1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. KAG-308

KAG-308 

Cat. No.: HY-128686
Handling Instructions

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.

For research use only. We do not sell to patients.

KAG-308 Chemical Structure

KAG-308 Chemical Structure

CAS No. : 1215192-68-9

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Description

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].

IC50 & Target

EC50: 17 nM (Human EP4 receptor), 160 nM (Human EP3 receptor), 1000 nM (Human EP2 receptor), 1000 nM (Human EP2 receptor)[1]
Ki: 2.57 nM (Human EP4 receptor), 32.4 nM (Human EP3 receptor), 52.9 nM (Human IP receptor), 1410 nM (Human EP1 receptor), 1540 nM (Human EP2 receptor)[1]

In Vitro

KAG-308 is a potent selective and orally active agonist of EP4 receptor, suppresses colitis and promots histological mucosal healing. 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). KAG-308 also exhibits potent agonist activity for human and mouse EP4 with an EC50 of 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay[1].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

460.52

Formula

C₂₄H₃₀F₂N₄O₃

CAS No.

1215192-68-9

SMILES

O[[email protected]](C1)[[email protected]](/C=C/[[email protected]@H](O)[[email protected]@H](C2=CC=CC(C)=C2)C)[[email protected]](C/3(F)F)([H])[[email protected]@]1([H])OC3=C/CCCC4=NN=NN4

Shipping

Room temperature in continental US; may vary elsewhere

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KAG-308
Cat. No.:
HY-128686
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KAG-308

Cat. No.: HY-128686