1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. BMT-145027

BMT-145027 

Cat. No.: HY-100728 Purity: 98.19%
Handling Instructions

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.

For research use only. We do not sell to patients.

BMT-145027 Chemical Structure

BMT-145027 Chemical Structure

CAS No. : 2018282-44-3

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Based on 1 publication(s) in Google Scholar

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Description

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.

IC50 & Target[1]

mGluR5

47 nM (EC50)

In Vitro

BMT-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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Drug-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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

438.83

Formula

C₂₃H₁₄ClF₃N₄

CAS No.

2018282-44-3

SMILES

ClC(C(C(F)(F)F)=C1)=CC=C1C2=NNC3=NC(C4=CC=CC=C4)=C(C#N)C(C5CC5)=C32

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2.4 mg/mL (5.47 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2788 mL 11.3939 mL 22.7879 mL
5 mM 0.4558 mL 2.2788 mL 4.5576 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Competition binding experiments are performed using a single concentration ( 5 nM) of [3H]-MethoxyPyEP in the presence of increasing concentrations of BMT-145027. The reaction is terminated by the addition of 5 mL of ice-cold ish buffer and rapid filtration. The filter is punched into a 96 well flex-plate and scintillation cocktail is added to each well. The plate is allowed to soak for 8 h and then read on the micro-beta counter. IC50 values are determined using non-linear regression four-parameter logistic equation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice are dosed i.p. with either vehicle or BMT-145027 at 10 and 30 mg/kg 60 min prior to the training session and tested for recognition. Animal behavior is video recorded during both training and testing and the amount of time spent exploring the objects determined using Cleversys software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BMT-145027BMT145027BMT 145027mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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BMT-145027
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HY-100728
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