Atrasentan

• CAT Number: I002268
• CAS Number: 173937-91-2
• Molecular Formula: C29H38N2O6
• Molecular Weight: 510.62
• Purity: ≥95%
• Synonyms: (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
• Target: Endothelin Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.0551 nM (for ET A receptor)
• InChI: InChI=1S/C29H38N2O6.ClH/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20;/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34);1H/t23-,27-,28+;/m1./s1
• InChIKey: IJFUJIFSUKPWCZ-SQMFDTLJSA-N
• SMILES: CCCCN(CCCC)C(=O)CN1CC(C(C1C2=CC=C(C=C2)OC)C(=O)O)C3=CC4=C(C=C3)OCO4

Atrasentan (CAT: I002268) is a selective endothelin receptor antagonist, primarily targeting the endothelin receptor type A (ETA). Endothelin receptors are involved in regulating blood vessel constriction and cell growth. By blocking the ETA receptors, atrasentan reduces the binding of endothelin-1 and inhibits its vasoconstrictive effects. This results in vasodilation and a decrease in blood pressure. Atrasentan has been studied for its potential application in treating conditions such as hypertension and diabetic nephropathy. It may help reduce blood pressure, improve kidney function, and mitigate the progression of kidney damage in patients with these conditions.

Reference

1. Drugs Today (Barc). 2006 May;42(5):299-312.

Atrasentan: a rationally designed targeted therapy for cancer.

Jimeno A(1), Carducci M.

Author information:
(1)Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University,
Baltimore, Maryland 21231-1000, USA.

Endothelin axis deregulation triggers a series of events that ultimately
activates proliferation, invasion, escape from programmed cell death, new vessel
formation, abnormal osteogenesis and alteration of nociceptive stimuli.
Atrasentan is a novel agent that effectively targets this pathway and is able to
inhibit and/or reverse several of these events. Biologic and clinical activity in
patients with prostate cancer have been demonstrated in a phase III,
placebo-controlled setting by the suppression of markers of biochemical prostate
cancer progression and a delay in time to disease progression. Atrasentan may
represent a therapeutic option in the management of prostate and other cancers
that is worthy of continued investigation.

2. Expert Opin Investig Drugs. 2004 Dec;13(12):1631-40.

Atrasentan: targeting the endothelin axis in prostate cancer.

Jimeno A(1), Carducci M.

Author information:
(1)Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins University,
Bunting-Blaustein Cancer Research Building, Room 1M89, 1650 Orleans Street,
Baltimore, MD 21231-1000, USA.

Endothelin axis deregulation triggers a series of events that lead to a profound
deregulation in cancer cells, including key tumorigenic cellular events such as
proliferation, invasion, escape from programmed cell death, new vessel formation,
abnormal osteogenesis and the alteration of nociceptive stimuli. Atrasentan is a
novel agent that effectively targets this pathway and is able to inhibit and/or
reverse several of those events. Biological and clinical activity in patients
with prostate cancer has been demonstrated in a Phase III clinical setting by the
suppression of markers of biochemical and clinical prostate cancer progression,
and by a delay in time to disease progression, especially in patients with bone
disease.