VU 0357121

Cat. No.: HY-15393 Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.

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

VU 0357121 Chemical Structure

CAS No. : 433967-28-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 119	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 119	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 69	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 237	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 367	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes^[1].

IC₅₀ & Target^[1]

mGlu5 Receptor

33 nM (EC₅₀)

In Vitro

VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca²⁺ mobilization assay in the low-expressing HEK293A-mGlu5 cell line^[1].

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

Molecular Weight

305.32

Formula

C₁₇H₁₇F₂NO₂

CAS No.

433967-28-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2

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 : ≥ 50 mg/mL (163.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2753 mL	16.3763 mL	32.7525 mL
5 mM	0.6551 mL	3.2753 mL	6.5505 mL
10 mM	0.3275 mL	1.6376 mL	3.2753 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.

Molarity Calculator
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 (8.19 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 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 (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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: 99.73%

Select Batch:

Data Sheet (269 KB) SDS (459 KB)

COA (244 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Hammond. Alexis S, et al. Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chemical Neuroscience (2010), 1(10), 702-716. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2753 mL	16.3763 mL	32.7525 mL	81.8813 mL
	5 mM	0.6551 mL	3.2753 mL	6.5505 mL	16.3763 mL
	10 mM	0.3275 mL	1.6376 mL	3.2753 mL	8.1881 mL
	15 mM	0.2184 mL	1.0918 mL	2.1835 mL	5.4588 mL
	20 mM	0.1638 mL	0.8188 mL	1.6376 mL	4.0941 mL
	25 mM	0.1310 mL	0.6551 mL	1.3101 mL	3.2753 mL
	30 mM	0.1092 mL	0.5459 mL	1.0918 mL	2.7294 mL
	40 mM	0.0819 mL	0.4094 mL	0.8188 mL	2.0470 mL
	50 mM	0.0655 mL	0.3275 mL	0.6551 mL	1.6376 mL
	60 mM	0.0546 mL	0.2729 mL	0.5459 mL	1.3647 mL
	80 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0235 mL
	100 mM	0.0328 mL	0.1638 mL	0.3275 mL	0.8188 mL

VU 0357121 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:

VU 0357121433967-28-3VU0357121VU-0357121mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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