L-AP4 (Synonyms: L-APB)

Cat. No.: HY-100781A Purity: 99.01%: FAQs
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L-AP4 (L-APB) is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively.

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L-AP4 Chemical Structure

CAS No. : 23052-81-5

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Other Forms of L-AP4:

D-AP4 Get quote
L-AP4 monohydrate Get quote

1 Publications Citing Use of MCE L-AP4

•Biochem Biophys Res Commun. 2020 Dec 17;533(4):1393-1399. [Abstract]

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
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Description

L-AP4 (L-APB) is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively^[1]^[2].

IC₅₀ & Target^[1]

mGlu₄

0.13 μM (EC₅₀)

mGlu8

0.29 μM (EC₅₀)

mGlu₆

1.0 μM (EC₅₀)

mGlu7

249 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	> 1000 μM Compound: L-AP4 3	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	[PMID: 16213710]
CHO	EC₅₀	> 1000 μM Compound: L-AP4 3	Activity at rat mGluR5 by measuring intracellular calcium concentration in CHO cells Activity at rat mGluR5 by measuring intracellular calcium concentration in CHO cells	[PMID: 16213710]
CHO	EC₅₀	0.34 μM Compound: L-AP4 3	Activity at rat mGluR6 by measuring cAMP formation in CHO cells Activity at rat mGluR6 by measuring cAMP formation in CHO cells	[PMID: 16213710]
HEK293	EC₅₀	< 100 μM Compound: 2 (L-AP4)	Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active	[PMID: 15801843]
HEK293	EC₅₀	0.03 μM Compound: L-AP4	Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	[PMID: 25958247]
HEK293	EC₅₀	0.03 μM Compound: L-AP4	Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	[PMID: 26814576]
HEK293	EC₅₀	0.07 μM Compound: L-AP4	Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	[PMID: 26814576]
HEK293	EC₅₀	0.096 μM Compound: L-AP4	Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting	[PMID: 20218620]
HEK293	EC₅₀	0.11 μM Compound: L-AP4	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	[PMID: 25958247]
HEK293	EC₅₀	0.13 μM Compound: L-AP4	Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader	[PMID: 20218620]
HEK293	EC₅₀	0.13 μM Compound: 2, L-AP4	Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry	[PMID: 22750138]
HEK293	EC₅₀	0.24 μM Compound: L-AP4	Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting	[PMID: 20218620]
HEK293	EC₅₀	0.3 μM Compound: L-AP4	Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader	[PMID: 20218620]
HEK293	EC₅₀	0.32 μM Compound: 2 (L-AP4)	Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells	[PMID: 15801843]
HEK293	EC₅₀	1 μM Compound: L-AP4	Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader	[PMID: 20218620]
HEK293	EC₅₀	1.91 μM Compound: L-AP4	Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	[PMID: 26814576]
HEK293	EC₅₀	249 μM Compound: L-AP4	Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader	[PMID: 20218620]
HEK293	EC₅₀	3.3 μM Compound: L-AP4	Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting	[PMID: 20218620]
HEK293	EC₅₀	3.45 μM Compound: L-AP4	Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	[PMID: 25958247]
HEK293	EC₅₀	306 μM Compound: L-AP4	Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting	[PMID: 20218620]
HEK293	EC₅₀	340 μM Compound: L-AP4	Agonist activity at rat mGlu7 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay Agonist activity at rat mGlu7 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	[PMID: 26814576]
HEK293	EC₅₀	426.4 μM Compound: L-AP4	Agonist activity at rat mGluR7 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay Agonist activity at rat mGluR7 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	[PMID: 25958247]
Pyramidal neuron	IC₅₀	0.26 μM Compound: L-AP4	sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4,L-AP5 and L-AP6 after exposure to quisqualic acid sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4,L-AP5 and L-AP6 after exposure to quisqualic acid	[PMID: 7966155]
Pyramidal neuron	IC₅₀	1.5 μM Compound: L-AP4	sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4, L-AP5 and L-AP6 before exposure to quisqualic acid sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4, L-AP5 and L-AP6 before exposure to quisqualic acid	[PMID: 7966155]
Pyramidal neuron	IC₅₀	1.7 μM Compound: L-AP4	sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4, L-AP5 and L-AP6 after reversal with L-alpha-AA sensitization of CA1 pyramidal neurons by 2 to depolarizations by L-AP4, L-AP5 and L-AP6 after reversal with L-alpha-AA	[PMID: 7966155]

In Vivo

L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunction^[2].
Intrathecal injection of 30 μg of L-AP4 does not significantly alter the paw withdrawal latency in these normal rats^[2].
Topical application of 5 to 50 μM L-AP4 to the spinal cord significantly inhibited the evoked response of neurons to touch, pressure, pinch, and von Frey filaments in a concentration-dependent fashion^[2].

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

Animal Model:	Rats.^[2]
Dosage:	5-30 μg.
Administration:	Intrathecal inhection 4-5 days.
Result:	Dose-dependently increased paw withdrawal threshold.

Molecular Weight

183.10

Formula

C₄H₁₀NO₅P

CAS No.

23052-81-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@@H](N)CCP(O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (273.07 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.4615 mL	27.3075 mL	54.6150 mL
5 mM	1.0923 mL	5.4615 mL	10.9230 mL
10 mM	0.5461 mL	2.7307 mL	5.4615 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. 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.

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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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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: 99.01%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) Elemental Analysis Report (104 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O	1 mM	5.4615 mL	27.3075 mL	54.6150 mL	136.5374 mL
	5 mM	1.0923 mL	5.4615 mL	10.9230 mL	27.3075 mL
	10 mM	0.5461 mL	2.7307 mL	5.4615 mL	13.6537 mL
	15 mM	0.3641 mL	1.8205 mL	3.6410 mL	9.1025 mL
	20 mM	0.2731 mL	1.3654 mL	2.7307 mL	6.8269 mL
	25 mM	0.2185 mL	1.0923 mL	2.1846 mL	5.4615 mL
	30 mM	0.1820 mL	0.9102 mL	1.8205 mL	4.5512 mL
	40 mM	0.1365 mL	0.6827 mL	1.3654 mL	3.4134 mL
	50 mM	0.1092 mL	0.5461 mL	1.0923 mL	2.7307 mL
	60 mM	0.0910 mL	0.4551 mL	0.9102 mL	2.2756 mL
	80 mM	0.0683 mL	0.3413 mL	0.6827 mL	1.7067 mL
	100 mM	0.0546 mL	0.2731 mL	0.5461 mL	1.3654 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.

L-AP4 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:

L-AP423052-81-5L-APBmGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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