| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO|58.27|100| | [form ]
Solid | [color ]
White to off-white | [InChIKey]
MBPXGBINIINSEU-UHFFFAOYSA-N | [SMILES]
O=C(O)CCC1=CC2=C(N(C3=CC=C(OC4=CC=CC=C4)C=C3)C=C2CCC5=CC=CC=C5)C=C1.NC(CO)(CO)CO |
| Hazard Information | Back Directory | [Description]
ASB14780 is a potent inhibitor of cPLA2α. | [Uses]
ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM[1]. | [in vivo]
TPA (tetradecanoyl phorbol acetate) causes acute inflammation with ear, resulting in edema[1].
ASB14780 (50 mg/kg; p.o.; once) suppresses the increase in the ear thickness elicited by the application of TPA (tetradecanoyl phorbol acetate) in mouse[1].
ASB14780 (5 mg/kg; 20 mg/kg; p.o.; once daily) attenuates AHR (airway hyperreactivity), and inhibits IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner[1].
ASB14780 shows well oral activity of 89.6% in mouse calculated from the ratio of oral administration’s AUC (10 mg/kg; p.o.) and intravenonous administration’s AUC (1 mg/kg; i.v.)[1].
Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780[1]
| Model | F (%) | AUC (h μg/mL) | Cmax (μg/mL) | | mouse | 89.6 | 7.12 | 5.12 | | dog | 34.3 | 17.1 | 4.96 | | monkey | 30.9 | 4.96 | 2.29 |
Note: Based on 10 mg/kg p.o. dosing data.
| Animal Model: | TPA (Tetradecanoyl Phorbol Acetate)-induced Ear Edema Model in mouse (female C57BL/6 mice)[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; 30 min before TPA stimulation | | Result: | Showed high potency and inhibited ear swelling by 30% and indicated the in vivo anti-inflammatory activity.
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| Animal Model: | Guinea Pig Ovalbumin (OVA)-induced Asthma Model[1] | | Dosage: | 5 mg/kg, 20 mg/kg | | Administration: | Oral gavage; two single doses; 1 h before and 8 h after passively sensitized administration | | Result: | Exhibits suppression on IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.
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| [storage]
Store at -20°C | [References]
[1] Tomoo T, et al. Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors. J Med Chem. 2014. 57(17):7244-62. DOI:10.1021/jm500494y |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|