Referencia número: HY-100781A

L-AP4

(Synonyms: L-APB)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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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Pureza: 99.01%
No. CAS: 23052-81-5
Fòrmula: C₄H₁₀NO₅P
Peso molecular:183.10

Almacenamiento:

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

L-AP4 Chemical Structure

No. CAS: 23052-81-5

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas mGluR :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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: 3, L-AP4	Activity at rat recombinant mGluR5 expressed in CHO cells assessed as intracellular calcium concentration Activity at rat recombinant mGluR5 expressed in CHO cells assessed as intracellular calcium concentration	[PMID: 17350267]
CHO	EC₅₀	0.34 μM Compound: 3, L-AP4	Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production	[PMID: 17350267]
CHO	EC₅₀	>1000 μM Compound: 3, L-AP4	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	[PMID: 17350267]
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	0.32 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	0.56 μM Compound: L-AP4	Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production	[PMID: 17602546]
HEK293	EC₅₀	0.69 μM Compound: L-AP4	Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production	[PMID: 17602546]
HEK293	EC₅₀	0.08 μM Compound: 1, L-AP4	Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	[PMID: 17722902]
HEK293	EC₅₀	0.128 μM Compound: 1, L-AP4	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	[PMID: 17722902]
HEK293	EC₅₀	2.08 μM Compound: 1, L-AP4	Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	[PMID: 17722902]
HEK293	EC₅₀	440 μM Compound: 1, L-AP4	Agonist activity at rat mGluR7 receptor expressed HEK293 cells assessed as effect on inositol phosphate production Agonist activity at rat mGluR7 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	[PMID: 17722902]
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	0.13 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	0.24 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	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	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	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	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	0.03 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	0.11 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	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	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]
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	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	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]
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.

Chemical Information

No. CAS 23052-81-5
Appearance Solid
Peso molecular 183.10
Fòrmula C₄H₁₀NO₅P
Color White to off-white
SMILES

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

L-APB
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (1)

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Biochem Biophys Res Commun

Identification of 2-PMPA as a novel inhibitor of cytosolic carboxypeptidases. [Abstract]

2020 Dec 17;533(4):1393-1399. PMID: 33092792

Solvente y solubilidad

In Vitro:

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

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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.

Keywords

L-AP4

1 Cited Publications

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L-AP4

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) L-AP4

Ver todos los productos específicos de isoformas mGluR

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

L-AP4

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) L-AP4

Ver todos los productos específicos de isoformas mGluR

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

L-AP4 Related Classifications

HY-100781A Related Classifications