Search Result

Pathways Recommended:	Antibody-drug Conjugate/ADC Related

Results for "

Drug addiction

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (1) AP-1 (1) Apoptosis (3) Carboxylesterase (CES) (1) Dopamine Receptor (1) Dopamine Transporter (1) GABA Receptor (1) GPR6 (1) HIV Integrase (1) iGluR (1) Interleukin Related (1) mGluR (4) Neuropeptide Y Receptor (1) Neurotensin Receptor (1) NF-κB (1) NO Synthase (1) Opioid Receptor (2) Phosphodiesterase (PDE) (1) PPAR (1) Reference Standards (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) Trace Amine-associated Receptor (TAAR) (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Metabolic Disease (1) Neurological Disease (21)

By Targets:

5-HT Receptor (3)

Adenosine Receptor (1)

AP-1 (1)

Apoptosis (3)

Carboxylesterase (CES) (1)

Dopamine Receptor (1)

Dopamine Transporter (1)

GABA Receptor (1)

GPR6 (1)

HIV Integrase (1)

iGluR (1)

Interleukin Related (1)

mGluR (4)

Neuropeptide Y Receptor (1)

Neurotensin Receptor (1)

NF-κB (1)

NO Synthase (1)

Opioid Receptor (2)

Phosphodiesterase (PDE) (1)

PPAR (1)

Reference Standards (1)

TNF Receptor (1)

Toll-like Receptor (TLR) (1)

Trace Amine-associated Receptor (TAAR) (1)

By Research Areas:

Cancer (3)

Cardiovascular Disease (1)

Metabolic Disease (1)

Neurological Disease (21)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Drug Intermediate Drug Isomer Drug Derivative Drug Metabolite Antibody-Drug Conjugates (ADCs) Peptide-Drug Conjugates (PDCs) Radionuclide-Drug Conjugates (RDCs) Drug-Linker Conjugates for ADC ADC Linker

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111308

RTI-118	Neuropeptide Y Receptor	Neurological Disease
RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve agent addiction including selectively decrease self-administration .

HY-101478

Fenobam	mGluR Apoptosis	Neurological Disease Cancer
Fenobam is a selective and orally active mGluR5 antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the K_d values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .

HY-P2259

TAT-GluA2 3Y 2 Publications Verification	iGluR HIV Integrase Adenosine Receptor	Cardiovascular Disease Neurological Disease
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .

HY-139178

KVA-D-88	Phosphodiesterase (PDE)	Neurological Disease
KVA-D-88 is a blood-brain barrier-permeable PDE4 inhibitor with IC₅₀ values of 140 and 880 nM for PDE4B and PDE4D, respectively. KVA-D-88 induces cAMP accumulation and inhibits neuroactive substance-mediated hyperlocomotion, locomotor sensitization. KVA-D-88 can be used for the research of drug addiction .

HY-147319

RTI-7470-44	Trace Amine-associated Receptor (TAAR)	Neurological Disease
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .

HY-116910

CPP-115	GABA Receptor	Neurological Disease
CPP-115 is a GABA transaminase inactivator with higher affinity and lower retinal toxicity than Vigabatrin (HY-15399). CPP-115 increases brain GABA levels by inhibiting GABA transaminase catabolism. CPP-115 can be used in the study of drug addiction and infantile spasms .

HY-P2046

β-Endorphin (rat)	Opioid Receptor	Neurological Disease
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .

HY-158014

JJC8-089	Dopamine Transporter	Neurological Disease
JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .

HY-124446

Dibromsalicil	Carboxylesterase (CES)	Metabolic Disease
Dibromsalicil (Compound 31) is a carboxylesterase (CES) inhibitor with activity of 72.7 nM against hiCE (human intestinal carboxylesterase) and 53.5 nM against rCE (rabbit liver carboxylesterase). Dibromsalicil has almost no activity against hCE1 (human liver carboxylesterase) and cholinesterase .

HY-101478A

Fenobam hydrate	mGluR Apoptosis	Neurological Disease Cancer
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the K_d values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .

HY-174898

5-HT2C agonist-9	5-HT Receptor	Neurological Disease
5-HT2C agonist-9 (Compound 33) is a 5-HT2C agonist with an EC₅₀ of 1.4 nM for h5-HT2C. 5-HT2C agonist-9 can be used in the research of diseases such as depression, drug addiction, alcoholism, PTSD and neuropathic pain .

HY-175191

5-HT2A agonist 4	5-HT Receptor	Neurological Disease
5-HT2A agonist 4 (Compound 70) is a 5-HT2A agonist with an EC₅₀ of 0.30  nM for h5-HT2A. 5-HT2A agonist 4 can be used for depression, drug addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain research .

HY-175192

5-HT2A agonist 5	5-HT Receptor	Neurological Disease
5-HT2A agonist 5 (Compound 88) is a 5-HT2A agonist with an EC₅₀ of 0.01  nM for h5-HT2A. 5-HT2A agonist 5 can be used for depression, drug addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain research .

HY-103573

VU 0360223	mGluR	Neurological Disease
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM .

HY-12698

NNC 63-0532	Opioid Receptor	Neurological Disease
NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC₅₀s of 305 nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction .

HY-11056

PF-04363467	Dopamine Receptor	Neurological Disease
PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness .

HY-101478R

Fenobam (Standard)	Reference Standards mGluR Apoptosis	Neurological Disease Cancer
Fenobam (Standard) is the analytical standard of Fenobam. This product is intended for research and analytical applications. Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .

HY-124907

AI 3-25755 OMS-403	PPAR	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 .

HY-179594

HTS10307	AP-1	Neurological Disease
HTS10307 is a small molecule AP1 Transcription Factor ΔFOSB inhibitor. HTS10307 inhibits the binding of ΔFOSB/JUND and ΔFOSB to DNA with IC₅₀ values of ~3 μM and ~7 μM, respectively. HTS10307 can be used as a chemical probe for investigating the role of ΔFOSB in pathological conditions such as drug addiction, Alzheimer’s disease, and Parkinson’s disease .

HY-182551

SR-12062	Neurotensin Receptor	Others Neurological Disease
SR-12062 is a Neurotensin receptor 1 (NTSR1) full agonist that modulates NTSR1 to trigger intracellular Ca ²⁺ mobilization. SR-12062 can be used for the research of schizophrenia, parkinson’s disease, drug addiction .

HY-179646

CIAC101	Toll-like Receptor (TLR) NO Synthase NF-κB TNF Receptor Interleukin Related	Neurological Disease
CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC₅₀ of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (HY-D1056) (LPS)-induced NF-κB activation and reduces the expression of pro-inflammatory mediators (iNOS, IL-1β, TNF-α, and IL-6). CIAC101 robust antineuroinflammatory activity with efficacy against drug-evoked neurobehavioral adaptations. CIAC101 can be used for the research of addiction and neurological disease .

HY-182011

GPR6 inverse agonist 2	GPR6	Neurological Disease
GPR6 inverse agonist 2 (Compound 575) is a selective GPR6 inverse agonist, with IC₅₀ values of < 0.1 μM and 1~30 μM against GPR6 and GPR3, respectively. GPR6 inverse agonist 2 exhibits preliminary cardiac safety, with an IC₅₀ of 21.71 μM for hERG. GPR6 inverse agonist 2 can be used in the research of movement disorders such as Parkinson's disease .

Cat. No.	Product Name

HY-L083

Anti-Cancer Metabolism Compound Library	3,552 compounds
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth. MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

Anti-Cancer Metabolism Compound Library

3,552 compounds

Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.

MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P2259

TAT-GluA2 3Y 2 Publications Verification	iGluR HIV Integrase Adenosine Receptor	Cardiovascular Disease Neurological Disease
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .

HY-P2046

β-Endorphin (rat)	Opioid Receptor	Neurological Disease
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .

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