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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
10039 Results for "
selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (10039)
10039 Results for "selectivity" in MCE Product Catalog:
Cat. No.: HY-10912R
CAS No.: 574013-66-4
Fexaramine (Standard) is the analytical standard of Fexaramine. This product is intended for research and analytical applications. Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .
Cat. No.: HY-109137R
CAS No.: 2004677-13-6
Synonyms: GS-9688 (Standard)
Research Areas:
Selgantolimod (Standard) is the analytical standard of Selgantolimod (HY-109137). This product is intended for research and analytical applications. Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection .
Synonyms: NT-814; BAY3427080
Target:
Research Areas:
Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
Cat. No.: HY-109197R
CAS No.: 1192171-69-9
Synonyms: EYP001 (Standard)
Target:
Research Areas:
Vonafexor (Standard) is the analytical standard of Vonafexor (HY-109197). This product is intended for research and analytical applications. Vonafexor (EYP001) is an orally active, non-steroidal and selective FXR agonist. Vonafexor shows significant HBsAg reduction when combined with Peg-IFNα. Vonafexor can be used for anti-HBV research .
Cat. No.: HY-10959R
CAS No.: 939981-39-2
Synonyms: RO5045337 (Standard)
Research Areas:
RG7112 (Standard) is the analytical standard of RG7112 (HY-10959). This product is intended for research and analytical applications. RG7112 is a potent, selective, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a Kd of 11 nM for binding to MDM2 .
Cat. No.: HY-110165R
CAS No.: 949467-71-4
Research Areas:
hENT4-IN-1 (Standard) is the analytical standard of hENT4-IN-1 (HY-110165). This product is intended for research and analytical applications. hENT4-IN-1 is a potent and selective human ENT4 (equilibrative nucleoside transporter 4) inhibitor with an IC50 of 74.4 nM .
Research Areas:
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo .
Cat. No.: HY-110198
CAS No.: 459841-96-4
Target:
Research Areas:
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
Cat. No.: HY-110244R
CAS No.: 1600515-49-8
Target:
Research Areas:
Tilfrinib (Standard) is the analytical standard of Tilfrinib (HY-110244). This product is intended for research and analytical applications. Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour .
Target:
Research Areas:
RA839 is a selective Nrf2/ARE pathway agonist and non-covalent small molecule binder of Keap1 (Kd is approximately 6 μM). RA839 prevents inducible nitric oxide synthase expression and nitric oxide release. RA839 exerts anti-rotaviral and anti-inflammatory effects .
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
PF-03654746 Tosylate is a potent, selective and brain-penetrant histamine H3 receptor antagonist. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
Cat. No.: HY-11067R
CAS No.: 211555-05-4
Target:
Research Areas:
WHI-P97 (Standard) is the analytical standard of WHI-P97 (HY-11067). This product is intended for research and analytical applications. WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .
Cat. No.: HY-11070R
CAS No.: 934995-87-6
Research Areas:
MK-0952 (Standard) is the analytical standard of MK-0952 (HY-11070). This product is intended for research and analytical applications. MK-0952 is a selective and orally active PDE4 inhibitor, with an IC50 of 0.53 nM. MK-0952 has the potential for Alzheimer’s disease study .
Cat. No.: HY-11087R
CAS No.: 271576-80-8
Synonyms: SD-06 (Standard)
Target:
Research Areas:
SD 0006 (Standard) is the analytical standard of SD 0006 (HY-11087). This product is intended for research and analytical applications. SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP Kinase, with an IC50 of 110 nM for p38α .
Cat. No.: HY-L932V0
2,000,000 compounds
Macrocyclic compounds (≥12-atom cyclic small molecules/peptides) have unique physicochemical properties. They form preorganized conformations with high binding affinity/selectivity, target traditional small-molecule-inaccessible proteins, and bridge small-molecule drugs and biological agents. As key protein phosphorylation enzymes, kinases are linked to tumors, COPD, etc., and are critical therapeutic targets. Traditional small-molecule kinase inhibitors lack selectivity, causing off-target toxicity, low bioavailability, and acquired resistance. Macrocycles’ semi-rigid structure restricts conformations, boosts binding selectivity, optimizes pharmacokinetics, and makes macrocyclization a core kinase inhibitor optimization strategy.
Thousands of bioactive macrocycles were curated from ChEMBL. Via Transformer, macrocyclization was converted into a chemical language translation task, enabling end-to-end macrocycle generation from linear precursors with simplified inputs. Macformer achieves efficient, automated linear molecule macrocyclization via deep learning; generated macrocycles have diversity, novelty, biocompatibility, and cover broader chemical space.
MCE collected thousands of marketed/clinical kinase inhibitors, using their fragments for macrocyclization to generate derivatives. After evaluating synthetic accessibility and physicochemical properties, a million-scale virtual macrocyclic library was built for kinase-related virtual and AI-driven screening.
Cat. No.: HY-L932V
2,000,000 compounds
Macrocyclic compounds (≥12-atom cyclic small molecules/peptides) have unique physicochemical properties. They form preorganized conformations with high binding affinity/selectivity, target traditional small-molecule-inaccessible proteins, and bridge small-molecule drugs and biological agents. As key protein phosphorylation enzymes, kinases are linked to tumors, COPD, etc., and are critical therapeutic targets. Traditional small-molecule kinase inhibitors lack selectivity, causing off-target toxicity, low bioavailability, and acquired resistance. Macrocycles’ semi-rigid structure restricts conformations, boosts binding selectivity, optimizes pharmacokinetics, and makes macrocyclization a core kinase inhibitor optimization strategy.
Thousands of bioactive macrocycles were curated from ChEMBL. Via Transformer, macrocyclization was converted into a chemical language translation task, enabling end-to-end macrocycle generation from linear precursors with simplified inputs. Macformer achieves efficient, automated linear molecule macrocyclization via deep learning; generated macrocycles have diversity, novelty, biocompatibility, and cover broader chemical space.
MCE collected thousands of marketed/clinical kinase inhibitors, using their fragments for macrocyclization to generate derivatives. After evaluating synthetic accessibility and physicochemical properties, a million-scale virtual macrocyclic library was built for kinase-related virtual and AI-driven screening.
Cat. No.: HY-L941
4,236 compounds
Orthosteric sites are highly conserved, leading to poor subtype selectivity, off-target toxicity and drug resistance in traditional drugs. By contrast, allosteric sites show low conservation, high hydrophobicity, weak polarity, confined geometry and dynamic cryptic properties, granting modulators high selectivity, functional tunability and safety. Thus, allosteric therapy has become a major focus in drug discovery.
MCE curated nearly 1,000 clinical-stage allosteric modulators, analyzed PDB complex structures to identify key pharmacophores and privileged scaffolds, then designed and filtered compounds using rational “scaffold derivation + physicochemical screening” with strict property criteria. The resulting compounds show high rigidity and shape complementarity to shallow, dynamic, hydrophobic allosteric pockets.
This library comprises 4,315 diverse, lead-like compounds ideal for allosteric drug discovery and target screening, covering kinases, GPCRs and more. All are analogs of clinical-stage molecules with similarity > 0.6, combining high druggability and allosteric binding potential to support efficient early-stage R&D.
Cat. No.: HY-K0361
MCE Mouse Pan B Cell Negative Selection Kit enables the efficient isolation of total B cells from mouse spleen, lymph nodes, bone marrow, or peritoneal lavage fluid. The principle involves using biotin-labeled monoclonal antibodies to label non-target cells (non-B cells), followed by the removal of these non-target cells through streptavidin-labeled magnetic beads, achieving the selective isolation of mouse B Cells.
Cat. No.: HY-L222
1,213 compounds
Linkers play a necessary role in the physicochemical properties and biological activity of the bifunctional molecule. These linkers are not a simply connection of two functional modules together, but its design and nature directly affect the stability, activity, selectivity, pharmacokinetics, and ultimately the therapeutic efficacy of the entire molecule. The length of the linker determines the extent of interaction between the two ligands and thus the maximum activity of the PROTAC molecule.
MCE has collected 1,213 PROTAC Linkers can be used for the design and synthesis of bifunctional molecules.
Cat. No.: HY-K0357
MCE Mouse Mature B Cell Negative Selection Kit enables the efficient isolation of mature B cells from single-cell suspensions prepared from mouse spleen, lymph nodes, or bone marrow. The principle involves using biotin-labeled monoclonal antibodies to label non-target cells (non-B cells), followed by the removal of these non-target cells through streptavidin-labeled magnetic beads, achieving the selective isolation of mouse mature B cells.
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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
