BMS-984923

Name: BMS-984923
Brand: MedChemExpress
SKU: HY-122559
Rating: 4.5 (1 reviews)

Cat. No.: HY-122559 Purity: 99.94% ee.: 100%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (K_i = 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.

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 605	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3000	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4800	In-stock	Estimated Time of Arrival: December 31
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:

(S,S)-BMS-984923 Get quote

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View All Isoforms

mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	> 3000 nM Compound: 16; BMS-984923	Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay	[PMID: 27496211]
HEK293	EC₅₀	> 3000 nM Compound: 16; BMS-984923	Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay	[PMID: 27496211]

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.

1375752-78-5

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
10 mM	0.2668 mL	1.3340 mL	2.6679 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

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

Handling Instructions (2659 KB)

References

[1]. Laura T Haas, et al. Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer's Mouse Phenotypes. Cell Rep. 2017 Jul 5;20(1):76-88. [Content Brief]

[2]. Hong Huang, et al. Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. [Content Brief]

Complete Stock Solution Preparation Table

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

BMS-984923 Related Classifications

Neurological Disease

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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BMS-984923

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Other Forms of BMS-984923:

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View All mGluR Isoform Specific Products:

Biological Activity

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References

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Complete Stock Solution Preparation Table

BMS-984923 Related Classifications

Keywords:

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