Description: IC50 Value: 0.0551 nM (for ET A receptor) [1] Atrasentan (A-147627) is an endothelin antagonist receptor being developed at Abbott Laboratories for the treatment of prostate cancer. in vitro: The combination of
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Antagonist of ET A receptor;Antagonist of ET B receptor
1.Salani D, Rosanò L, Di Castro V, Spinella F, Venuti A, Padley RJ, Nicotra MR, Natali PG, Bagnato A. (2002) ABT-627, a potent endothelin receptor A antagonist, inhibits ovarian carcinoma growth in vitro.. Clin Sci, 103 Suppl 48 (13):(318S-321S). [PMID:12193113][10.1021/op500134e]
2.Chiappori AA, Haura E, Rodriguez FA, Boulware D, Kapoor R, Neuger AM, Lush R, Padilla B, Burton M, Williams C et al.. (2008) Phase I/II study of atrasentan, an endothelin A receptor antagonist, in combination with paclitaxel and carboplatin as first-line therapy in advanced non-small cell lung cancer.. Clin Cancer Res, 14 (5):(1464-9). [PMID:18316570][10.1021/op500134e]
3.Sasser JM, Sullivan JC, Hobbs JL, Yamamoto T, Pollock DM, Carmines PK, Pollock JS. (2007) Endothelin A receptor blockade reduces diabetic renal injury via an anti-inflammatory mechanism.. J Am Soc Nephrol, 18 (1):(143-54). [PMID:17167119][10.1021/op500134e]
4.Nelson JB, Chan-Tack K, Hedican SP, Magnuson SR, Opgenorth TJ, Bova GS, Simons JW. (1996) Endothelin-1 production and decreased endothelin B receptor expression in advanced prostate cancer.. Cancer Res, 56 (4):(663-8). [PMID:8630991][10.1021/op500134e]
5.Opgenorth TJ, Adler AL, Calzadilla SV, Chiou WJ, Dayton BD, Dixon DB, Gehrke LJ, Hernandez L, Magnuson SR, Marsh KC et al.. (1996) Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist.. J Pharmacol Exp Ther, 276 (2):(473-81). [PMID:8632312][10.1021/op500134e]
6.Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, Kester JA, Mantei RA, Bal R, Sorensen BK et al.. (1996) 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.. J Med Chem, 39 (5):(1039-48). [PMID:8676339][10.1021/op500134e]
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