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BMT-145027
CAS No. 2018282-44-3
BMT-145027( —— )
Catalog No. M26073 CAS No. 2018282-44-3
BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 177 | Get Quote |
|
| 10MG | 305 | Get Quote |
|
| 25MG | 518 | Get Quote |
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| 50MG | 743 | Get Quote |
|
| 100MG | 1017 | Get Quote |
|
| 500MG | 2061 | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameBMT-145027
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NoteResearch use only, not for human use.
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Brief DescriptionBMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).
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DescriptionBMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).(In Vitro):BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM. BMT-145027 exhibits high MsLM stability (85% remaining) and a modest decrease in planarity (Fsp3 = 0.17).(In Vivo):BMT-145027 (30 mg/kg) leads to a significant increase in time spent with the novel object, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals(BMT-145027: 30 mg/kg) indicates a total plasma concentration of 2800 nM.
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In VitroBMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC50=47 nM), and a modest decrease in planarity (Fsp3 = 0.17). Importantly, BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM.
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In VivoDrug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the mice are reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spend more time exploring unfamiliar objects, improved memory is measured as time spent exploring the novel object. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30 mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a total plasma concentration of 2800 nM at 30 mg/kg.
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Synonyms——
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PathwayNeuroscience
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TargetGluR
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Recptor——
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Research Area——
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Indication——
Chemical Information
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CAS Number2018282-44-3
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Formula Weight438.84
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Molecular FormulaC23H14ClF3N4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 2.4 mg/mL (5.47 mM)
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SMILESFC(F)(F)c1cc(ccc1Cl)-c1n[nH]c2nc(-c3ccccc3)c(C#N)c(C3CC3)c12
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Evans blue
Evans Blue is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT).
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XAP044
XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm.
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Basimglurant
Basimglurant is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM).
