2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. VU6010572

VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant.

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

VU6010572 Chemical Structure

VU6010572 Chemical Structure

CAS No. : 2126784-39-0

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5 mg USD 250 In-stock
10 mg USD 406 In-stock
25 mg USD 812 In-stock
50 mg USD 1300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

VU6010572 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant[1][2].

IC50 & Target

mGluR3

245 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
245 nM
Compound: 4; VU6010572
Negative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence as
Negative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence as
[PMID: 31358468]
In Vivo

VU6010572 (3 mg/kg; i.p.) shows robust efficacy[1].
VU6010572 (3 mg/kg; i.p.; 45 minutes) produces lasting anxiolytic-like behavioral effects[2].

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

Animal Model: CD-1 mice[1]
Dosage: 3 mg/kg
Administration: I.p.
Result: Showed robust efficacy.
Animal Model: Rats[2]
Dosage: 3 mg/kg
Administration: I.p.; 45 minutes
Result: Produced lasting anxiolytic-like behavioral effects.
Molecular Weight

339.36

Formula

C20H18FNO3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=C(OC[C@@H](OC2=CC=CC=C2)C)C=CN1C3=CC=C(F)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (294.67 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 2.9467 mL 14.7336 mL 29.4672 mL
5 mM 0.5893 mL 2.9467 mL 5.8934 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 (protect from light, stored under nitrogen). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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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

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 (protect from light, stored under nitrogen). 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 2.9467 mL 14.7336 mL 29.4672 mL 73.6681 mL
5 mM 0.5893 mL 2.9467 mL 5.8934 mL 14.7336 mL
10 mM 0.2947 mL 1.4734 mL 2.9467 mL 7.3668 mL
15 mM 0.1964 mL 0.9822 mL 1.9645 mL 4.9112 mL
20 mM 0.1473 mL 0.7367 mL 1.4734 mL 3.6834 mL
25 mM 0.1179 mL 0.5893 mL 1.1787 mL 2.9467 mL
30 mM 0.0982 mL 0.4911 mL 0.9822 mL 2.4556 mL
40 mM 0.0737 mL 0.3683 mL 0.7367 mL 1.8417 mL
50 mM 0.0589 mL 0.2947 mL 0.5893 mL 1.4734 mL
60 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
80 mM 0.0368 mL 0.1842 mL 0.3683 mL 0.9209 mL
100 mM 0.0295 mL 0.1473 mL 0.2947 mL 0.7367 mL
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VU6010572 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:

VU60105722126784-39-0VU 6010572VU-6010572mGluRMetabotropic glutamate receptorspotentselectivemGlu3allostericCNSpenetrantInhibitorinhibitorinhibit

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