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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
279 Results for "
Inverse agonists
" in MedChemExpress (MCE) Product Catalog:
Products (279)
279 Results for "Inverse agonists" in MCE Product Catalog:
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LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
Cat. No.: HY-U00033
CAS No.: 127985-21-1
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Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging .
Cat. No.: HY-129636
CAS No.: 1611483-29-4
Synonyms: (E)-GABAB receptor antagonist 1
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CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
Cat. No.: HY-181960
CAS No.: 914302-78-6
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BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor (histamine H3 receptor) inverse agonist/antagonist, with a KB value of 0.08 nM for antagonizing agonist-induced activity and an IC50 value of 0.38 nM for directly inhibiting the basal activity of the receptor. BP1.3656B reduces alcohol consumption, alcohol-seeking behavior, alcohol self-administration, motivation to drink, alcohol relapse, alcohol-induced hyperlocomotion, and binge alcohol intake. BP1.3656B is applicable for the research of alcohol use disorder .
Cat. No.: HY-103186R
CAS No.: 264622-53-9
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MRS-1706 (Standard) is the analytical standard of MRS-1706. This product is intended for research and analytical applications. MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction .
Cat. No.: HY-10426R
CAS No.: 725247-18-7
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XCT790 (Standard) is the analytical standard of XCT790 (HY-10426). This product is intended for research and analytical applications. XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
Cat. No.: HY-111226R
CAS No.: 877387-37-6
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GSK5182 (Standard) is the analytical standard of GSK5182 (HY-111226). This product is intended for research and analytical applications. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .
Synonyms: SUVN-G3031
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Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
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Cat. No.: HY-108529R
CAS No.: 215030-90-3
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BMS493 (Standard) is the analytical standard of BMS493 (HY-108529). This product is intended for research and analytical applications. BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation . BMS493 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-14845
CAS No.: 88598-74-7
Synonyms: (S)-Mequitazine
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Levomequitazine (Compound V0114) ((S)-Mequitazine), the levorotatory enantiomer of Mequitazine (HY-B2168), is an orally active, inverse H4 receptor agonist (IC50s: 94 nM (hM2), 17 nM (hM3)). Levomequitazine strongly binds to human histamine H4 receptor. Levomequitazine antagonizes the activating action induced by histamine on H4 receptor. Levomequitazine induces a powerful and statistically significant anti-inflammatory effect. Levomequitazine can be used for research on inflammatory diseases .
Cat. No.: HY-32329
CAS No.: 57262-94-9
Synonyms: Org-8282
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Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
Synonyms: ZK 39106; LSU-65
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FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .
Cat. No.: HY-103146
CAS No.: 859502-43-5
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GR125487 is a highly selective 5-HT4 receptor antagonist and acts as an inverse agonist at constitutively active 5-HT4 (a) receptors. GR125487 inhibits adenylyl cyclase/cAMP signaling by blocking the Gs-coupled 5-HT4 receptor. GR125487 is used in research on 5-HT4 receptor function, neuropsychiatric disorders, and gastrointestinal motility .
Cat. No.: HY-122608
CAS No.: 1394808-82-2
Synonyms: SUVN-G3031 free base
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Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
Cat. No.: HY-32329A
CAS No.: 85650-57-3
Synonyms: MO-8282
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Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Cat. No.: HY-W822786
CAS No.: 144625-67-2
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GR125487 is a highly selective 5-HT4 receptor antagonist and acts as an inverse agonist at constitutively active 5-HT4 (a) receptors. GR125487 inhibits adenylyl cyclase/cAMP signaling by blocking the Gs-coupled 5-HT4 receptor. GR125487 is used in research on 5-HT4 receptor function, neuropsychiatric disorders, and gastrointestinal motility .
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JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis .
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Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Cat. No.: HY-107489R
CAS No.: 883093-10-5
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RO 4938581 (Standard) is the analytical standard of RO 4938581 (HY-107489). This product is intended for research and analytical applications. RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
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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
