2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. (1R,2S)-VU0155041

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.

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

(1R,2S)-VU0155041 Chemical Structure

(1R,2S)-VU0155041 Chemical Structure

CAS No. : 1263273-14-8

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (1R,2S)-VU0155041:

(1R,2S)-VU0155041 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.

IC50 & Target[1]

mGluR4

 

In Vitro

At both human and rat receptors, the Cis regioisomer of VU0155041 is similar in potency (798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4). Conversely, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. Fold-shift experiments at 30 μM of VU0155041 also shows that the Cis regioisomer is more effective at this concentration on both human and rat mGluR4. VU0155041, induces concentration-dependent shifts in the baseline when examined in fold shift experiments using the thallium flux assay. VU0155041 induces a response that reaches approximately 45% of the maximal glutamate response. VU0155041is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site. VU0155041 exhibitsselectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors[1].

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

(1R,2S)-VU0155041 Related Antibodies
In Vivo

VU0155041 is soluble in an aqueous vehicle and intracerebroventricular administration of 31 to 316 nM of VU0155041 dose-dependently decreases haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041, at doses of 31 and 92 nmol, is also able to significantly decrease the cataleptic effects of haloperidol, and the effects of the compound are still present 30 min after infusion. Icv infusion of a 316 nmol dose of VU0155041 also results in a significant reversal of akinesia[1].

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

316.18

Formula

C14H15Cl2NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@@H](C(NC2=CC(Cl)=CC(Cl)=C2)=O)CCCC1)O
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 (158.14 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 3.1628 mL 15.8138 mL 31.6276 mL
5 mM 0.6326 mL 3.1628 mL 6.3255 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)

Mass
=
Concentration
×
Volume
×
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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.91 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)

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: 95.09%

SDS (393 KB)

COA (251 KB) HNMR (253 KB) RP-HPLC (243 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Rats: TVC rats are injected with reserpine and kept in their home cages for 2 hr after injection. Activity is measured by placing rats in photocell activity cages equipped with 16×16 infrared beams. After a 30 min baseline period, rats are given a single intracerebroventricular injection of either L-AP4 (100, 300 or 1000 nM), VU0155041 (93 or 316 nM), or corresponding vehicles, and motor activity is recorded for an additional 30 min[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 3.1628 mL 15.8138 mL 31.6276 mL 79.0689 mL
5 mM 0.6326 mL 3.1628 mL 6.3255 mL 15.8138 mL
10 mM 0.3163 mL 1.5814 mL 3.1628 mL 7.9069 mL
15 mM 0.2109 mL 1.0543 mL 2.1085 mL 5.2713 mL
20 mM 0.1581 mL 0.7907 mL 1.5814 mL 3.9534 mL
25 mM 0.1265 mL 0.6326 mL 1.2651 mL 3.1628 mL
30 mM 0.1054 mL 0.5271 mL 1.0543 mL 2.6356 mL
40 mM 0.0791 mL 0.3953 mL 0.7907 mL 1.9767 mL
50 mM 0.0633 mL 0.3163 mL 0.6326 mL 1.5814 mL
60 mM 0.0527 mL 0.2636 mL 0.5271 mL 1.3178 mL
80 mM 0.0395 mL 0.1977 mL 0.3953 mL 0.9884 mL
100 mM 0.0316 mL 0.1581 mL 0.3163 mL 0.7907 mL
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(1R,2S)-VU0155041 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:

(1R,2S)-VU01550411263273-14-8mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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