2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. BMS-984923

BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.

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BMS-984923 Chemical Structure

BMS-984923 Chemical Structure

CAS No. : 1375752-78-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 605 In-stock
Solution
10 mM * 1 mL in DMSO USD 605 In-stock
Solid
1 mg USD 220 In-stock
5 mg USD 550 In-stock
10 mg USD 900 In-stock
25 mg USD 1850 In-stock
50 mg USD 3000 In-stock
100 mg USD 4800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BMS-984923:

BMS-984923 Related Antibodies

Top Publications Citing Use of Products

View All mGluR Isoform Specific Products:

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling[1][2].

In Vivo

BMS-984923 (7.5 mg/kg or 15 mg/kg, oral gavage, once) exhibits good oral bioavailability and BBB penetration[1].

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

Animal Model: C57Bl6J male mice[1].
Dosage: 7.5 mg/kg or 15 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage, once.
Result: The plasma concentration exceeded 2 μM at 10 hr. Brain concentrations were nearly as high as plasma concentrations when measured 3 hr after a 7.5 mg/kg oral dose
Clinical Trial
Molecular Weight

374.82

Formula

C22H15ClN2O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1O[C@H](C2=CC=CC=C2Cl)[C@@H](C3=CC(C#CC4=CC=CC=C4)=CN=C3)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (133.40 mM; Need ultrasonic; 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 2.6679 mL 13.3397 mL 26.6795 mL
5 mM 0.5336 mL 2.6679 mL 5.3359 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.67 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.94% ee.: 100%

COA (253 KB) HNMR (259 KB) NP-HPLC (119 KB) LCMS (257 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6679 mL 13.3397 mL 26.6795 mL 66.6987 mL
5 mM 0.5336 mL 2.6679 mL 5.3359 mL 13.3397 mL
10 mM 0.2668 mL 1.3340 mL 2.6679 mL 6.6699 mL
15 mM 0.1779 mL 0.8893 mL 1.7786 mL 4.4466 mL
20 mM 0.1334 mL 0.6670 mL 1.3340 mL 3.3349 mL
25 mM 0.1067 mL 0.5336 mL 1.0672 mL 2.6679 mL
30 mM 0.0889 mL 0.4447 mL 0.8893 mL 2.2233 mL
40 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6675 mL
50 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3340 mL
60 mM 0.0445 mL 0.2223 mL 0.4447 mL 1.1116 mL
80 mM 0.0333 mL 0.1667 mL 0.3335 mL 0.8337 mL
100 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6670 mL
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BMS-984923 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:

BMS-9849231375752-78-5BMS984923BMS 984923mGluRMetabotropic glutamate receptorsAlzheimer'sdiseaseSAMAβoInhibitorinhibitorinhibit

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