2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  3. Endogenous Metabolite mGluR Phosphatase
  4. DL-AP3

DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect.

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DL-AP3 Chemical Structure

DL-AP3 Chemical Structure

CAS No. : 5652-28-8

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Based on 1 publication(s) in Google Scholar

DL-AP3 Related Antibodies

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Description

DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect[1][2][3].

IC50 & Target[1]

mGluR 1

 

mGluR 5

 

In Vitro

DL-AP3 (10 µM, 6 h) alleviates oxygen-glucose deprivation (OGD)-induced injury (cell viability) in primary neurons[1].
DL-AP3 (10 µM, 6 h) recovers the decreased levels of p-Akt1 and the increase of cytochrome C induced by OGD in primary neurons[1].
DL-AP3 (1-100 µM) inhibits activity of rat brain phosphoserine phosphatase, with an IC50 of 187 µM and Ki of 77 µM[2].
DL-AP3 (10 μM, 10 min) together with SKF81297 (5  μM) induces a significant Long-term potentiation (LTP) in the slices of Fmr1 KO mice[3].

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

DL-AP3 Related Antibodies

Cell Viability Assay[1]

Cell Line: Primary neurons with oxygen-glucose deprivation (OGD) treatment
Concentration: 10 µM
Incubation Time: 24 h or 72 h
Result: Attenuated the inhibitory effect of OGD on neuronal viability.

Western Blot Analysis[1]

Cell Line: Primary neurons with oxygen-glucose deprivation (OGD) treatment
Concentration: 10 µM
Incubation Time: 6 h
Result: Increased the decreased levels of p-Akt1, and decreased the increase of cytochrome C.
In Vivo

DL-AP3 (4 mg/kg,  i.p., for 5 weeks) with SKF81297 (1 mg/kg,  i.p.) reduces the hyperactivity phenotype in Fmr1 KO mice[3].
DL-AP3 (4.0-12.0 mg/animal, i.c.v. infusion, 100 μL) blocks development of visceral pain symptoms and neuroendocrinological changes in the blood plasma of sheep[4].

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

Animal Model: Fmr1 KO mice[3]
Dosage: 4 mg/kg with SKF81297 (1 mg/kg)
Administration: i.p., for 5 weeks.
Result: Reduced the distance traveled by Fmr1 KO mice (open-field test).
Reduced the swim latency on the final day in the Fmr1 KO mice (Morris Water Maze test).
Animal Model: Sheep with visceral pain evoked by colonic distension (CD)[4]
Dosage: 4.0-12.0 mg/animal
Administration: i.c.v. infusion, 100 μL
Result: Decreased intensity from appearance of clinical signs of visceral pain caused by CD test.
Diminished the increase of plasma cortisol, E, NE and DA concentrations caused by visceral pain provoked by CD episode.
Molecular Weight

169.07

Formula

C3H8NO5P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(CP(O)(O)=O)C(O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 5 mg/mL (29.57 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.9147 mL 29.5735 mL 59.1471 mL
5 mM 1.1829 mL 5.9147 mL 11.8294 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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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C2

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

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working 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).
Purity & Documentation

Purity: ≥98.0%

COA (247 KB) HNMR (251 KB) CNMR (309 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 (sealed storage, away from moisture). 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
H2O 1 mM 5.9147 mL 29.5735 mL 59.1471 mL 147.8677 mL
5 mM 1.1829 mL 5.9147 mL 11.8294 mL 29.5735 mL
10 mM 0.5915 mL 2.9574 mL 5.9147 mL 14.7868 mL
15 mM 0.3943 mL 1.9716 mL 3.9431 mL 9.8578 mL
20 mM 0.2957 mL 1.4787 mL 2.9574 mL 7.3934 mL
25 mM 0.2366 mL 1.1829 mL 2.3659 mL 5.9147 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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DL-AP3 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:

DL-AP35652-28-8Endogenous MetabolitemGluRPhosphataseMetabotropic glutamate receptorsOxygen-glucose deprivationOGDneuronneuroprotectiveFmr1 KOpainInhibitorinhibitorinhibit

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