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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
87 Results for "
Orthosteric
" in MedChemExpress (MCE) Product Catalog:
Products (87)
87 Results for "Orthosteric" 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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2 Cited Publications
Synonyms: AVL-3288; UCI-4083
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CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
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2 Cited Publications
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VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
1
1 Cited Publications
Cat. No.: HY-W011417
CAS No.: 606-59-7
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Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
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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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1 Cited Publications
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BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
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YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .
Cat. No.: HY-175552
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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-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 .
CCX-777 is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 is widely used in cancer-related research .
Cat. No.: HY-W011417R
CAS No.: 606-59-7
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Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
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SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis .
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-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-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 .
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ONO-9780307 is a specific synthetic LPA1 (lysophosphatidic acid receptor 1) antagonist with an IC50 value of 2.7 nM .
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 .
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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
