L-AP4 (Synonyms: L-APB)

目录号: HY-100781A 纯度: 99.01%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

L-AP4 (L-APB) 是一种有效的、代谢型谷氨酸受体 (mGluR) 的特异性激动剂，其对 mGlu₄, mGlu₈, mGlu₆ 和 mGlu₇ 受体的 EC₅₀ 值分别为 0.13, 0.29, 1.0, 249 μM。

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L-AP4 Chemical Structure

CAS No. : 23052-81-5

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规格	价格	是否有货
10 mM * 1 mL in Water	￥3245	In-stock
5 mg	￥2950	In-stock
10 mg	￥5000	In-stock
50 mg		询价
100 mg		询价

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Customer Review

Other Forms of L-AP4:

D-AP4 询价
L-AP4 monohydrate 询价

MCE 顾客使用本产品发表的 1 篇科研文献

•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

生物活性
纯度 & 产品资料
参考文献

生物活性

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

mGlu₄

0.13 μM (EC₅₀)

mGlu8

0.29 μM (EC₅₀)

mGlu₆

1.0 μM (EC₅₀)

mGlu7

249 μM (EC₅₀)

细胞效力
(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]

体内研究
(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].

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.

分子量

183.10

Formula

C₄H₁₀NO₅P

CAS 号

23052-81-5

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

H₂O 中的溶解度 : 50 mg/mL (273.07 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.01%

选择批次：

Data Sheet (601 KB) SDS (251 KB)

COA (282 KB) 元素分析报告 (207 KB)

产品使用指南 (1538 KB)

参考文献

[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]

L-AP4 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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L-AP4 (Synonyms: L-APB)

Customer Review

Other Forms of L-AP4:

MCE 顾客使用本产品发表的 1 篇科研文献

L-AP4 相关产品

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参考文献

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L-AP4 相关分类

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L-AP4 (Synonyms: L-APB)

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L-AP4 相关抗体

MCE 顾客使用本产品发表的 1 篇科研文献

L-AP4 相关产品

•同靶点产品:

•同靶点蛋白产品:

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生物活性

纯度 & 产品资料

参考文献

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L-AP4 相关分类

完整储备液配制表

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