167838-64-4
Chemical Structure
FR173657
Synonym(s): FK-3657
- CAS No.: 167838-64-4
- Formula:C30H27Cl2N5O4
- Molecular Weight:592.47
IUPAC Name: (E)-3-(6-acetamidopyridin-3-yl)-N-(2-((2,4-dichloro-3-(((2-methylquinolin-8-yl)oxy)methyl)phenyl)(methyl)amino)-2-oxoethyl)acrylamide
InChIKey: XCKWRUGRUFVXGC-NTEUORMPSA-N
SMILES: O=C(NCC(N(C1=CC=C(Cl)C(COC2=C3N=C(C)C=CC3=CC=C2)=C1Cl)C)=O)/C=C/C4=CC=C(NC(C)=O)N=C4
Biological Activity: FR173657 (FK-3657) is an orally active, selective bradykinin B2 receptor antagonist. FR173657 induces Apoptosis, G0/G1 phase arrest, and p38 MAPK/p27Kip1 signaling. FR173657 blocks afferent neuron activation, tumor vascular hyperpermeability, tumor angiogenesis/growth, colorectal proliferation, kinin-mediated invasion/migration, and airway plasma extravasation. FR173657 can be used in research on inflammatory pain, asthma, triple-negative breast cancer, psoriasis, pancreatitis, acute cystitis, skin inflammation, sarcoma 180, colorectal liver metastasis, and Carrageenan-induced pleurisy[1][2][3][4][5][6][7][8][9][10].
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FR173657 | 99.00% | FR173657 (FK-3657) is an orally active, selective bradykinin B2 receptor antagonist. FR173657 induces Apoptosis, G0/G1 phase arrest, and p38 MAPK/p27Kip1 signaling. FR173657 blocks afferent neuron activation, tumor vascular hyperpermeability, tumor angiogenesis/growth, colorectal proliferation, kinin-mediated invasion/migration, and airway plasma extravasation. FR173657 can be used in research on inflammatory pain, asthma, triple-negative breast cancer, psoriasis, pancreatitis, acute cystitis, skin inflammation, sarcoma 180, colorectal liver metastasis, and Carrageenan-induced pleurisy. | ||||||||||||||||||||
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References
- [1]. Asano M, et al. The identification of an orally active, nonpeptide bradykinin B2 receptor antagonist, FR173657. British journal of pharmacology. 1997 Feb;120(4):617-24. [Content Brief]
- [2]. Ishihara K, et al. Roles of bradykinin in vascular permeability and angiogenesis in solid tumor. International immunopharmacology. 2002 Mar;2(4):499-509.
- [3]. da Costa PLN, et al. The kallikrein-Kinin system modulates the progression of colorectal liver metastases in a mouse model. BMC cancer. 2018 Apr 04;18(1):382.
- [4]. Griesbacher T, et al. The nonpeptide B2 receptor antagonist FR173657: inhibition of effects of bradykinin related to its role in nociception. British journal of pharmacology. 1998 Jul;124(6):1328-34.
- [5]. Watanabe M, et al. Effects of the orally active non-peptide bradykinin B2 receptor antagonist, FR173657, on plasma extravasation in guinea pig airways. European journal of pharmacology. 1999 Feb 19;367(2-3):373-8.
- [6]. Dubuc C, et al. Targeting intracellular B2 receptors using novel cell-penetrating antagonists to arrest growth and induce apoptosis in human triple-negative breast cancer. Oncotarget. 2018 Feb 09;9(11):9885-9906.
- [7]. Lesage A, et al. In vitro pharmacological profile of a new small molecule bradykinin B2 receptor antagonist. Frontiers in Pharmacology. 2020 Jun 19;11:916. [Content Brief]
- [8]. Soley BDS, et al. B and B kinin receptor blockade improves psoriasis-like disease. British journal of pharmacology. 2020 Aug;177(15):3535-3551.
- [9]. Majima M, et al. Effects of an orally active non-peptide bradykinin B2 receptor antagonist, FR173657, on plasma exudation in rat carrageenin-induced pleurisy. British journal of pharmacology. 1997 Jun;121(4):723-30.
- [10]. Griesbacher T, et al. Effects of the non-peptide B2 receptor antagonist FR173657 in models of visceral and cutaneous inflammation. Inflammation research : official journal of the European Histamine Research Society ... [et al.]. 2000 Oct;49(10):535-40.
