Art. -Nr.: HY-15277

AM966

Name: AM966
Brand: MedChemExpress
SKU: HY-15277
Price: 70.00 USD
Availability: InStock
Rating: 5 (20 reviews)

20 Cited Publications

Kundenbewertung

Based on 20 publication(s) in Google Scholar

AM966 is a high affinity, selective, oral LPA₁-antagonist, inhibits LPA-stimulated intracellular calcium release (IC₅₀=17 nM).

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Reinheit : 98.91%
CAS. Nr.: 1228690-19-4
Formel: C₂₇H₂₃ClN₂O₅
Molecular Weight:490.93

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AM966 Chemical Structure

CAS. Nr.: 1228690-19-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (3)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AM966 is a high affinity, selective, oral LPA₁-antagonist, inhibits LPA-stimulated intracellular calcium release (IC₅₀=17 nM).

IC₅₀ & Target

LPA₁^[1]

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1600 nM Compound: 29	Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis	10.1039/C4MD00333K
CHO	IC₅₀	17 nM Compound: 29	Antagonist activity at human LPA1 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis Antagonist activity at human LPA1 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis	10.1039/C4MD00333K
CHO	IC₅₀	1700 nM Compound: 29	Antagonist activity at human LPA2 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis Antagonist activity at human LPA2 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis	10.1039/C4MD00333K

In Vitro

AM966 is a potent, selective, orally bioavailable LPA₁ receptor antagonist. AM966 inhibits LPA₁-mediated chemotaxis of human A2058 melanoma cells (IC₅₀=138±43 nM), IMR-90 human lung fibroblasts (IC₅₀=182±86 nM) and CHO mLPA₁ cells (IC₅₀=469±54 nM)^[1]. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA₁ over LPA_2-5, with an IC₅₀ value of 3.8±0.4 nM. Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by Mianserin^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation in a 3 day Bleomycin (HY-108345) model. AM966 inhibits lung fibrosis, maintains mouse body weight and decreases lung inflammation 14 days after Bleomycin lung injury. AM966 reduces vascular leakage, tissue injury and pro-fibrotic cytokine production in the 14 day Bleomycin study. AM966 demonstrates greater efficacy compared to Pirfenidone (HY-B0673) in the 14 day Bleomycin model. AM966 decreases mortality and fibrosis at late time points after Bleomycin injury^[1].

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

Chemical Information

CAS. Nr. 1228690-19-4
Appearance Solid
Molecular Weight 490.93
Formel C₂₇H₂₃ClN₂O₅
Color White to off-white
SMILES

O=C(O)CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4Cl)C)=O)C(C)=NO3)C=C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (20)

All WB

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Journal Impact Factor

Cell Metab

Secreted phospholipase A2 modifies extracellular vesicles and accelerates B cell lymphoma. [Abstract]

2022 Apr 5;34(4):615-633.e8. PMID: 35294862
Autophagy

A defective lysophosphatidic acid-autophagy axis increases miscarriage risk by restricting decidual macrophage residence. [Abstract]

2022 Oct;18(10):2459-2480. PMID: 35220880
Cell Commun Signal

LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration. [Abstract]

2023 Sep 25;21(1):257. PMID: 37749552
Apoptosis

Inhibition of TNF-α-induced neuronal apoptosis by antidepressants acting through the lysophosphatidic acid receptor LPA1. [Abstract]

2019 Jun;24(5-6):478-498. PMID: 30840161
Neuropsychopharmacol Rep

Antidepressant amitriptyline-induced matrix metalloproteinase-9 activation is mediated by Src family tyrosine kinase, which leads to glial cell line-derived neurotrophic factor mRNA expression in rat astroglial cells. [Abstract]

2019 Sep;39(3):156-163. PMID: 31025529
Biochem Pharmacol

Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts. [Abstract]

2015 Jun 15;95(4):311-23. PMID: 25888927

AM966 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2015 Jun 15;95(4):311-23. [Abstract]

CHO-K1 cells express LPA₁ receptors coupled to ERK1/2 phosphorylation. Inhibition of LPA-induced phospho-ERK1/2 by AM966. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 30 min and then treated with LPA (300 nM) for 15 min. Values are expressed as percent of p-ERK stimulation elicited by LPA in the absence of antagonist and are the mean ± SEM of three experiments.
Eur J Pharmacol

Downregulation of connexin 43 potentiates amitriptyline-induced brain-derived neurotrophic factor expression in primary astrocytes through lysophosphatidic acid receptor1/3, Src, and extracellular signal-regulated kinase. [Abstract]

2022 Jun 15;925:174986. PMID: 35490723
Eur J Pharmacol

Antidepressants induce profibrotic responses via the lysophosphatidic acid receptor LPA1. [Abstract]

2020 Apr 15:873:172963. PMID: 32007501
Eur J Pharmacol

Mirtazapine increases glial cell line-derived neurotrophic factor production through lysophosphatidic acid 1 receptor-mediated extracellular signal-regulated kinase signaling in astrocytes. [Abstract]

2019 Oct 5:860:172539. PMID: 31306636
J Lipid Res

EBV promotes alveolar trabecula resorption via extracellular vesicle remodeling by group IIA secreted phospholipase A2. [Abstract]

2026 Mar 3;67(4):101014. PMID: 41786250
J Neurochem

Lysophosphatidic acid induces thrombospondin-1 production in primary cultured rat cortical astrocytes. [Abstract]

2021 Aug;158(4):849-864. PMID: 33118159
J Pharmacol Exp Ther

LPA1 Mediates Antidepressant-Induced ERK1/2 Signaling and Protection from Oxidative Stress in Glial Cells. [Abstract]

2016 Nov;359(2):340-353. PMID: 27605627

AM966 purchased from MedChemExpress. Usage Cited in: J Pharmacol Exp Ther. 2016 Nov;359(2):340-353. [Abstract]

Concentration-dependent effects of LPA receptor antagonists on antidepressant- and LPA-induced ERK1/2 phosphorylation in C6 glioma cells. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 10 min and then exposed to either vehicle or 1 μM LPA (A), 15 μM Amitriptyline (C) or 5 μM Mianserin (E) for 10 min.
J Pharmacol Exp Ther

Positive and Negative Cross-Talk between Lysophosphatidic Acid Receptor 1, Free Fatty Acid Receptor 4, and Epidermal Growth Factor Receptor in Human Prostate Cancer Cells. [Abstract]

2016 Oct;359(1):124-33. PMID: 27474750
J Biol Chem

Identification of Lysophosphatidic Acid Receptor 1 in Astroglial Cells as a Target for Glial Cell Line-derived Neurotrophic Factor Expression Induced by Antidepressants. [Abstract]

2016 Dec 30;291(53):27364-27370. PMID: 27864362

AM966 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2016 Dec 30;291(53):27364-27370. [Abstract]

Effect of LPAR antagonists on ERK1/2 phosphorylation and FRS2 phosphorylation evoked by either amitriptyline (A) or LPA (B).
Cell Mol Bioeng

Lysophosphatidic Acid (LPA) Receptor Signaling Promotes the Adaptation of Malignant Cellular Functions in Highly Migratory Osteosarcoma Cells Under Hypoxic and Low-Glucose Conditions. [Abstract]

2025 Oct 13;18(6):577-588. PMID: 41328303
J Clin Med

Eicosopentaneoic Acid and Other Free Fatty Acid Receptor Agonists Inhibit Lysophosphatidic Acid- and Epidermal Growth Factor-Induced Proliferation of Human Breast Cancer Cells. [Abstract]

2016 Jan 26;5(2):16. PMID: 26821052
Acta Histochem

Lysophosphatidic acid (LPA) receptor signaling enhances malignant potential in highly migratory lung cancer cells under hypoxic conditions. [Abstract]

2025 May 23;127(3):152268. PMID: 40412000
The Ohio State University

2025.
Seoul National University

2024 Feb.
Washington State University

2015 May.

AM966 purchased from MedChemExpress. Usage Cited in: Washington State University. 2015 May.

Effects of LPAR antagonists on growth factor-induced phosphorylation of ERK in DU145 cells. Serum starved DU145 cells are incubated with 10 μM LPA, with or without either 100 nM AM966 or 10 μM Ki16425 for 10 minutes. Whole-cell extracts, equalized for protein, are immunoblotted for phospho-ERK (pERK) and for actin (loading control).

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (203.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.0370 mL

10.1848 mL

20.3695 mL

5 mM

0.4074 mL

2.0370 mL

4.0739 mL

10 mM

0.2037 mL

1.0185 mL

2.0370 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (20.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

All Cell Biology Signal Pathway Related

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca²⁺]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca²⁺ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
Ca²⁺ Staining Technique
Ca²⁺ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca²⁺ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

Verweise

[1]. Swaney, JS, et al. A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol. 2010 Aug;160(7):1699-713. [Content Brief]

[2]. Olianas MC, et al. Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts. Biochem Pharmacol. 2015 Jun 15;95(4):311-23. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0370 mL	10.1848 mL	20.3695 mL	50.9238 mL
	5 mM	0.4074 mL	2.0370 mL	4.0739 mL	10.1848 mL
	10 mM	0.2037 mL	1.0185 mL	2.0370 mL	5.0924 mL
	15 mM	0.1358 mL	0.6790 mL	1.3580 mL	3.3949 mL
	20 mM	0.1018 mL	0.5092 mL	1.0185 mL	2.5462 mL
	25 mM	0.0815 mL	0.4074 mL	0.8148 mL	2.0370 mL
	30 mM	0.0679 mL	0.3395 mL	0.6790 mL	1.6975 mL
	40 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2731 mL
	50 mM	0.0407 mL	0.2037 mL	0.4074 mL	1.0185 mL
	60 mM	0.0339 mL	0.1697 mL	0.3395 mL	0.8487 mL
	80 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6365 mL
	100 mM	0.0204 mL	0.1018 mL	0.2037 mL	0.5092 mL

Bioz

Keywords

AM966

20 Cited Publications

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AM966

Publications Citing Use of MedChemExpress (MCE) AM966

Alle LPL Receptor Isoform-spezifische Produkte anzeigen