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135070-05-2
  • names:

    4'-((2-cyclopropyl-7-methyl-3H-imidazo[4,5-b]pyridin-3-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid

  • CAS号:

    135070-05-2

    MDL Number:
  • MF(分子式): C24H21N3O2 MW(分子量): 383.451
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
E-4177
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中文别名 E-4177
英文别名 E-4177; E-4177; E4177.
CAS号 135070-05-2
SMILES O=C(C1=CC=CC=C1C2=CC=C(CN3C(C4CC4)=NC5=C(C)C=CN=C53)C=C2)O
Inchi InChI=1S/C24H21N3O2/c1-15-12-13-25-23-21(15)26-22(18-10-11-18)27(23)14-16-6-8-17(9-7-16)19-4-2-3-5-20(19)24(28)29/h2-9,12-13,18H,10-11,14H2,1H3,(H,28,29)
InchiKey VWWMGPCUZVOLLK-UHFFFAOYSA-N
分子式 Formula C24H21N3O2
分子量 Molecular Weight 383.451
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 E-4177(CAS:135070-05-2):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionE-4177 is an angiotensin type 1 receptor antagonist potentially for the treatment of hypertension. In rat adrenal cortex and liver, E4177 competitively inhibited the specific binding of 125I-[Sar1,Ile8]Ang II, with IC50 being (5.2 +/- 1.0) x 10(-8) M for the adrenal cortex and (1.2 +/- 0.3) x 10(-7) M for the liver. These IC50 values were similar to those for losartan, which showed an IC50 of (6.0 +/- 0.9) x 10(-8) M for the adrenal cortex and (1.3 +/- 0.5) x 10(-7) M for the liver. E4177 is a potent AT1 Ang II-receptor antagonist that may be clinically useful for the treatment of cardiovascular diseases such as hypertension.
Application1
Application2
Application3
警示图
危险性 Warning
危险性警示
安全声明
安全防护
备注
[1]Kuma S, Oki E, Onohara T, Komori K, Maehara Y. Angiotensin II-induced growth of vascular smooth muscle cells is associated with modulation of cell surface area and platelet-derived growth factor receptor expression. Clin Exp Pharmacol Physiol. 2007 Mar;34(3):153-60. PubMed PMID: 17250632.
[2]Tanaka M, Umemoto S, Kawahara S, Kubo M, Itoh S, Umeji K, Matsuzaki M. Angiotensin II type 1 receptor antagonist and angiotensin-converting enzyme inhibitor altered the activation of Cu/Zn-containing superoxide dismutase in the heart of stroke-prone spontaneously hypertensive rats. Hypertens Res. 2005 Jan;28(1):67-77. PubMed PMID: 15969257.
[3] Matsuda H, Hayashi K, Arakawa K, Naitoh M, Kubota E, Honda M, Matsumoto A, Suzuki H, Yamamoto T, Kajiya F, Saruta T. Zonal heterogeneity in action of angiotensin-converting enzyme inhibitor on renal microcirculation: role of intrarenal bradykinin. J Am Soc Nephrol. 1999 Nov;10(11):2272-82. PubMed PMID: 10541285.
[4] Matsumoto K, Morishita R, Moriguchi A, Tomita N, Yo Y, Nishii T, Nakamura T, Higaki J, Ogihara T. Prevention of renal damage by angiotensin II blockade, accompanied by increased renal hepatocyte growth factor in experimental hypertensive rats. Hypertension. 1999 Aug;34(2):279-84. PubMed PMID: 10454454.
[5] Uehara Y, Hirawa N, Kawabata Y, Numabe A, Gomi T, Ikeda T, Omata M. Angiotensin II subtype-1 receptor antagonists improve hemodynamic and renal changes without affecting glucose metabolisms in genetic rat model of non-insulin-dependent diabetes mellitus. Am J Hypertens. 1999 Jan;12(1 Pt 1):21-7. PubMed PMID: 10075380.
6: Nakano N, Morishita R, Moriguchi A, Nakamura Y, Hayashi SI, Aoki M, Kida I, Matsumoto K, Nakamura T, Higaki J, Ogihara T. Negative regulation of local hepatocyte growth factor expression by angiotensin II and transforming growth factor-beta in blood vessels: potential role of HGF in cardiovascular disease. Hypertension. 1998 Sep;32(3):444-51. PubMed PMID: 9740609.7: Kim S, Izumi Y, Yano M, Hamaguchi A, Miura K, Yamanaka S, Miyazaki H, Iwao H. Angiotensin blockade inhibits activation of mitogen-activated protein kinases in rat balloon-injured artery. Circulation. 1998 May 5;97(17):1731-7. PubMed PMID: 9591768.8: Kakiki M, Ishihara H. Pharmacokinetics, metabolism and pharmacodynamics of a benzimidazole angiotensin II type 1 receptor antagonist in the beagle dog and cynomologus monkey. Xenobiotica. 1998 Jan;28(1):77-91. PubMed PMID: 9493321.9: Kakiki M, Morohashi K, Nomura M, Omura T, Horie T. Expression of aldosterone synthase cytochrome P450 (P450aldo) mRNA in rat adrenal glomerulosa cells by angiotensin II type 1 receptor. Endocr Res. 1997 Nov;23(4):277-95. PubMed PMID: 9430819.10: Kim S, Wanibuchi H, Hamaguchi A, Miura K, Yamanaka S, Iwao H. Angiotensin blockade improves cardiac and renal complications of type II diabetic rats. Hypertension. 1997 Nov;30(5):1054-61. PubMed PMID: 9369255.1
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