Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
55 Results for "
abuse liability
" in MedChemExpress (MCE) Product Catalog:
Products (55)
55 Results for "abuse liability" in MCE Product Catalog:
13
13 Publications Verification
Synonyms: AZD1390
Target:
Research Areas:
Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
4
4 Cited Publications
Cat. No.: HY-18101A
CAS No.: 206996-13-6
Target:
Research Areas:
BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .
3
3 Cited Publications
Target:
Research Areas:
HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability .
1
Target:
Research Areas:
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
Category:
Simple Phenylpropanols Phenylpropanoids Plants Myristica fragrans Houtt. Myristicaceae Extract
Target:
Cat. No.: HY-172429
CAS No.: 2489185-38-6
Synonyms: ORIC-114
Target:
Research Areas:
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-162455
CAS No.: 3041127-59-4
Target:
Research Areas:
NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders .
Cat. No.: HY-168046
CAS No.: 2542029-03-6
Target:
Research Areas:
ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .
Synonyms: MM-110; (±)-18-Methoxycoronaridine
Research Areas:
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse . Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis .
Cat. No.: HY-172429A
Synonyms: ORIC-114 hemihydrate
Target:
Research Areas:
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-16639
CAS No.: 1448895-09-7
Target:
Research Areas:
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
Target:
Research Areas:
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
Target:
Research Areas:
SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .
Target:
Research Areas:
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics .
Cat. No.: HY-161511
CAS No.: 2641630-97-7
Target:
Research Areas:
LPH-5 is a selective 5-HT2A receptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2A receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2A receptor. LPH-5 can be used to further explore the 5-HT2A receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .
Cat. No.: HY-175258
CAS No.: 3105974-36-2
Research Areas:
PAD2/4-IN-1 (Compound 4f) is an orally active inhibitor of PAD2 and PAD4 with IC50 values of 23 nM and 10 nM, respectively. PAD2/4-IN-1 can inhibit protein citrullination in neutrophils and reduce hERG channel liabilities. PAD2/4-IN-1 can be used in the research of autoimmune diseases, neurological disorders, and cancers .
Cat. No.: HY-W002328
CAS No.: 1621-91-6
Cat. No.: HY-139266
CAS No.: 1438278-55-7
Target:
Research Areas:
7'-Methoxy NABUTIE (Compound 23) is a derivative of Aminoalkylindole. 7'-Methoxy NABUTIE can be used in the study of alcohol abuse .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
