23 Results for "

opioid ligands

" in MedChemExpress (MCE) Product Catalog:
Products (23)

23 Results for "opioid ligands" in MCE Product Catalog:

1
1 Cited Publications
Cat. No.: HY-120511
CAS No.: 1256921-89-7
Purity:  99.60%
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (Ki = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-104006
CAS No.: 1069498-96-9
Purity:  99.12%
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
loading...
    loading...
Cat. No.: HY-P2159
CAS No.: 75790-53-3
Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .
loading...
    loading...
Cat. No.: HY-101231
CAS No.: 121264-04-8
Purity:  98.68%
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
loading...
    loading...
Cat. No.: HY-P1793
CAS No.: 83471-50-5
α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer .
loading...
    loading...
Cat. No.: HY-W048697
CAS No.: 201532-01-6
Research Areas:  

Others

Fmoc-D-Pen(Trt)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize analogs of cyclic lanthionine enkephalin, a δ-opioid receptor selective ligand .
loading...
    loading...
Cat. No.: HY-W013154
CAS No.: 136030-33-6
Research Areas:  

Others

Fmoc-Tic-OH, an Fmoc-protected derivative of Tic, is a solid-phase peptide synthesis monomer. Fmoc-Tic-OH protects the amino group of Tic via a base-labile Fmoc group, allowing conformationally constrained Tic residues to be stepwise coupled to peptide chains, and the Fmoc protecting group can be removed under piperidine conditions. Fmoc-Tic-OH can be used for peptide synthesis and opioid receptor ligand research .
loading...
    loading...
Cat. No.: HY-178235
CAS No.: 873573-64-9
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .
loading...
    loading...
Cat. No.: HY-W856819
CAS No.: 469-22-7
Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease .
loading...
    loading...
Cat. No.: HY-144606
CAS No.: 2767446-03-5
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
loading...
    loading...
Cat. No.: HY-W019787
CAS No.: 75513-71-2
Target:  

Opioid Receptor CXCR

Research Areas:  

Neurological Disease

BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
loading...
    loading...
Cat. No.: HY-P3839
CAS No.: 207392-60-7
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
loading...
    loading...
Cat. No.: HY-P5070
CAS No.: 142155-24-6
Gluten Exorphin A5 is an orally active δ-opioid receptor ligand. Gluten Exorphin A5 exhibits opioid agonist biological activity, analgesic activity, stress-induced analgesia regulatory effects, memory-promoting effects, and non-cytotoxicity. Gluten Exorphin A5 modulates intestinal permeability, can cross in vitro human intestinal epithelial cells via paracellular transport, and resists brush border peptidase hydrolysis. Gluten Exorphin A5 can be used in the research of stress-related processes and cognitive processes .
loading...
    loading...
Cat. No.: HY-P1793A
α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer .
loading...
    loading...
Cat. No.: HY-P11642A
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
loading...
    loading...
Cat. No.: HY-174307
CAS No.: 687634-09-9
Target:  

Dopamine Receptor

Research Areas:  

Neurological Disease

Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction) .
loading...
    loading...
Cat. No.: HY-126063
CAS No.: 125190-72-9
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

ICI-204448 free acid is a κ-opioid agonist with limited access to the CNS, ICI-204448 free acid can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
loading...
    loading...
Cat. No.: HY-124907
CAS No.: 328-04-1
Synonyms: OMS-403
Target:  

PPAR

Research Areas:  

Neurological Disease

AI 3-25755 (OMS-403) is a peroxisome proliferator-activated receptor gamma (PPARγ) agonist. AI 3-25755 can be used for research on opioid abuse and smoking cessation .
loading...
    loading...
Cat. No.: HY-179365
CAS No.: 63463-07-0
Synonyms: β-NTA dihydrochloride
Target:  

Drug Intermediate

Research Areas:  

Others

β-Naltrexamine (β-NTA) dihydrochloride is a key synthetic intermediate used in the preparation of irreversible ligands for opioid receptors .
loading...
    loading...
Cat. No.: HY-104006R
CAS No.: 1069498-96-9
Research Areas:  

Neurological Disease

CYM51010 (Standard) is the analytical standard of CYM51010 (HY-104006). This product is intended for research and analytical applications. CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
loading...
    loading...