AM966 MedChemExpress (MCE)

Product Name	AM966
Synonyms	AM966 AM 966 AM-966 CS-2784 {4'-[4-({[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]-4-biphenylyl}acetic acid 4'-[4-[[[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]-[1,1'-biphenyl]-4-acetic acid Synonyms AM966 AM 966 AM-966 CS-2784 {4'-[4-({[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]-4-biphenylyl}acetic acid 4'-[4-[[[(1R)-1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]-[1,1'-biphenyl]-4-acetic acid [1,1'-BIPHENYL]-4-ACETIC ACID, 4'-[4-[[[(1R)-1-(2-CHLOROPHENYL)ETHOXY]CARBONYL]AMINO]-3-METHYL-5-ISOXAZOLYL]- (R)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)aMino)-3-Methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid
CAS	1228690-19-4
EINECS
Chemical Formula	C27H23ClN2O5
Molecular Weight	490.93
inchi
Package	10 mM * 1 mL;2 mg;5 mg;10 mg;50 mg;100 mg
Price	Email to quote
Descriptions	AM966 AM966 MedChemExpress (MCE) HY-15277 1228690-19-4 99.86% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions AM966 AM966 MedChemExpress (MCE) HY-15277 1228690-19-4 99.86% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM). 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 LPA2-5, 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]. 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]. Mice[1] The oral exposure of AM966 is determined in fasted mice. Animals received AM966 (10 mg/kg) in vehicle (water) by oral gavage and are then killed by CO2 inhalation at 1, 2, 4, 8 and 24 h post dose (n=2 animals per time point for each test compound). Blood (approximately 300 µL) is collected via cardiac puncture into EDTA-containing tubes and centrifuged at 1450×g for 10 min. The plasma is removed and analysed for AM966 content by liquid chromatography-mass spectrometry (LCMS). Briefly, known amounts of AM966 are added to thawed mouse plasma to yield a concentration range from 0.8 to 4000 ng/mL. Mouse plasma samples are precipitated using acetonitrile (1:4, v:v) containing the internal standard buspirone. A 10 µL aliquot of the analyte mixture is injected using a Leap PAL autosampler. Analyses are performed using an Agilent Zorbax SB-C8 column (2.1×50 mm 5 µm) linked to a Shimadzu LC-10AD VP with SCL-10A VP system controller. Tandem mass spectrometric detection is carried out on a PE Sciex API3200 in the positive ion mode (ESI) by multiple reaction monitoring. The calibration curves are constructed by plotting the peak-area ratio of analysed peaks against known concentrations. The lower limit of quantitation is 0.8 ng/mL. The data are subjected to linear regression analysis with 1/x2weighting. CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate[2]. LPA1[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

MedChemExpress (MCE) also provides

Thalidomide-4-O-C2-NH2

Category: Signaling Pathways
CAS: 2341840-99-9
Last Update: 2025-04-01 14:45:47

PPARα-MO-1

Category: Signaling Pathways
CAS: 810677-36-2
Last Update: 2025-04-01 14:45:47

Netupitant N-oxide

Category: Signaling Pathways
CAS: 910808-11-6
Last Update: 2025-04-01 14:45:47

MK-0812

Category: Signaling Pathways
CAS: 624733-88-6
Last Update: 2025-04-01 14:45:47

TS-011

Category: Signaling Pathways
CAS: 339071-18-0
Last Update: 2025-04-01 14:45:47

SCH 530348 sulfate

Category: Signaling Pathways
CAS: 705260-08-8
Last Update: 2025-04-01 14:45:47

BAG 956

Category: Signaling Pathways
CAS: 853910-02-8
Last Update: 2025-04-01 14:45:47

YM758

Category: Signaling Pathways
CAS: 312752-85-5
Last Update: 2025-04-01 14:45:47


Supplier Name	MedChemExpress (MCE)
Contact	sales
Tel	609-228-6898
Mobile	609-228-6898
QQ
Email	sales@medchemexpress.com; tech@medchemexpress.com
Website	https://www.medchemexpress.com/
Wechat

Request for quotation

Supplier Contact