryptophan (N-acetyltryptophan) is an inhibitor of neurokinin 1 receptor (NK1-receptor, NK1R).

Aprepitant is a Substance P Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

Maropitant is a selective neurokinin (NK1) receptor antagonist.