L-AP4 (Synonyms: L-APB)

目錄號: HY-100781A 純度: 99.01%: FAQs
Data Sheet SDS COA 產品使用指南技術支持

L-AP4 (L-APB) 是一種有效的、代謝型谷氨酸受體 (mGluR) 的特異性激動劑，其對 mGlu₄, mGlu₈, mGlu₆ 和 mGlu₇ 受體的 EC₅₀ 值分別為 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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規(guī)格	價格	是否有貨
10 mM * 1 mL in Water	￥3245	In-stock
5 mg	￥2950	In-stock
10 mg	￥5000	In-stock
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100 mg		詢價

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Customer Review

Other Forms of L-AP4:

D-AP4 詢價
L-AP4 monohydrate 詢價

MCE 顧客使用本產品發(fā)表的 1 篇科研文獻

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

L-AP4 相關產品

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

生物活性
純度 & 產品資料
參考文獻

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)

細胞效力
(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]

體內研究
(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 號

23052-81-5

性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數據

細胞實驗：

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

配制儲備液

濃度溶劑體積質量	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

查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

摩爾計算器
稀釋計算器

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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數量

只

由于實驗過程有損耗，建議您多配一只動物的量

計算結果

工作液所需濃度 : mg/mL

該產品水溶性佳，請具體參考實測水 / PBS / Saline 中的溶解度數據。

您所需的儲備液濃度超過該產品的實測溶解度，如有需要，請與 MCE 中國技術支持聯系。

純度 & 產品資料

純度: 99.01%

選擇批次：

Data Sheet (601 KB) SDS (251 KB)

COA (282 KB)

產品使用指南 (1538 KB)

參考文獻

[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 相關分類

Neurological Disease

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	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

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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 顧客使用本產品發(fā)表的 1 篇科研文獻