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KAG-308

Catalog No. T15642 CAS 1215192-68-9

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing, which potently inhibits TNF-α production.

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KAG-308, CAS 1215192-68-9

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100 mg	10-14 weeks	Inquiry

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing, which potently inhibits TNF-α production.
Targets&IC50	EP1 receptor (human):1410 nM（ki）, EP4 receptor (human):(EC50)17 nM, EP4 receptor (human):（ki）2.57 nM, EP3 receptor (human):160 nM(EC50), EP3 receptor (human):32.4 nM（ki）, EP2 receptor (human):1000 nM(EC50), EP2 receptor (human):1540 nM（ki）, IP receptor (human):52.9 nM（ki）
In vitro	KAG-308 shows effective agonist activity for human and mouse EP4 (EC50: 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay). KAG-308 shows a Ki and EC50 values of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over human EP1 (Ki, 1410 nM; EC50, 1000 nM), EP2 (Ki, 1540 nM; EC50, 1000 nM), EP3 (Ki, 32.4 nM; EC50, 160 nM) and IP receptor (Ki, 52.9 nM; EC50, >10000 nM) [1].

Molecular Weight	460.52
Formula	C24H30F2N4O3
CAS No.	1215192-68-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Watanabe Y, et al. KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration. Eur J Pharmacol. 2015 May 5;754:179-89.

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Keywords

KAG-308 1215192-68-9 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor KAG308 KAG 308 inhibitor inhibit

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