MedKoo Cat#: 555556 | Name: KAG-308

Description:

WARNING: This product is for research use only, not for human or veterinary use.

KAG-308 is an orally active, selective EP4 (prostaglandin E2 receptor subtype 4) agonist with demonstrated anti-inflammatory and anti-fibrotic properties. In preclinical models, KAG-308 showed potent EP4 agonistic activity with an EC₅₀ of 1.9 nM in cAMP accumulation assays using EP4-expressing cells. In mouse models of pulmonary fibrosis, oral administration of KAG-308 at 1–3 mg/kg significantly reduced lung fibrosis markers, including hydroxyproline content and TGF-β1 expression. Additionally, in collagen-induced arthritis models, KAG-308 treatment reduced joint swelling and inflammatory cytokine production, with efficacy comparable to or better than standard anti-inflammatory agents. These data support KAG-308 as a promising therapeutic candidate for inflammatory and fibrotic diseases.

Chemical Structure

KAG-308
KAG-308
CAS#1215192-68-9

Theoretical Analysis

MedKoo Cat#: 555556

Name: KAG-308

CAS#: 1215192-68-9

Chemical Formula: C24H30F2N4O3

Exact Mass: 460.2286

Molecular Weight: 460.53

Elemental Analysis: C, 62.59; H, 6.57; F, 8.25; N, 12.17; O, 10.42

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
KAG-308; KAG 308; KAG308;
IUPAC/Chemical Name
4-[(Z)-(1S,5R,6R,7R)-6-[(1E,3R,4R)-3-Hydroxy-4-(m-tolyl)-1-pentenyl]-7-hydroxy-4,4-difluoro-2-oxabicyclo[3.3.0]octan-3-ylidene]-1-(tetrazol-5-yl)butane
InChi Key
KSELABKNBIUMGG-YGBAREPYSA-N
InChi Code
InChI=1S/C24H30F2N4O3/c1-14-6-5-7-16(12-14)15(2)18(31)11-10-17-19(32)13-20-23(17)24(25,26)21(33-20)8-3-4-9-22-27-29-30-28-22/h5-8,10-12,15,17-20,23,31-32H,3-4,9,13H2,1-2H3,(H,27,28,29,30)/b11-10+,21-8-/t15-,17+,18-,19-,20+,23-/m1/s1
SMILES Code
FC1(F)/C(O[C@@]2([H])C[C@@H](O)[C@H](/C=C/[C@@H](O)[C@@H](C3=CC=CC(C)=C3)C)[C@@]12[H])=C/CCCC4=NN=NN4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Agonists for EP4 receptor, a prostaglandin E2 receptor subtype, appear to be a promising therapeutic strategy for ulcerative colitis (UC) due to their anti-inflammatory and epithelial regeneration activities.

Preparing Stock Solutions

The following data is based on the product molecular weight 460.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Nishimura R, Shirasaki T, Tsuchiya K, Miyake Y, Watanabe Y, Hibiya S, Watanabe S, Nakamura T, Watanabe M. Establishment of a system to evaluate the therapeutic effect and the dynamics of an investigational drug on ulcerative colitis using human colonic organoids. J Gastroenterol. 2019 Jan 1. doi: 10.1007/s00535-018-01540-y. [Epub ahead of print] PubMed PMID: 30599053. 2: Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T. Ligand binding to human prostaglandin E receptor EP(4) at the lipid-bilayer interface. Nat Chem Biol. 2019 Jan;15(1):18-26. doi: 10.1038/s41589-018-0131-3. Epub 2018 Dec 3. PubMed PMID: 30510193. 3: Watanabe Y, Murata T, Amakawa M, Miyake Y, Handa T, Konishi K, Matsumura Y, Tanaka T, Takeuchi K. 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. doi: 10.1016/j.ejphar.2015.02.021. Epub 2015 Feb 19. PubMed PMID: 25704618.