Atrasentan - CAS 173937-91-2
Catalog number: 173937-91-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Endothelin Receptor
atrasentan hydrochloride is the orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.
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US brand name: Xinlay; Code names: (+)-A 127722; ABT-627; A 127722; Xinlay; ABT 627; NSC720763; A-147627.
Current Developer:
Abbott Laboratories
1.Moderate additive effects of endothelin receptor A blockade in Ren-2 transgenic rats subjected to various types of RAS blockade.
Vaněčková I1, Řezáčová L2, Kuneš J2, Zicha J2. Life Sci. 2016 Jan 14. pii: S0024-3205(16)30020-0. doi: 10.1016/j.lfs.2016.01.020. [Epub ahead of print]
AIMS: Chronic endothelin receptor A (ETA) blockade lowered blood pressure (BP) by decreasing angiotensin-dependent vasoconstriction and attenuating calcium influx. We tested whether the addition of ETA blockade to renin-angiotensin system (RAS) blockade would have further effects on the principal vasoactive systems contributing to BP maintenance in Ren-2 transgenic rats (TGR).
2.Prediction of the effect of atrasentan on renal and heart failure outcomes based on short-term changes in multiple risk markers.
Schievink B1, de Zeeuw D1, Smink PA1, Andress D2, Brennan JJ2, Coll B2, Correa-Rotter R3, Hou FF4, Kohan D5, Kitzman DW6, Makino H7, Parving HH8, Perkovic V9, Remuzzi G10, Tobe S11, Toto R12, Hoekman J13, Lambers Heerspink HJ14. Eur J Prev Cardiol. 2016 May;23(7):758-68. doi: 10.1177/2047487315598709. Epub 2015 Jul 30.
BACKGROUND: A recent phase II clinical trial (Reducing Residual Albuminuria in Subjects with Diabetes and Nephropathy with AtRasentan trial and an identical trial in Japan (RADAR/JAPAN)) showed that the endothelin A receptor antagonist atrasentan lowers albuminuria, blood pressure, cholesterol, hemoglobin, and increases body weight in patients with type 2 diabetes and nephropathy. We previously developed an algorithm, the Parameter Response Efficacy (PRE) score, which translates short-term drug effects into predictions of long-term effects on clinical outcomes.
3.A Meta-Analysis and Indirect Comparison of Endothelin A Receptor Antagonist for Castration-Resistant Prostate Cancer.
Qi P1, Chen M2, Zhang LX3, Song RX4, He ZH5, Wang ZP4. PLoS One. 2015 Jul 20;10(7):e0133803. doi: 10.1371/journal.pone.0133803. eCollection 2015.
BACKGROUND: Endothelin A (ET-A) receptor antagonists including zibotentan and atrasentan, have been suggested as a treatment for castration-resistant prostate cancer (CRPC). Our aim was to conduct a meta-analysis and indirect comparison to assess the efficacy and safety of ET-A receptor antagonists for treatment of CRPC.
4.Atrasentan increased the expression of klotho by mediating miR-199b-5p and prevented renal tubular injury in diabetic nephropathy.
Kang WL1,2, Xu GS3. Sci Rep. 2016 Jan 27;6:19979. doi: 10.1038/srep19979.
Atrasentan is a promising therapy for treating diabetic nephropathy (DN). Here we evaluated whether atrasentan down-regulated the miR-199b-5p expression, thereby increasing klotho and preventing renal tubular injury in DN. One-hundred patients with type 2 diabetes mellitus (T2DM) and 40 healthy subjects were included. A DN mice model was established by an injection of streptozotocin (STZ). Human renal proximal tubular epithelial HK-2 cells were exposed to high glucose (20 mmol/L). Treated the mice and HK-2 cells with atrasentan, and we then investigated whether and how miR-199b-5p and Klotho were involved in preventing renal tubular injury in DN. In patients, the serum miR-199b-5p level increased and the klotho concentration decreased in accordance with elevated albuminuria. Atrasentan down-regulated miR-199b-5p and up-regulated klotho of the DN mice and HK-2 cells exposed to high glucose. High glucose promoted the binding of histone H3 to the miR-199b-5p promoter, and atrasentan canceled this effect.
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CAS 173937-91-2 Atrasentan

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