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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
108 Results for "
Negative allosteric modulator
" in MedChemExpress (MCE) Product Catalog:
Products (108)
108 Results for "Negative allosteric modulator" in MCE Product Catalog:
Cat. No.: HY-16636
CAS No.: 1443118-44-2
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ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 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-129274
CAS No.: 911114-85-7
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RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [ 3h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers .
Cat. No.: HY-117467
CAS No.: 1801151-15-4
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BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power .
Cat. No.: HY-P11259
CAS No.: 3090687-02-5
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
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AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
Cat. No.: HY-129636A
CAS No.: 797-17-1
Synonyms: GABAB receptor antagonist 1
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(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
Cat. No.: HY-118285
CAS No.: 579482-31-8
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Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
Cat. No.: HY-157998
CAS No.: 2760515-88-4
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
Cat. No.: HY-103574R
CAS No.: 757949-98-7
Synonyms: ADX-10059 hydrochloride (Standard)
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Raseglurant hydrochloride (Standard) is the analytical standard of Raseglurant hydrochloride (HY-103574). This product is intended for research and analytical applications. Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .
Cat. No.: HY-120093
CAS No.: 1663564-42-8
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GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases .
Cat. No.: HY-110191R
CAS No.: 1443748-47-7
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VU0469650 (Standard) is the analytical standard of VU0469650 (HY-110191). This product is intended for research and analytical applications. VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
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.
Cat. No.: HY-100667R
CAS No.: 2199-87-3
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UBP608 (Standard) is the analytical standard of UBP608 (HY-100667). This product is intended for research and analytical applications. UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .
Cat. No.: HY-103561R
CAS No.: 6971-97-7
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DCB (Standard) is the analytical standard of DCB (HY-103561). This product is intended for research and analytical applications. DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of the metabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5). DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .
Cat. No.: HY-108710R
CAS No.: 1809085-30-0
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VU0650786 (Standard) is the analytical standard of VU0650786 (HY-108710). This product is intended for research and analytical applications. VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
Cat. No.: HY-101281R
CAS No.: 2092923-21-0
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VU 6008667 (Standard) is the analytical standard of VU 6008667 (HY-101281). This product is intended for research and analytical applications. VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .
Cat. No.: HY-103572R
CAS No.: 946619-21-2
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MNI137 (Standard) is the analytical standard of MNI137 (HY-103572). This product is intended for research and analytical applications. MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
Cat. No.: HY-107509R
CAS No.: 885104-09-6
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LY2389575 hydrochloride (Standard) is the analytical standard of LY2389575 (hydrochloride) (HY-107509). This product is intended for research and analytical applications. LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .
Cat. No.: HY-103320AR
CAS No.: 2387505-78-2
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Calhex 231 hydrochloride (Standard) is the analytical standard of Calhex 231 hydrochloride (HY-103320A). This product is intended for research and analytical applications. Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
Cat. No.: HY-103575R
CAS No.: 1224431-15-5
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MFZ 10-7 (Standard) is the analytical standard of MFZ 10-7 (HY-103575). This product is intended for research and analytical applications. MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5 . MFZ 10-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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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
