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

MedKoo CAT#: 526926

CAS#: 135070-05-2

Description: E-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.

Chemical Structure

CAS# 135070-05-2

Theoretical Analysis

MedKoo Cat#: 526926
Name: E-4177
CAS#: 135070-05-2
Chemical Formula: C24H21N3O2
Exact Mass: 383.1634
Molecular Weight: 383.451
Elemental Analysis: C, 75.18; H, 5.52; N, 10.96; O, 8.34

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: E-4177; E-4177; E4177.

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


InChi Code: 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)


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: >2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 383.451 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

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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.

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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.

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11: Kakiki M, Morohashi K, Nomura M, Omura T, Horie T. Regulation of aldosterone synthase cytochrome P450 (CYP11B2) and 11 beta-hydroxylase cytochrome P450 (CYP11B1) expression in rat adrenal zona glomerulosa cells by low sodium diet and angiotensin II receptor antagonists. Biol Pharm Bull. 1997 Sep;20(9):962-8. PubMed PMID: 9331977.

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13: Seki T, Yamazaki K, Kayano M. Determination of angiotensin II receptor antagonist (E4177) in human plasma and urine by high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl. 1997 Jan 10;688(1):101-6. PubMed PMID: 9029319.

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15: Makino N, Sugano M, Hata T, Taguchi S, Yanaga T. Chronic low-dose treatment with enalapril induced cardiac regression of left ventricular hypertrophy. Mol Cell Biochem. 1996 Oct-Nov;163-164:239-45. PubMed PMID: 8974063.

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17: Makino N, Hata T, Sugano M, Dixon IM, Yanaga T. Regression of hypertrophy after myocardial infarction is produced by the chronic blockade of angiotensin type 1 receptor in rats. J Mol Cell Cardiol. 1996 Mar;28(3):507-17. PubMed PMID: 9011634.

18: Shimakura K, Sanaka M, Wang L, Mineshita S, Miyazaki M. Pulmonary edema induced by angiotensin II in rats. Jpn J Pharmacol. 1995 Apr;67(4):383-9. PubMed PMID: 7650872.

19: Song K, Miyazaki M, Okunishi H, Ishii K, Takai S, Shiota N, Kim S, Mendelsohn FA. Localization and quantitation of active renin in monkey kidney by radioinhibitor binding and in vitro autoradiography. Am J Hypertens. 1994 Jun;7(6):529-35. PubMed PMID: 7917151.

20: Okunishi H, Song K, Oka Y, Kobayashi T, Kawamoto T, Ishihara H, Mori N, Miyazaki M. In vitro pharmacology of a novel non-peptide angiotensin II-receptor antagonist, E4177. Jpn J Pharmacol. 1993 Jul;62(3):239-44. PubMed PMID: 8411773.