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MedKoo Cat#: 525004 | Name: Embusartan

Description:

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

Embusartan, also known as BAY 10-6734, is a potent, orally active angiotensin II receptor antagonist being developed by Bayer as an antihypertensive agent. The compound has potential for once daily administration with antihypertensive activity still present over a 24-h period. Embusartan was under preclinical development in Germany for the treatment of hypertension.

Chemical Structure

Embusartan
Embusartan
CAS#156001-18-2

Theoretical Analysis

MedKoo Cat#: 525004

Name: Embusartan

CAS#: 156001-18-2

Chemical Formula: C25H24FN5O3

Exact Mass: 461.1863

Molecular Weight: 461.49

Elemental Analysis: C, 65.07; H, 5.24; F, 4.12; N, 15.18; O, 10.40

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 #
No Data
Synonym
Embusartan; Bay 10-6734; Embusartan [INN]; UNII-4MY73645XA.
IUPAC/Chemical Name
6-n-Butyl-4-methoxycarbonyl-2-oxo-1-((2'-(1H-tetrazol-5-yl)-3-fluorobiphenyl-4-yl)methyl)-1,2-dihydropyridine
InChi Key
LYVGOAYMIAQLHI-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H24FN5O3/c1-3-4-7-19-12-18(25(33)34-2)14-23(32)31(19)15-17-11-10-16(13-22(17)26)20-8-5-6-9-21(20)24-27-29-30-28-24/h5-6,8-14H,3-4,7,15H2,1-2H3,(H,27,28,29,30)
SMILES Code
CCCCc1cc(cc(=O)n1Cc2ccc(cc2F)c3ccccc3c4[nH]nnn4)C(=O)OC
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, not in water
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 461.49 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: Wang JM, Tan J, Leenen FH. Central nervous system blockade by peripheral administration of AT1 receptor blockers. J Cardiovasc Pharmacol. 2003 Apr;41(4):593-9. PubMed PMID: 12658061. 2: Balt JC, Mathy MJ, Pfaffendorf M, van Zwieten PA. Sympatho-inhibitory properties of various AT1 receptor antagonists. J Hypertens Suppl. 2002 Jun;20(5):S3-11. PubMed PMID: 12184061. 3: Balt JC, Mathy MJ, Pfaffendorf M, van Zwieten PA. Inhibition of facilitation of sympathetic neurotransmission and angiotensin II-induced pressor effects in the pithed rat: comparison between valsartan, candesartan, eprosartan and embusartan. J Hypertens. 2001 Dec;19(12):2241-50. PubMed PMID: 11725169. 4: Zhang J, Leenen FH. Peripheral administration of AT1 receptor blockers and pressor responses to central angiotensin II and sodium. Can J Physiol Pharmacol. 2001 Oct;79(10):861-7. Erratum in: Can J Physiol Pharmacol 2001 Dec;79(12):1045. PubMed PMID: 11697745. 5: Zhang J, Leenen FH. AT(1) receptor blockers prevent sympathetic hyperactivity and hypertension by chronic ouabain and hypertonic saline. Am J Physiol Heart Circ Physiol. 2001 Mar;280(3):H1318-23. PubMed PMID: 11179079. 6: Warnholtz A, Nickenig G, Schulz E, Macharzina R, Bräsen JH, Skatchkov M, Heitzer T, Stasch JP, Griendling KK, Harrison DG, Böhm M, Meinertz T, Münzel T. Increased NADH-oxidase-mediated superoxide production in the early stages of atherosclerosis: evidence for involvement of the renin-angiotensin system. Circulation. 1999 Apr 20;99(15):2027-33. PubMed PMID: 10209008. 7: Iouzalen L, Stepien O, Marche P. Effects of BAY 10-6734 (Embusartan), a new angiotensin II type I receptor antagonist, on vascular smooth muscle cell growth. J Pharmacol Exp Ther. 1999 Apr;289(1):181-7. PubMed PMID: 10087002. 8: Böhm M, Zolk O, Flesch M, Schiffer F, Schnabel P, Stasch JP, Knorr A. Effects of angiotensin II type 1 receptor blockade and angiotensin-converting enzyme inhibition on cardiac beta-adrenergic signal transduction. Hypertension. 1998 Mar;31(3):747-54. PubMed PMID: 9495257. 9: Breithaupt-Grögler K, Malerczyk C, Belz GG, Butzer R, Herrmann V, Stass H, Wensing G. Pharmacodynamic and pharmacokinetic properties of an angiotensin II receptor antagonist--characterization by use of Schild regression technique in man. Int J Clin Pharmacol Ther. 1997 Oct;35(10):434-41. PubMed PMID: 9352392. 10: Stasch JP, Knorr A, Hirth-Dietrich C, Krämer T, Hübsch W, Dressel J, Fey P, Beuck M, Sander E, Frobel K, Kazda S. Long-term blockade of the angiotensin II receptor in renin transgenic rats, salt-loaded Dahl rats, and stroke-prone spontaneously hypertensive rats. Arzneimittelforschung. 1997 Sep;47(9):1016-23. PubMed PMID: 9342414. 11: Flesch M, Schiffer F, Zolk O, Pinto Y, Stasch JP, Knorr A, Ettelbrück S, Böhm M. Angiotensin receptor antagonism and angiotensin converting enzyme inhibition improve diastolic dysfunction and Ca(2+)-ATPase expression in the sarcoplasmic reticulum in hypertensive cardiomyopathy. J Hypertens. 1997 Sep;15(9):1001-9. PubMed PMID: 9321748.