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KAG-308

Cat. No. M10842
KAG-308 Structure
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Biological Activity

KAG-308 is an effective, selective, orallyable EP4 receptor (a subtype of prostaglandin E2 receptor) agonist that inhibits colitis, promotes tissue mucosal healing, and effectively inhibits the production of TNF-α. KAG-308 for human EP4 receptors Ki value and EC50 The values were 2.57 nM and 17 nM, respectively, which were more selective than EP1, EP2, EP3, and IP receptors.

Chemical Information
Molecular Weight 460.52
Formula C24H30F2N4O3
CAS Number 1215192-68-9
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yasutaka Murahashi, et al. Sci Rep. Oral administration of EP4-selective agonist KAG-308 suppresses mouse knee osteoarthritis development through reduction of chondrocyte hypertrophy and TNF secretion

[2] Ryu Nishimura, et al. J Gastroenterol. Establishment of a system to evaluate the therapeutic effect and the dynamics of an investigational drug on ulcerative colitis using human colonic organoids

[3] Yosuke Toyoda, et al. Nat Chem Biol. Ligand binding to human prostaglandin E receptor EP 4 at the lipid-bilayer interface

[4] Yusuke Watanabe, et al. Eur J Pharmacol. 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

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Keywords: KAG-308 supplier, Prostaglandin Receptor, inhibitors, activators

 
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