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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
17 Results for "
conformational disorder
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "conformational disorder" in MCE Product Catalog:
11
11 Publications Verification
Research Areas:
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
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2 Cited Publications
Cat. No.: HY-N0735
CAS No.: 104112-82-5
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LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
Cat. No.: HY-N0735R
CAS No.: 104112-82-5
Cat. No.: HY-144326
CAS No.: 2766509-32-2
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Aβ-IN-1 is a Aβ1-42 aggregation inhibitor. Aβ-IN-1 inhibits Aβ1-42 self-aggregation in vitro by delaying the exponential growth phase or reduces the quantity of fibrils in the steady state. Aβ-IN-1 can be used for the research of conformational disorders .
Cat. No.: HY-144327
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Aβ-IN-2 is a Aβ1-42 aggregation inhibitor. Aβ-IN-2 inhibits Aβ1-42 self-aggregation in vitro by delaying the exponential growth phase or reduces the quantity of fibrils in the steady state. Aβ-IN-2 can be used for the research of conformational disorders .
Cat. No.: HY-174282
CAS No.: 2324109-06-8
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RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD) .
Cat. No.: HY-175807
CAS No.: 1112431-86-3
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ppGalNAc-T2-IN-1 is a polypeptide N-acetylgalactosaminyltransferase 2 (ppGalNAc-T2) inhibitor with an IC50 of 7.11 μM. ppGalNAc-T2-IN-1 is applicable for research on metabolic and neurodevelopmental disorders .
Cat. No.: HY-106964A
CAS No.: 734513-52-1
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(Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia .
Cat. No.: HY-187505
CAS No.: 3052796-86-5
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ZG-2585 is an orally active and selective thyroid hormone receptor β (THRβ) agonist. ZG-2585 selectively activates THRβ over THRα, driving allosteric conformational changes and coactivator recruitment. ZG-2585 reduces body weight, hepatic steatosis and lipid accumulation in a Western diet-induced metabolic disorder model. ZG-2585 can be used for the research of metabolic disorders, including obesity, dyslipidemia and metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-187650
CAS No.: 2507890-46-0
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LuAF60097 is a serotonin transporter (SERT) ligand. LuAF60097 binds to the extracellular vestibule (S2 site) of SERT with high affinity and to the central binding site (S1) with lower affinity, triggering conformational changes that exert combined competitive and non-competitive inhibitory effects on serotonin reuptake. LuAF60097 is applicable to research related to depression and anxiety disorders .
Cat. No.: HY-131642
CAS No.: 53861-57-7
Synonyms: H-Gla-OH
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L-γ-Carboxyglutamic acid (H-Gla-OH) is a mGluR2 antagonist with an IC50 of 102 μM. L-γ-Carboxyglutamic acid binds to the mGluR2 receptor site via the overlapping extended amino acid conformation of its amino and carboxyl groups with glutamic acid, and its additional acidic group locates in a restricted region, thereby blocking the full activation of the receptor. L-γ-Carboxyglutamic acid can be used for the research of neurological disorders .
Cat. No.: HY-180880
CAS No.: 668435-69-6
TFAP2β modulator-1 (compound A6) is a potent TFAP2β modulator that promotes TFAP2β condensation by inducing conformational changes in the intrinsically disordered region. TFAP2β modulator-1 promotes TFAP2β condensation, induces apoptosis, and exhibits anti-tumor functions in esophageal squamous cell carcinoma (ESCC) cells, mouse models, and organoids. TFAP2β modulator-1 can be used for ESCC research .
Cat. No.: HY-181605
CAS No.: 3075862-29-9
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MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder .
Cat. No.: HY-L950
2,742 compounds
Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases.
Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries.
MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.
Cat. No.: HY-181888
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GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND) .
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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
