114798-36-6
Chemical Structure
EXP3179
Synonym(s): Losartan Carboxaldehyde; DuP 167
- CAS No.: 114798-36-6
- Formula:C22H21ClN6O
- Molecular Weight:420.89
IUPAC Name: 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazole-5-carbaldehyde
InChIKey: FQZSMTSTFMNWQF-UHFFFAOYSA-N
SMILES: [H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(C=C3)CN4C(C([H])=O)=C(N=C4CCCC)Cl
Biological Activity: EXP3179 (Losartan Carboxaldehyde) is a metabolite of Losartan (HY-17512). EXP3179 binds to AT1R with an affinity of 20 nM and blocks ANGII-induced AT1R signaling, inhibiting ERK1/2 activation. EXP3179 reduces NADPH oxidase activity. EXP3179 inhibits Phenylephrine (HY-B0769)-induced aortic contraction through an endothelium-dependent, NO-dependent mechanism. EXP3179 dose-dependently inhibits type I collagen-induced platelet aggregation and activation through GPVI binding, reducing platelet adhesion to the injured site. EXP3179 lowers blood pressure in normotensive and spontaneously hypertensive rats and mice. EXP3179 can be used for research on type 2 diabetes, hypertensive heart disease, hypertension, thrombosis, and coronary artery disease[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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EXP3179 | 98.09% | EXP3179 (Losartan Carboxaldehyde) is a metabolite of Losartan (HY-17512). EXP3179 binds to AT1R with an affinity of 20 nM and blocks ANGII-induced AT1R signaling, inhibiting ERK1/2 activation. EXP3179 reduces NADPH oxidase activity. EXP3179 inhibits Phenylephrine (HY-B0769)-induced aortic contraction through an endothelium-dependent, NO-dependent mechanism. EXP3179 dose-dependently inhibits type I collagen-induced platelet aggregation and activation through GPVI binding, reducing platelet adhesion to the injured site. EXP3179 lowers blood pressure in normotensive and spontaneously hypertensive rats and mice. EXP3179 can be used for research on type 2 diabetes, hypertensive heart disease, hypertension, thrombosis, and coronary artery disease. | ||||||||||||||||||||
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EXP3179 (Standard) | ≥98% | EXP3179 (Standard) (Losartan Carboxaldehyde (Standard)) is the analytical standard of EXP3179 (HY-114950). This product is intended for research and analytical applications. EXP3179 is a metabolite of Losartan (HY-17512). EXP3179 binds to AT1R with an affinity of 20 nM and blocks ANGII-induced AT1R signaling, inhibiting ERK1/2 activation. EXP3179 reduces NADPH oxidase activity. EXP3179 inhibits Phenylephrine (HY-B0769)-induced aortic contraction through an endothelium-dependent, NO-dependent mechanism. EXP3179 dose-dependently inhibits type I collagen-induced platelet aggregation and activation through GPVI binding, reducing platelet adhesion to the injured site. EXP3179 lowers blood pressure in normotensive and spontaneously hypertensive rats and mice. EXP3179 can be used for research on type 2 diabetes, hypertensive heart disease, hypertension, thrombosis, and coronary artery disease. | ||||||||||||||||||||
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References
- [1]. Pershadsingh HA. New generation angiotensin II type 1 receptor antagonists that selectively modulate peroxisome proliferator‐activated receptor‐γ. Drug development research. 2006 Aug;67(8):687-97.
- [2]. Moreno MU, et al. Association of phagocytic NADPH oxidase activity with hypertensive heart disease: a role for cardiotrophin-1?. Hypertension. 2014 Mar;63(3):468-74.
- [3]. Sauge E, et al. Losartan metabolite EXP3179 is a unique blood pressure-lowering AT1R antagonist with direct, rapid endothelium-dependent vasoactive properties. Vascular pharmacology. 2022 Dec;147:107112.
- [4]. Li R, et al. Blocking platelet glycoprotein VI (GPVI) as a promising antithrombotic treatment. Drug discovery today. 2025 Oct;30(10):104473.
- [5]. Bene M, et al. LOSARTAN REJUVENATES SERUM AND HEART METABOLOME OF AGED MICE BY ANGIOTENSIN DEPENDENT AND INDEPENDENT MECHANISMS. Innovation in Aging. 2024 Dec 1;8(Supplement_1):1144-.
- [6]. Schieffer MB, et al. Comparative effects of AT1-antagonism and angiotensin-converting enzyme inhibition on markers of inflammation and platelet aggregation in patients with coronary artery disease. Journal of the American College of Cardiology. 2004 Jul 21;44(2):362-8.
- [7]. Kumra H, et al. Improving response of pancreatic cancer to losartan: Mechanistic insights and implications for personalized therapy[J]. Cancer Research, 2026, 86(7_Supplement): 1781-1781.
