144143-96-4 Eprosartan mesylate AKSci O812
 
 
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  O812    AKSci Reference Standard
Eprosartan mesylate
, 99% (HPLC)
 
Eprosartan monomethanesulfonate




IDENTITY
CAS Number:144143-96-4
MDL Number:MFCD08141807
MF:C24H28N2O7S2
MW:520.62
SPECIFICATIONS & PROPERTIES
Purity:99% (HPLC)
Spectra:NMR, LCMS, FT-IR, HPLC
Physical Form:White to off-white crystalline powder
Melting Point:250-253°C
Long-Term Storage:Store at room temperature

BIOLOGICAL INFO
Solubility:DMSO: >10mg/mL
Application(s):Angiotensin II receptor antagonist

REVIEW

 Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT1 receptor. Its affinity for the AT1 receptor is 1,000 times greater than for the AT2 receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT1 receptor. Eprosartan has also been shown to bind to AT1 receptors both presynaptically and synaptically. Its action on presynaptic AT1 receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough).

REFERENCES
[1]Ruilope L, Jager B, Prichard B: Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial. Blood Press. 2001;10(4):223-9.
[2] Hedner T: The clinical profile of the angiotensin II receptor blocker eprosartan. J Hypertens Suppl. 2002 Jun;20(5):S33-8.
[3] Puig JG, Lopez MA, Bueso TS, Bernardino JI, Jimenez RT: Clinical profile of eprosartan. Cardiovasc Drugs Ther. 2002 Dec;16(6):543-9.
[4] Ruilope L, Jager B: Eprosartan for the treatment of hypertension. Expert Opin Pharmacother. 2003 Jan;4(1):107-14.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319

Precautionary Statements
P264; P280; P302+P352; P305+P351+P338; P321; P332+P313; P337+P313; P362


Current as of August 26, 2019

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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For research use only. Not for diagnostic or therapeutic use.
Not for human use.


CATEGORIES

 APIs and Bioactives > Angiotensin Receptor Blockers


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