Neurokinin Receptor NK receptor There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues. www.MedChemExpress.com 1 Neurokinin Receptor Inhibitors & Modulators Aprepitant Befetupitant (MK-0869; MK-869; L-754030) Cat. No.: HY-10052 (Ro67-5930) Cat. No.: HY-19670 Bioactivity: Aprepitant (MK-0869) is a selective and high-affinity Bioactivity: Befetupitant is a high-affinity, nonpeptide, competitive neurokinin 1 receptor antagonist with a Kd of 86 pM. tachykinin 1 receptor ( NK1R) antagonist. Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg Fezolinetant Fosaprepitant (ESN-364) Cat. No.: HY-19632 (L-758298) Cat. No.: HY-14407 Bioactivity: Fezolinetant is an antagonist of the neurokinin 3 receptor Bioactivity: Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist (NK3R), used for the treatment of menopausal hot flushes. for the prevention of chemotherapy-induced nausea and vomiting. Purity: 98.29% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Fosaprepitant dimeglumine GR 159897 (MK-0517; L785298) Cat. No.: HY-14407A Cat. No.: HY-107691 Bioactivity: Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor Bioactivity: GR 159897 is a highly potent, selective, competitive, antagonist for the prevention of chemotherapy-induced nausea brain-penetrated non-peptide antagonist at tachykinin NK2 and vomiting. IC50 Value: Target: NK1 receptor in vitro: receptors, inhibits binding of [ 3H]GR100679 to hNK -CHO Fosaprepitant (also known as MK-0517 and L-758,298) is a 2 water-soluble phosphoryl prodrug for aprepitant, which, when… cells and rat colon membranes with pKis of 9.51 and … Purity: 99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: Hemokinin 1 mouse Ibodutant Cat. No.: HY-P1030 (MEN 15596) Cat. No.: HY-14770 Bioactivity: Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 Bioactivity: Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor antagonist with a pKi of 10.1. receptor and human NK2 receptor, respectively. Purity: 98.41% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 250 mg, 500 mg Kassinin Maropitant Cat. No.: HY-P0250 Cat. No.: HY-10053 Bioactivity: Kassinin is a peptide derived from the Kassina frog. It Bioactivity: Maropitant is a neurokinin (NK1) receptor antagonist. IC50 belongs to tachykinin family of neuropeptides. It is secreted value: Target: NK1 receptor Maropitant is the first NK1 as a defense response, and is involved in neuropeptide receptor antagonist developed to treat and prevent emesis in signalling. dogs. Treatment with 1 mg/kg Maropitant citrate, significantly reduced the size of ulcerative dermatitis (UD) lesions in… Purity: >98% Purity: 99.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Men 10376 Men 10376 TFA (Neurokinin-2 receptor antagonist) Cat. No.: HY-P1276 (Neurokinin-2 receptor antagonist (TFA)) Cat. No.: HY-P1276A Bioactivity: Men 10376 is a selective tachykinin NK-2 receptor antagonist, Bioactivity: Men 10376 TFA is a selective tachykinin NK-2 receptor with a Ki of 4.4 μM for rat small intestine NK-2 receptor. antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor [1]. Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg MEN11467 Monohydroxy Netupitant D6 Cat. No.: HY-U00207 Cat. No.: HY-G0012S Bioactivity: MEN11467 is a selective and orally- effective peptidomimetic Bioactivity: Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy tachykinin NK1 receptor antagonist. Netupitant, which is a metabolite of Netupitant. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg Netupitant Netupitant D6 (CID 6451149) Cat. No.: HY-16346 (CID-6451149 D6) Cat. No.: HY-16346S Bioactivity: Netupitant (CID-6451149) is a highly potent and selective, Bioactivity: Netupitant D6 is the deuterium labeled orally active neurokinin-1 receptor antagonist with Ki of 0.95 Netupitant(CID-6451149), which is a highly potent and nM. IC50 value: 0.95 nM (Ki) [1] Target: NK1 receptor in selective, orally active neurokinin-1 receptor antagonist. vitro: Netupitant also dose-dependently inhibited the SP response as expected from an NK1 receptor antagonist.… Purity: 99.78% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg Netupitant metabolite Monohydroxy Netupitant Neurokinin A (Monohydroxy Netupitant) Cat. No.: HY-G0012 (α-Neurokinin; Neuromedin L; Substance K) Cat. No.: HY-P0197 Bioactivity: Monohydroxy Netupitant is the metabolite of Netupitant, which Bioactivity: Neurokinin A acts via neurokinin 2 ( NK-2) receptor. is a highly selective NK1 receptor antagonist. Purity: >98% Purity: 98.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 25 mg Neurokinin A(4-10) Neurokinin A(4-10) TFA Cat. No.: HY-P0236 Cat. No.: HY-P0236A Bioactivity: Neurokinin A (4-10) is a tachykinin NK2 receptor agonist. Bioactivity: Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist [1]. Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg, 25 mg www.MedChemExpress.com 3 Neurokinin antagonist 1 Neurokinin B Cat. No.: HY-U00320 Cat. No.: HY-P0242 Bioactivity: Neurokinin antagonist 1 is a Neurokinin antagonist Bioactivity: Neurokinin B belongs to the tachykinin family of peptides. extracted from patent WO1998045262A1. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 25 mg Neurokinin B TFA NK-1 Antagonist 1 Cat. No.: HY-P0242A Cat. No.: HY-106659 Bioactivity: Neurokinin B TFA belongs to the tachykinin family of peptides. Bioactivity: NK-1 Antagonist 1 is an antagonist of NK-1 receptor, used in Neurokinin B binds a family of GPCRs-including neurokinin the research of NK-1 related diseases and conditions such as receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological cough, overactive bladder, alcohol dependency and depression. effect [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 25 mg NKP608 Pavinetant Cat. No.: HY-18006 (MLE-4901; AZD2624; AZD4901) Cat. No.: HY-14432 Bioactivity: NKP608 is a non-peptidic derivative of 4-aminopiperidine which Bioactivity: Pavinetant (MLE-4901) is a neurokinin-3 receptor ( NK3R) acts as a selective, specific and potent antagonist at the antagonist. neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. Purity: 99.34% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Physalaemin Rolapitant Cat. No.: HY-P0255 (SCH619734) Cat. No.: HY-14751 Bioactivity: Physalaemin, a non-mammalian tachykinin, binds selectively to Bioactivity: Rolapitant (SCH619734) is a potent, selective and orally neurokinin-1 ( NK1) receptor with high affinity. active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM. Purity: >98% Purity: 98.01% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Saredutant SB-222200 (SR 48968; SR 48968C) Cat. No.: HY-106910 Cat. No.: HY-15722 Bioactivity: Saredutant is a selective NK2 receptor antagonist. Bioactivity: SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Scyliorhinin II Senktide Cat.