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1215192-68-9
  • names:

    KAG-308

  • CAS号:

    1215192-68-9

    MDL Number:
  • MF(分子式): C24H30F2N4O3 MW(分子量): 460.52
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
KAG-308

KAG-308(1215192-68-9)一种新型确定的EP4选择性激动剂,选择性激动剂,显示出治疗溃疡性结肠炎的功效可通过口服,并可以降低结直肠癌发生的风险,KAG-308是EP4 receptor (一种前列腺素E2受体亚型) 激动剂,可以抑制结肠炎,促进组织粘膜愈合,有效抑制 TNF-α 的产生。KAG-308 对人EP4受体的Ki值和 EC50值分别为2.57nM和17 nM,对其选择性高于EP1,EP2,EP3 和 IP 受体。KAG-308 is a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis, KAG-308 can bring about lower risk of colorectal carcinogenesis by oral administration.

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中文别名 KAG-308(cas:1215192-68-9)
英文别名 KAG-308,1215192-68-9,KAG 308,KAG308
CAS号 1215192-68-9
SMILES O[C@H](C1)[C@H](/C=C/[C@@H](O)[C@@H](C2=CC=CC(C)=C2)C)[C@](C/3(F)F)([H])[C@@]1([H])OC3=C/CCCC4=NN=NN4
Inchi 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
InchiKey KSELABKNBIUMGG-YGBAREPYSA-N
分子式 Formula C24H30F2N4O3
分子量 Molecular Weight 460.52
闪点 FP No data available
熔点 Melting point No data available
沸点 Boiling point No data available
Polarizability极化度
密度 Density No data available
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid power
储藏条件 Storage conditions 请根据产品建议的存储条件进行存储,Please store the product under the recommended condition sin the description.
KAG-308(CAS:1215192-68-9)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
产品说明 KAG-308(1215192-68-9)是EP4 receptor(一种前列腺素 E2 受体亚型) 激动剂,KAG-308详细参数见主页
IntroductionKAG08(1215192-68-9) is a potent selective and orally active agonist of EP4 receptor
Application1
Application2
Application3
KAG-308(1215192-68-9) 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. However, the clinical development of orally-available EP4 agonists for mild to moderate UC has not yet been reported. Furthermore, the possibility of an increased risk of colitis-associated cancer (CAC) through direct proliferative effects on epithelial cells via EP4 signaling has not been ruled out. Recently, we identified KAG-308 as an orally-available EP4-selective agonist. Here, we investigated the pharmacological and pharmacokinetic profiles of KAG-308. Then, we compared KAG-308 and sulfasalazine (SASP) for their abilities to prevent colitis and promote mucosal healing in a mouse model of dextran sulfate sodium (DSS)-induced colitis. Finally, the effect of KAG-308 treatment on CAC was evaluated in an azoxymethane (AOM)/DSS-induced CAC mouse model. KAG-308 selectively activated EP4 and potently inhibited tumor necrosis factor-α production in peripheral whole blood and T cells. Oral administration of KAG-308, which showed relatively high bioavailability, suppressed the onset of DSS-induced colitis and promoted histological mucosal healing, while SASP did not. KAG-308 also prevented colorectal carcinogenesis by inhibiting colitis development and consequently decreasing mortality in a CAC model, whereas SASP had marginal effects. In contrast, MF-482, an EP4 antagonist, increased mortality. These results indicated that orally-administered KAG-308 suppressed colitis development and promoted mucosal healing. Moreover, it exhibited preventive effects on colorectal carcinogenesis, and thus may be a new therapeutic strategy for the management of UC that confers a reduced risk of colorectal carcinogenesis.

1: Nishimura R, Shirasaki T, Tsuchiya K, Miyake Y, Watanabe Y, Hibiya S, WatanabeS, 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, HosoyaT, 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.

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