Forasartan

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

MedKoo CAT#: 317950

CAS#: 145216-43-9

Description: Forasartan is a nonpeptide angiotensin II receptor antagonist with antihypertensive activity. Forasartan competes with angiotensin II for binding at the AT1 receptor subtype in vascular smooth muscle, thereby blocking angiotensin II-mediated vasoconstriction resulting in vascular dilatation. In addition, the antagonistic effect on AT1 in the adrenal gland, prevents angiotensin II-induced stimulation of aldosterone synthesis and secretion by the adrenal cortex.


Chemical Structure

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Forasartan
CAS# 145216-43-9

Theoretical Analysis

MedKoo Cat#: 317950
Name: Forasartan
CAS#: 145216-43-9
Chemical Formula: C23H28N8
Exact Mass: 416.24
Molecular Weight: 416.520
Elemental Analysis: C, 66.32; H, 6.78; N, 26.90

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: Forasartan; SC-52458; SC 52458; SC52458.

IUPAC/Chemical Name: 5-[(3,5-dibutyl-1,2,4-triazol-1-yl)methyl]-2-[2-(2H-tetrazol-5-yl)phenyl]pyridine

InChi Key: YONOBYIBNBCDSJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H28N8/c1-3-5-11-21-25-22(12-6-4-2)31(28-21)16-17-13-14-20(24-15-17)18-9-7-8-10-19(18)23-26-29-30-27-23/h7-10,13-15H,3-6,11-12,16H2,1-2H3,(H,26,27,29,30)

SMILES Code: CCCCC1=NN(C(=N1)CCCC)CC2=CN=C(C=C2)C3=CC=CC=C3C4=NNN=N4

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 416.52 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: Kushiku K, Yamada H, Shibata K, Tokunaga R, Katsuragi T, Furukawa T.
Upregulation of immunoreactive angiotensin II release and angiotensinogen mRNA
expression by high-frequency preganglionic stimulation at the canine cardiac
sympathetic ganglia. Circ Res. 2001 Jan 19;88(1):110-6. PubMed PMID: 11139482.


2: Aki Y, Tomohiro A, Nishiyama A, Kiyomoto K, Kimura S, Abe Y. The role of
basally synthesized nitric oxide in modulating the renal vasoconstrictor action
of angiotensin II. Hypertens Res. 1997 Dec;20(4):251-6. PubMed PMID: 9453259.


3: McMahon EG, Yang PC, Babler MA, Suleymanov OD, Palomo MA, Olins GM, Cook CS.
Effects of SC-52458, an angiotensin AT1 receptor antagonist, in the dog. Am J
Hypertens. 1997 Jun;10(6):671-7. PubMed PMID: 9194514.


4: Usune S, Furukawa T. Effects of SC-52458, a new nonpeptide angiotensin II
receptor antagonist, on increase in cytoplasmic Ca2+ concentrations and
contraction induced by angiotensin II and K(+)-depolarization in guinea-pig
taenia coli. Gen Pharmacol. 1996 Oct;27(7):1179-85. PubMed PMID: 8981065.


5: Ohta K, Kim S, Hamaguchi A, Yukimura T, Miura K, Takaori K, Iwao H. Role of
angiotensin II in extracellular matrix and transforming growth factor-beta 1
expression in hypertensive rats. Eur J Pharmacol. 1994 Sep 15;269(1):115-9.
PubMed PMID: 7828653.


6: Olins GM, Corpus VM, Chen ST, McMahon EG, Palomo MA, McGraw DE, Smits GJ, Null
CL, Brown MA, Bittner SE, et al. Pharmacology of SC-52458, an orally active,
nonpeptide angiotensin AT1 receptor antagonist. J Cardiovasc Pharmacol. 1993
Oct;22(4):617-25. PubMed PMID: 7505365.


7: de la Hoz JC. [Bee (Apis mellifera, Hymenoptera: Apoidea) visitation to
cantaloupe Cucumis melo (Cucurvitaceae) flowers in Panama]. Rev Biol Trop. 2007
Jun;55(2):677-80. Spanish. PubMed PMID: 19069779.


8: Krovat EM, Langer T. Non-peptide angiotensin II receptor antagonists: chemical
feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26.
PubMed PMID: 12593652.


9: Katsuragi T, Sato C, Guangyuan L, Honda K. Inositol(1,4,5)trisphosphate signal
triggers a receptor-mediated ATP release. Biochem Biophys Res Commun. 2002 May
3;293(2):686-90. PubMed PMID: 12054523.


10: Hagmann M, Nussberger J, Naudin RB, Burns TS, Karim A, Waeber B, Brunner HR.
SC-52458, an orally active angiotensin II-receptor antagonist: inhibition of
blood pressure response to angiotensin II challenges and pharmacokinetics in
normal volunteers. J Cardiovasc Pharmacol. 1997 Apr;29(4):444-50. PubMed PMID:
9156352.


11: Bauer JH, Reams GP. The angiotensin II type 1 receptor antagonists. A new
class of antihypertensive drugs. Arch Intern Med. 1995 Jul 10;155(13):1361-8.
Review. PubMed PMID: 7794084.


12: Ohta K, Kim S, Hamaguchi A, Miura K, Yukimura T, Iwao H. Cardiac
hypertrophy-related gene expression in spontaneously hypertensive rats: crucial
role of angiotensin AT1 receptor. Jpn J Pharmacol. 1995 Jan;67(1):95-9. PubMed
PMID: 7745853.


13: Tokunaga R, Kushiku K, Yamada K, Yamada H, Furukawa T. Possible involvement
of calcium-calmodulin pathways in the positive chronotropic response to
angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001
Aug;86(4):381-9. PubMed PMID: 11569611.