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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
214 Results for "
PAM,
" in MedChemExpress (MCE) Product Catalog:
Products (214)
214 Results for "PAM," in MCE Product Catalog:
Cat. No.: HY-175670
Target:
Research Areas:
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
Cat. No.: HY-184478
CAS No.: 3103822-75-6
Target:
Research Areas:
GABAA receptor modulator-14 is an orally active, blood-brain barrier permeable selective positive allosteric modulator (PAM) of extrasynaptic δ-containing GABAA receptors (α4β3δ subtype) with an EC50 of 0.8 μM. GABAA receptor modulator-14 selectively enhances tonic neuronal inhibition by potentiating GABA-evoked currents mediated by extrasynaptic δ-GABAARs, produces rapid sustained antidepressant effects, elevates slow-wave NREM sleep and shows no addiction liability in mice. GABAA receptor modulator-14 can be applied to major depressive disorder (MDD) and comorbid insomnia research .
Cat. No.: HY-N0754
CAS No.: 877822-40-7
Cat. No.: HY-P70948
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: F11R; JAM-A; Prev. JAM1; JAMA; Junctional Adhesion Molecule 1; Platelet Adhesion Molecule 1; PAM-1; Platelet F11 Receptor; JCAM; CD321 Antigen; Junctional Adhesion Molecule A; JAM; JAM-1; KAT; F11 Receptor; CD321
Species:
Human
Source:
HEK293
Cat. No.: HY-P73853
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: F11R; JAM-A; Prev. JAM1; JAMA; Junctional Adhesion Molecule 1; Platelet Adhesion Molecule 1; PAM-1; Platelet F11 Receptor; JCAM; CD321 Antigen; Junctional Adhesion Molecule A; JAM; JAM-1; KAT; F11 Receptor; CD321
Species:
Rat
Source:
HEK293
Cat. No.: HY-P73854
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: F11R; JAM-A; Prev. JAM1; JAMA; Junctional Adhesion Molecule 1; Platelet Adhesion Molecule 1; PAM-1; Platelet F11 Receptor; JCAM; CD321 Antigen; Junctional Adhesion Molecule A; JAM; JAM-1; KAT; F11 Receptor; CD321
Species:
Rat
Source:
HEK293
Cat. No.: HY-P73855
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: F11R; JAM-A; Prev. JAM1; JAMA; Junctional Adhesion Molecule 1; Platelet Adhesion Molecule 1; PAM-1; Platelet F11 Receptor; JCAM; CD321 Antigen; Junctional Adhesion Molecule A; JAM; JAM-1; KAT; F11 Receptor; CD321
Species:
Mouse
Source:
HEK293
Cat. No.: HY-P78322
Purity: ≥ 95%, as determined by Bis-Tris PAGE.
Synonyms: F11R; JAM-A; Prev. JAM1; JAMA; Junctional Adhesion Molecule 1; Platelet Adhesion Molecule 1; PAM-1; Platelet F11 Receptor; JCAM; CD321 Antigen; Junctional Adhesion Molecule A; JAM; JAM-1; KAT; F11 Receptor; CD321
Species:
Mouse
Source:
HEK293
Cat. No.: HY-175505
CAS No.: 2894793-37-2
Target:
Research Areas:
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-P703041
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: UHMK1; U2AF Homology Motif Kinase 1; KIS; Kist; PAM COOH-Terminal Interactor Protein 2; Serine/Threonine-Protein Kinase Kist; U2AF Homology Motif (UHM) Kinase 1; P-CIP2; Kinase Interacting With Leukemia-Associated Gene (Stathmin); Kinase Interacting With
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-175504
CAS No.: 932544-59-7
Target:
Research Areas:
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Synonyms: RG-7816; RO-7017773
Target:
Research Areas:
Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .
Cat. No.: HY-175532
CAS No.: 3062458-27-6
Target:
Research Areas:
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
Cat. No.: HY-L170
258 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 258 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
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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
