Catalog No.
Product Name
Application
Product Information
Citations
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P2X1 Receptor Antagonist
NF449 octasodium is a potent antagonist of the P2X1 receptor, exhibiting IC50 values of 0.28 nM, 0.69 nM, and 120 nM for recombinant P2X1, recombinant P2X1 with 5, and P2X2+3 receptors, respectively. It selectively targets the Gsα subunit of G proteins, effectively inhibiting GTP[γS] binding to Gsα-s and reducing adenylyl cyclase activity. NF449 octasodium is useful in research focused on the regulation of P2X1 receptor-mediated signaling pathways and β-adrenergic receptor interactions. -
Somatostatin
Tyr-Somatostatin-28 is a potent somatostatin analog featuring a tyrosine residue at the N-terminus. This modification enhances its stability and bioactivity, making it an important tool for studying somatostatin receptor interactions and signaling pathways. Tyr-Somatostatin-28 has applications in neurobiology and endocrinology research, particularly in the investigation of hormone regulation and therapeutic targets for diseases such as acromegaly and neuroendocrine tumors. -
Potassium Channel Blocker
Besipirdine hydrochloride is a potassium channel blocker that exerts both cholinergic and adrenergic effects. Its cholinergic activity is characterized by stimulation of phosphatidylinositol turnover and a reduction in potassium currents, while its adrenergic activity promotes norepinephrine release through the inhibition of presynaptic α2-adrenergic receptors and the blocking of norepinephrine reuptake. This compound is applicable in research related to Alzheimer's disease, providing insights into potential therapeutic pathways. -
Neurokinin-1 Receptor Antagonist
TAK-637 is an orally active antagonist of the neurokinin-1 receptor, known for its role in modulating neuronal signaling pathways. This compound has been shown to enhance bladder storage capacity and may provide insights into the treatment of functional bowel diseases, including irritable bowel syndrome. TAK-637 serves as a valuable tool for researchers investigating the therapeutic potential of neurokinin-1 receptor modulation in urological and gastrointestinal disorders. -
NK1 Receptor Antagonist
TKA-731 is an NK1 receptor antagonist that effectively modulates nociceptive signaling. It has demonstrated the ability to reverse mechanical hyperalgesia and exhibit analgesic properties in neuropathic pain models, particularly in guinea pigs. This compound is valuable for research applications focused on understanding and targeting neuropathic pain mechanisms. -
NK3 Receptor Antagonist
SSR 146977 is a selective antagonist of the tachykinin NK3 receptor. It demonstrates potent inhibition of neurokinin B binding to NK3 receptors in Chinese hamster ovary cells, with a Ki value of 0.26 nM. This compound is valuable in research focused on neurokinin signaling pathways and their implications in physiological and pathological conditions. -
NK1 Receptor Antagonist
Rolapitant hydrochloride is a potent and selective neurokinin 1 (NK1) receptor antagonist, demonstrating a Ki value of 0.66 nM. This compound is distinguished by its long-acting and orally active properties. In pharmacological studies, rolapitant hydrochloride exhibits significant anti-emetic activity, as evidenced by its effectiveness in a ferret emesis model. Its unique mechanism makes it a valuable tool for research on emesis and nausea pathways. -
NK1R Fragment
Neurokinin Receptor (393-407), rat, is a fragment of the rat neurokinin 1 receptor (NK1R), which is known for its role in mediating cellular responses to substance P through rapid internalization and subsequent recycling to the plasma membrane. This reagent is essential for investigating neurogenic inflammation and offers insights into the pathways associated with NK1R signaling. It serves as a valuable tool for researchers studying receptor dynamics and neuroinflammatory mechanisms. -
NK1 Receptor Antagonist
L-703606 oxalate is a selective antagonist of the NK1 receptor, effectively inhibiting its activity. This compound plays a significant role in the study of gastric acid secretion, providing insights into neurokinin signaling pathways. Its potent inhibitory effects make it a valuable tool for research in gastrointestinal physiology and related disorders. -
NK1 Antagonist
CP 122721 hydrochloride is a potent, selective non-peptide antagonist of the neurokinin NK1 receptor, exhibiting a pIC50 of 9.8 in human NK1 receptor assays using IM-9 cells. This compound demonstrates significant anxiolytic and antidepressant-like properties, making it a valuable tool for research in anxiety and mood disorder studies. It is suitable for investigating the role of NK1 receptors in neuropsychiatric conditions. -
Neurokinin Receptor
Dapitant is a non-peptide antagonist targeting the neurokinin-1 (NK1) receptor, demonstrating high affinity for the human receptor. By inhibiting the binding of Substance P to NK1 receptors, Dapitant effectively blocks neurokinin-mediated biological effects. This compound serves as a potential therapeutic candidate for various conditions associated with Substance P, including neurogenic inflammation and pain modulation, making it valuable for research in pain management and inflammatory disorders. -
NK1 Antagonist
FK888 is a highly selective dipeptide antagonist of the neurokinin-1 (NK1) receptor. It demonstrates a potent ability to displace [3H]-substance P binding, with a Ki value of 0.69 nM, making it an effective tool for studying NK1-related pathways. FK888 has been shown to inhibit substance P-induced airway edema in guinea pigs following both intravenous and oral administration, offering valuable insights for research in respiratory and inflammatory conditions. -
Substance P Analog
[Glp5,Sar9] Substance P (5-11) is an analog of the neuropeptide Substance P, specifically designed to interact with the neurokinin-1 (NK1) receptor. This compound demonstrates potent biological activity by modulating pain perception and inflammatory responses, making it valuable in research focused on neurobiology and pain management. Its unique structure allows for the exploration of receptor binding and activity, facilitating the development of therapeutic agents targeting NK1 receptors. -
Neurokinin-1 Receptor Antagonist
SLV-317 free base is a potent antagonist of the neurokinin-1 receptor, demonstrating oral bioactivity. It effectively inhibits substance P-induced effects, making it valuable for research into neurogenic inflammation and pain pathways. This compound is suitable for studies focused on the modulation of neurokinin signaling and its implications in various neurological disorders. -
NK2R Agonist
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) is a selective agonist for the NK2 receptor (NK2R), exhibiting a potent EC50 of 3.7 nM for human NK2R. This compound has demonstrated significant biological activity by inhibiting weight loss in diet-induced obese mouse models and ameliorating Loperamide-induced voiding dysfunction in wild-type mice. It serves as a valuable tool for research into neurokinin receptor-mediated disorders, including obesity, insulin resistance, and type 2 diabetes. -
Active Compound
(R)-Casopitant, an NK(1)-receptor antagonist, serves as an active compound for research applications targeting chemotherapy-induced nausea and vomiting. As the isomer of Casopitant, (R)-GW679769 offers potential insights into the modulation of neurokinin signaling pathways. This compound is instrumental in evaluating therapeutic strategies for alleviating chemotherapy-related side effects. -
Substance P Analog
Substance P, Free Acid is a native analog of substance P that offers structural similarity without the associated biological activity. This compound can be utilized in research focused on neuropeptide signaling pathways and the role of substance P in various physiological processes. Its unique properties make it suitable for studies investigating receptor interactions and neurogenic inflammation. -
NK1 Inhibitor
SR140333B is a selective inhibitor of the neurokinin-1 (NK1) receptor, primarily involved in modulating pain and inflammatory responses. This compound demonstrates significant efficacy in reducing LPS-induced fever and attenuating LPS-induced alterations in brain tissue in rat models. SR140333B is valuable for research focusing on neuroinflammation, pain pathways, and the therapeutic potential of NK1 receptor modulation. -
Neurokinin Receptor Antagonist
Benzomalvin A is a potent antagonist of neurokinin receptors, derived from Penicillium sp. This compound demonstrates significant inhibitory activity against substance P, exhibiting Ki values of 12, 42, and 43 μM at guinea pig, rat, and human neurokinin NK1 receptors, respectively. Benzomalvin A is instrumental in research focused on neurokinin signaling pathways and its implications in various physiological and pathological processes. -
SP1-7 Ligand
Leucyl-phenylalanine amide is a dipeptide analog that serves as a specific ligand for the SP1-7 receptor, exhibiting a binding affinity characterized by a Ki value of 10.2 nM. This compound is valuable for research focused on neuropeptide signaling pathways and can be utilized in studies exploring the functional roles of SP1-7 in various physiological contexts. Notably, it does not show binding activity to human NK-1 or NK-3 receptors, making it a selective tool for targeted biological investigations. -
NK1 Receptor Antagonist
Maropitant citrate hydrate is an orally active antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant antiemetic properties, making it effective in preventing vomiting. Additionally, Maropitant has been reported to inhibit ulcerative dermatitis, highlighting its utility in various research applications related to gastrointestinal and inflammatory conditions. -
Analog of Substance P
[MePhe8,Sar9] Substance P is an analog of the neuropeptide Substance P, functioning as a neurotransmitter and neuromodulator in the central nervous system (CNS). This compound exhibits biological activity relevant to pain modulation and neuroinflammation. It is utilized in research applications focused on the roles of neuropeptides in various physiological and pathological processes, including nociception and stress responses. -
NK1/NK2 Receptor Antagonist
S 16474 is a cyclic peptide that functions as an antagonist of NK1 and NK2 receptors. This compound demonstrates significant activity in modulating neurogenic inflammation. S 16474 is suitable for research applications focusing on pain pathways and inflammatory responses mediated by neurokinins. -
Substance P Fragment
Substance P (2-11) is a peptide fragment of Substance P that primarily targets neurokinin receptors. It exhibits contractile activity in guinea pig ileum, indicating its potential role in gastrointestinal motility. Additionally, Substance P (2-11) has been shown to inhibit the permeation of tritiated Substance P across blood-brain barrier endothelial cell monolayers, making it relevant for research in neurobiology and drug delivery. -
NK3 Receptor Antagonist
GSK256471 is a non-peptide antagonist targeting the tachykinin NK3 receptor, exhibiting a pKi of 8.9 for the human recombinant receptor and 8.4 for the guinea pig native receptor. This compound demonstrates over 100-fold selectivity against NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 irreversibly inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and has been shown to mitigate wet dog shaking behavior and suppress dopamine release. This compound serves as a valuable tool for studying the pathophysiology of schizophrenia. -
Analog of Substance P
Substance P-Gly-Lys-Arg is an analog of Substance P designed to interact with neurokinin receptors. This peptide exhibits key biological activity in modulating pain perception and inflammatory responses, making it a valuable tool for studying neuropeptide signaling pathways. Research applications include investigating the role of Substance P in pain management and exploring therapeutic avenues for neuroinflammatory conditions. -
NK1 Receptor Antagonist
(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant biological activity by inhibiting NK1 receptor-mediated signaling pathways, which play a crucial role in pain perception, inflammation, and neurogenic responses. This compound is valuable for research in neurobiology, cancer therapy, and the development of analgesics targeting the NK1 receptor. -
NK-3 Antagonist
PD-161182 is a non-peptide antagonist targeting the neurokinin-3 (NK-3) receptor. It exhibits potential activity in modulating NK-3 receptor-related pathways, making it a valuable tool for studying various central nervous system disturbances, as well as pain, inflammation, and diseases affecting the pulmonary and skin systems. This compound is essential for researchers exploring the therapeutic implications of NK-3 antagonism in these contexts. -
NK1 Receptor Antagonist
ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. This compound demonstrates antitumor activity, particularly in breast cancer cells that exhibit high expression of the NK1 receptor. ASN-1377642 may facilitate research into targeted cancer therapies and the role of neurokinin signaling in tumor progression. -
Neurokinin Receptor Antagonist
L-659877 is a neurokinin receptor antagonist that serves as a valuable tool for investigating peptide fragmentation and structural properties. This compound facilitates the study of collision-induced dissociation mechanisms, allowing researchers to analyze the structural changes of beta-fragment ions across varying lengths. Its application is essential for advancing understanding in neuropharmacology and peptide-based therapeutics. -
Neurokinin Receptor Inhibitor
SCH 60057 is a potent neurokinin receptor inhibitor, selectively targeting NK1 and NK2 receptors with IC50 values of 6 μM and 12 μM, respectively. This compound is derived from Acremonium sp. and is useful in research applications related to pain modulation, inflammation, and neurogenic disorders. Its ability to inhibit neurokinin signaling pathways makes it a valuable tool for investigating the roles of these receptors in various biological processes. -
Substance P Antagonist
FR 113680 is a tripeptide antagonist that selectively targets the NK1 neurokinin receptor, inhibiting the action of substance P. This compound displays significant biological activity in modulating pain and inflammatory responses. It is widely utilized in research exploring the role of neurokinin pathways in various neurological and psychiatric disorders. -
Neurokinin B Antagonist
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B, primarily targeting the Neurokinin Receptor, with a pA2 value of 5.5. This compound selectively inhibits Neurokinin B activity without affecting Substance P or Neurokinin A, making it valuable for studies of neuromodulation and neuropeptide signaling. Its ability to modulate neurokinin pathways is relevant for research in neurobiology and potential therapeutic applications related to pain and inflammatory responses. -
Substance P Fragment
Substance P (3-11) is a truncated form of the neuropeptide Substance P that effectively crosses the blood-brain barrier. This fragment exhibits potent contracting activity on guinea pig ileum and stimulates chemotaxis in human monocytes. It is utilized in research focused on neuroinflammation, pain pathways, and immune response modulation. -
NK-1 Agonist
[Pro9]-Substance P is a highly selective and reversible agonist of the NK-1 tachykinin receptors, demonstrating an EC50 of 0.93 nM. This compound plays a significant role in modulating neurokinin signaling pathways and is instrumental in research focused on pain management, neuroinflammation, and various neurological disorders. Its precise activity profile makes it an invaluable tool for studying the therapeutic potential of NK-1 receptor modulation. -
Substance P (6-11) Analogue
[Glp6] Substance P (6-11) is a potent analogue of substance P (6-11) that primarily targets tachykinin receptors. This compound is known to stimulate the formation of [3H]-inositol monophosphate ([3H]-IP1) in rat urinary bladder tissues. It serves as a valuable tool in research focused on neuropeptide signaling, pain pathways, and bladder function. -
NK1 Receptor Antagonist
Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist that effectively inhibits the action of substance P at the NK1 receptor. This compound demonstrates key biological activity in modulating neurogenic inflammation and pain pathways. It is predominantly used in research applications involving pain management, gastrointestinal disorders, and anxiety models, making it a valuable tool for studying the neurokinin system and its therapeutic potential. -
NTSR1 Anagonist
Zalsenertant tetraxetan is a DOTA-conjugated antagonist of the neurohypophyseal hormone receptor subtype 1 (NTSR1). Labeled with the radioactive isotope Lu-177 (177Lu), it serves as a valuable tool for molecular imaging to identify potential responders. This compound is particularly relevant in radiotherapy research for solid tumors, facilitating the exploration of targeted therapeutic strategies. -
Neurokinin Receptor
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor, demonstrating a 46% inhibition of substance P binding at a concentration of 100 μg/mL in vitro. Additionally, it exhibits weak inhibitory activity against indoleamine 2,3-dioxygenase (IDO), with an IC50 value of 130 μM for recombinant IDO. Isolated from Penicillium, Benzomalvin C features a distinct epoxide group at C-19 and C-20, which differentiates it from other benzomalvins such as A, B, and E. This compound may prove valuable in neurobiology and cancer research applications due to its modulation of neurokinin signaling and IDO activity. -
NK1 Receptor Antagoinst
CGP-49823 is a selective antagonist of the neurokinin 1 receptor (NK1 receptor) with oral bioavailability. It exhibits potent anti-anxiety effects, demonstrated in social interaction assays in rats, and shows a slow development of tolerance without eliciting anxiety-like withdrawal symptoms upon cessation. This compound is applicable in research focused on anxiety and depression. -
NK1/NK2 Receptor Antagonist
DNK-333 is a potent dual antagonist of the NK1 and NK2 receptors, exhibiting IC50 values of 4.8 nM and 5.5 nM, respectively. This compound effectively inhibits Neurokinin A (NKA)-induced bronchoconstriction, making it a valuable tool for research on respiratory conditions such as asthma. Its balanced activity at both receptor sites allows for exploring therapeutic strategies targeting neurokinin signaling pathways. -
NK1 Receptor Antagonist
Vestipitant mesylate is a selective NK1 receptor antagonist that effectively crosses the blood-brain barrier. With a high affinity for the human NK1 receptor (pKi: 9.65), this compound is instrumental in studying various neuropsychiatric conditions, including depression and anxiety disorders, as well as in investigating its effects on nausea and vomiting. Its oral bioavailability further facilitates its use in in vivo research applications. -
NK2 Receptor Antagonist
GR 87389 is a potent antagonist of the NK2 receptor, effectively inhibiting its activity. This compound has been shown to competitively block GA 64349-induced contractions in smooth muscle strips derived from human detrusor, prostate, and prostatic urethra tissues. GR 87389 is valuable in research applications focused on the role of NK2 receptors in smooth muscle physiology and potential therapeutic strategies for related disorders. -
NK-1 Receptor Antagonist
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies. -
NK2 Receptor Antagonist
Bz-Dab(NBD)-AwFpP-Nle-NH2 is a specific antagonist of the NK2 receptor, exhibiting potent activity with a pKi of 8.87 nM. This fluorescent compound, with excitation at 340 nm and emission at 505 nm, is valuable for studies investigating NK2 receptor-related signaling pathways and their roles in various biological processes. Its applications include receptor characterization and evaluation of receptor function in physiological and pathological contexts. -
NK2 Receptor Antagonist
L-659837 is a selective antagonist of the neurokinin-2 (NK2) receptor, effectively inhibiting GR 64349-induced contraction. This compound serves as a valuable tool in the investigation of urinary bladder disorders, allowing researchers to explore its therapeutic potential in conditions like overactive bladder and related urinary dysfunctions. -
Substance P Release Inhibitor
Dilopetine citrate is a potent inhibitor of substance P release, demonstrating significant activity in attenuating the vocalizations of isolated guinea pig pups in a dose-dependent manner. Its mechanisms suggest potential applications in the field of psychiatry, particularly as an antidepressant agent. This compound may facilitate research on the modulation of neuropeptide systems involved in mood regulation and pain perception. -
SP1-7 Ligand
Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) functions as a potent ligand for the substance P 1–7 (SP1-7) binding site, exhibiting a Ki value of 1.5 nM. This compound demonstrates significant anti-allodynic and anti-hyperalgesic properties in animal models of neuropathic pain when administered centrally. However, it shows no distinct effects when delivered peripherally via intraperitoneal injection. Phenylalanylphenylalanylamide is valuable for investigations into pain-related disorders and therapeutic interventions. -
NK1R Antagonist
Telmapitant is an orally active antagonist of the neurokinin-1 receptor (NK1R). This compound exhibits antiemetic properties, making it valuable for studying delayed onset emesis. It is utilized in research to investigate the mechanisms and treatment options related to nausea and vomiting. -
Tachykinin ReceptoR Antagonist
YM-44778 is a selective antagonist of tachykinin receptors, specifically blocking NK1, NK2, and NK3 receptors with pKi values of 8.08, 8.55, and 8.24, respectively. This compound demonstrates significant inhibition of bladder pressure elevation induced by the neuropeptide substance [Sar9,Met(O2)11]-P in anesthetized rat models. Its pharmacological profile makes YM-44778 valuable for research in bladder function and disorders related to tachykinin signaling.
