L-AP4 monohydrate

SKU:BHB21900038
Research Validated
Overview
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L-AP4 monohydrate (CAS 2247534-79-6) is an agonist supplied as a solid. Reported to act on mGlu, mGlu8, mGlu7. Relevant to GPCR/G Protein and Neuronal Signaling research. Molecular formula C4H12NO6P, molecular weight 201.11 g/mol.
Purity 99.0%
CAS Number 2247534-79-6
Molecular Weight 201.11 g/mol
Form Solid
Target mGlu, mGlu8, mGlu7
Storage 4°C as supplied; in solvent -80°C
Options selector
Catalog no. Size
HY-100781B-5MG 5 mg
HY-100781B-10MG 10 mg
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg
  • Lead time: shown per option in the variant selector.
  • Storage: 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: refrigerate at 4°C as soon as possible.
Field Specification
Target mGlu, mGlu8, mGlu7
Alternative names L-APB monohydrate
CAS no. 2247534-79-6
Applications
  • Functional Assay (In Vitro)
Molecular weight 201.11
Molecular formula C4H12NO6P
Purity 99.0%
SMILES O=C(O)[C@@H](N)CCP(O)(O)=O.O
Form Solid
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-100781B
Main SKU BHB21900038
Agonists

Compound Overview

L-AP4 monohydrate, also known as L-APB monohydrate, is a potent, specific agonist of the group III mGluRs, with EC50 values of 0.13 μM, 0.29 μM, 1.0 μM and 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. It is supplied as a white to off-white solid (C4H12NO6P, MW 201.11) at 99.0% purity.

Physical & Chemical Properties

CAS Number 2247534-79-6
Molecular Formula C4H12NO6P
Molecular Weight 201.11 g/mol
Purity 99.0%
Appearance Solid
Color White to off-white
SMILES O=C(O)[C@@H](N)CCP(O)(O)=O.O
Target mGlu, mGlu8, mGlu7
Signaling Pathway GPCR/G Protein; Neuronal Signaling
Solubility In Vitro: DMSO: 10 mg/mL (49.72 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

IC50 & Target[1]

mGlu4

0.13 μM (EC50)

mGlu8

0.29 μM (EC50)

mGlu6

1.0 μM (EC50)

mGlu7

249 μM (EC50)

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989.

[2]. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

SolventSolubilityNotes
DMSO10 mg/mL (49.72 mM)requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility)

Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.

Data provided by the manufacturer.

In Vivo

In eight nerve-ligated rats, the paw withdrawal threshold to von Frey filament application rises significantly, and does so dose-dependently, with L-AP4 (5-30 μg, intrathecal injection 4-5 days). No evident motor dysfunction accompanies intrathecal delivery of the various L-AP4 doses[2]. Paw withdrawal latency in these normal rats is not significantly changed by an intrathecal injection of L-AP4 at 30 μg[2]. When 5 to 50 μM L-AP4 was applied topically to the spinal cord, neuronal responses evoked by touch, pressure, pinch, and von Frey filaments were significantly inhibited, with the extent of inhibition depending on concentration[2].

Animal ModelRats.[2]
Dosage5-30 μg.
AdministrationIntrathecal inhection 4-5 days.
ResultDose-dependently increased paw withdrawal threshold.

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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Identification of 2-PMPA as a novel inhibitor of cytosolic carboxypeptidases. Biochem Biophys Res Commun 2020 Dec 17;533(4):1393-1399. PMID: 33092792

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