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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
30 Results for "
orthosteric inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "orthosteric inhibitor" in MCE Product Catalog:
4
4 Cited Publications
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PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
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4 Cited Publications
Cat. No.: HY-N1910
CAS No.: 20784-60-5
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1 Cited Publications
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a Kd of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .
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γ-Glu-Tyr is an orally active gut microbiota-derived metabolite and a competitive DPP-IV inhibitor with an IC50 of 6.77 mM against hDPP-IV. γ-Glu-Tyr weakly activates hCaSR. γ-Glu-Tyr decreases colonic pro-inflammatory cytokine (IL-6, IL-1β, TNF-α) levels. γ-Glu-Tyr activates the cAMP/PKA signaling pathway and inhibits NF-κB phosphorylation, thereby reducing inflammatory responses. γ-Glu-Tyr can be used for research on type 2 diabetes and ulcerative colitis .
Cat. No.: HY-175552
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Cat. No.: HY-174801
CAS No.: 3117797-30-2
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XL-3156 is a cGAS inhibitor. XL-3156 occupies both allosteric and orthosteric sites simultaneously, and inhibits the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of diseases such as autoimmune diseases and inflammation .
Cat. No.: HY-159829
CAS No.: 1803346-98-6
Synonyms: NBI-1117568; HTL-0016878
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
Cat. No.: HY-W668775
CAS No.: 871100-12-8
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Quin-C7 is an orally active FPR2/ALX antagonist. Quin-C7 binds to the orthosteric ligand-binding pocket of FPR2/ALX, modulates receptor activation, and inhibits pro-inflammatory ERK signaling mediated by serum amyloid A (SAA). Quin-C7 reduces pro-inflammatory mediators TNF-α levels, increases anti-inflammatory IL-10, decreases inflammatory neutrophils and pro-inflammatory M1 macrophages, downregulates ERK1/2 phosphorylation, and upregulates JNK1/2/3 phosphorylation. Quin-C7 blocks FPR2/mFpr2 signaling, reduces brain lesion volume. Quin-C7 can be used for the research of inflammatory bowel disease and neuromyelitis optica spectrum disorder .
Cat. No.: HY-176487
CAS No.: 3080315-51-8
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SARM1-IN-6 (Compound 22b) is a brain-permeable SARM1 orthosteric inhibitor, the IC50 of SARM1-IN-6 against NAM is 0.069 μM .
Cat. No.: HY-117764
CAS No.: 1413405-33-0
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LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
Cat. No.: HY-176550
CAS No.: 1787243-08-6
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ASIC1a antagonist-1 (Compound 5b) is an orthosteric noncompetitive Acid sensing ion channels 1a (ASIC1a) antagonist with an IC50 of 27 nM (pH 6.7). ASIC1a antagonist-1 shifts pH dependence of ASIC1a activation and inhibits its maximal evoked response. ASIC1a antagonist-1 completely inhibits long-term potentiation (LTP) induction in CA3-CA1 pathway. ASIC1a antagonist-1 can be used for brain diseases and pathologies research .
Cat. No.: HY-174802
CAS No.: 3117797-77-7
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XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
Cat. No.: HY-170805
CAS No.: 1327276-39-0
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UNC0737 is an orthosteric choline kinase inhibitor. UNC0737 is also a poor inhibitor of G9a (IC50 = 5000 nM) and GLP (IC50 > 10000 nM) in the SAHH-coupled assays .
Cat. No.: HY-176783
CAS No.: 3080315-83-6
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GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research .
Cat. No.: HY-124956
CAS No.: 957136-80-0
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GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research .
Cat. No.: HY-120694
CAS No.: 1355454-05-5
Synonyms: RUC-2
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ML165 (RUC-2) is an aIIbb3 receptor antagonist. ML165 has orthosteric inhibition effect at the RGD binding domain. ML165 inhibits platelet adhesion to fibrinogen, and inhibits platelet aggregation (IC50: 96 nM) .
Cat. No.: HY-158104
Cat. No.: HY-P10051A
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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
