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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:
Synonyms: THCCC
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PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator .
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ONO-8590580 is a GABAA α5 negative allosteric modulator.
Cat. No.: HY-124393
CAS No.: 1253291-12-1
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GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
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VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
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DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic 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-107774
CAS No.: 1801151-09-6
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BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
Cat. No.: HY-115483
CAS No.: 1946021-40-4
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VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease .
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VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
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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.
Cat. No.: HY-W565924
CAS No.: 935685-90-8
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STX107 is a metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulator (NAM) with a pKi of 8.32. STX107 inhibits glutamate-induced Ca 2+ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .
Cat. No.: HY-103320
CAS No.: 652973-93-8
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Calhex 231 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 Ca 2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
Cat. No.: HY-15470
CAS No.: 309712-55-8
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GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
Cat. No.: HY-120411
CAS No.: 111127-62-9
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Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels .
Cat. No.: HY-147558
CAS No.: 2513102-41-3
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CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
Cat. No.: HY-147559
CAS No.: 2513102-64-0
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CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
Cat. No.: HY-168494
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GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penetrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases .
Cat. No.: HY-145370
CAS No.: 2222010-71-9
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GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
Cat. No.: HY-119765
CAS No.: 1243310-20-4
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VU0366248 is a mGlu5 negative allosteric modulator .
Cat. No.: HY-103573
CAS No.: 1274859-33-4
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VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM .
Cat. No.: HY-119941
CAS No.: 1848252-81-2
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VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM .
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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
