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

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

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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

BMT-145027 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

BMT-145027 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

438.83

Formula

C23H14ClF3N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 2.4 mg/mL (5.47 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2788 mL 11.3939 mL 22.7879 mL 56.9697 mL
5 mM 0.4558 mL 2.2788 mL 4.5576 mL 11.3939 mL
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BMT-145027 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMT-1450272018282-44-3BMT145027BMT 145027mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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