Tasosartan
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MedKoo CAT#: 318792

CAS#: 145733-36-4

Description: Tasosartan is an angiotensin II receptor antagonist.


Chemical Structure

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Tasosartan
CAS# 145733-36-4

Theoretical Analysis

MedKoo Cat#: 318792
Name: Tasosartan
CAS#: 145733-36-4
Chemical Formula: C23H21N7O
Exact Mass: 411.18
Molecular Weight: 411.469
Elemental Analysis: C, 67.14; H, 5.14; N, 23.83; O, 3.89

Price and Availability

Size Price Availability Quantity
1g USD 3850
2g USD 5450
5g USD 8650
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Synonym: Tasosartan

IUPAC/Chemical Name: 8-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one

InChi Key: ADXGNEYLLLSOAR-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)

SMILES Code: O=C1CCC2=C(C)N=C(C)N=C2N1CC3=CC=C(C4=CC=CC=C4C5=NN=NN5)C=C3

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 411.47 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Korkes H, Oliveira LG, Berlinck L, Borges AF, Goes FS, Watanabe S, Landman C, Sass N. PP138. Human fetal malformations associated with the use of angiotensin II receptor antagonist. Pregnancy Hypertens. 2012 Jul;2(3):314-5. doi: 10.1016/j.preghy.2012.04.249. Epub 2012 Jun 13. PubMed PMID: 26105460.

2: Elokdah HM, Friedrichs GS, Chai SY, Harrison BL, Primeau J, Chlenov M, Crandall DL. Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71. PubMed PMID: 12113820.

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5: Viigimaa M, Allikmets K, Parik T, Skards J, Franken A, Häss G. Tasosartan and hydroclorothiazide as combination therapy in the treatment of severe essential hypertension: comparison with enalapril. Tasosartan Study Group. Cardiovasc Drugs Ther. 2000 Aug;14(4):447-9. PubMed PMID: 10999653.

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7: Andrawis NS, Battle MM, Klamerus KJ, Burghart PH, Neefe L, Weinryb I, Mayer P, Abernethy DR. A pharmacokinetic and pharmacodynamic study of the potential drug interaction between tasosartan and atenolol in patients with stage 1 and 2 essential hypertension. J Clin Pharmacol. 2000 Mar;40(3):231-41. PubMed PMID: 10709151.

8: Hines J, Fluharty SJ, Sakai RR. The angiotensin AT(1) receptor antagonist irbesartan has near-peptide affinity and potently blocks receptor signaling. Eur J Pharmacol. 1999 Nov 12;384(1):81-9. PubMed PMID: 10611423.

9: Timmermans PB. Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F. Review. PubMed PMID: 10579749.

10: Timmermans PB. Angiotensin II receptor antagonists: an emerging new class of cardiovascular therapeutics. Hypertens Res. 1999 Jul;22(2):147-53. Review. PubMed PMID: 10487332.

11: Rhéaume C, Waib PH, Lacourcière Y, Cléroux J. Effects of angiotensin antagonism with tasosartan on regional and systemic haemodynamics in hypertensive patients. J Hypertens. 1998 Dec;16(12 Pt 2):2085-9. PubMed PMID: 9886901.

12: Neutel JM, Buckalew V, Chrysant SG, Mroczek WJ, Ruff DA, Weber M. Efficacy and tolerability of tasosartan, a novel angiotensin II receptor blocker: results from a 10-week, double-blind, placebo-controlled, dose-titration study. Tasosartan Investigators Group. Am Heart J. 1999 Jan;137(1):118-25. PubMed PMID: 9878944.

13: Ellingboe JW, Collini MD, Quagliato D, Chen J, Antane M, Schmid J, Hartupee D, White V, Park CH, Tanikella T, Bagli JF. Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group. J Med Chem. 1998 Oct 22;41(22):4251-60. PubMed PMID: 9784100.

14: Lacourcière Y, Pool JL, Svetkey L, Gradman AH, Larochelle P, de Champlain J, Smith WB. A randomized, double-blind, placebo-controlled, parallel-group, multicenter trial of four doses of tasosartan in patients with essential hypertension. Tasosartan Investigator's Group. Am J Hypertens. 1998 Apr;11(4 Pt 1):454-61. PubMed PMID: 9607384.

15: Brunner HR. The new angiotensin II receptor antagonist, irbesartan: pharmacokinetic and pharmacodynamic considerations. Am J Hypertens. 1997 Dec;10(12 Pt 2):311S-317S. Review. PubMed PMID: 9438775.

16: Ellingboe JW, Antane M, Nguyen TT, Collini MD, Antane S, Bender R, Hartupee D, White V, McCallum J, Park CH, et al. Pyrido[2,3-d]pyrimidine angiotensin II antagonists. J Med Chem. 1994 Feb 18;37(4):542-50. PubMed PMID: 8120871.