186497-07-4

186497-07-4 structure

Name: Zibotentan (ZD4054)
Chemical Name: N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
CAS Number: 186497-07-4
Molecular Formula: C₁₉H₁₆N₆O₄S
Molecular Weight: 424.433
Catalog: Biochemical Inhibitor G protein coupled receptor(GPCR & G Protein) Endothelin Receptor Antagonist
Create Date: 2018-06-11 20:18:33
Modify Date: 2024-01-02 11:41:42
Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054) treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.

Name	N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
Synonyms	N-(3-Methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide Zd 4054 S1456_Selleck ZD4054 Zibotentan

Description	Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054) treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor Research Areas >> Cancer
References	[1]. Zibotentan James, N.D., Growcott, J.W. Drugs Fut 2009, 34(8): 624. [2]. Clarkson-Jones JA, Kenyon AS, Kemp J, Lenz EM, Oliver SD, Swaisland H.,Disposition and metabolism of the specific endothelin A receptor antagonist zibotentan (ZD4054) in healthy volunteers.,Xenobiotica. 2012 Apr;42(4):363-71. Epub 2011 Oct 20. [3]. Li J, Liu Y, Qian J, Wu L, Kemp J, Nii M, Tomkinson H, Zuo Y, Ranson M, Usami M.,Single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (ZD4054) in Chinese men with advanced solid tumors.,Cancer Chemother Pharmacol. 2012 Jul;70( [4]. Nelson JB, Fizazi K, Miller K, Higano C, Moul JW, Akaza H, Morris T, McIntosh S, Pemberton K, Gleave M.,Phase 3, randomized, placebo-controlled study of zibotentan (ZD4054) in patients with castration-resistant prostate cancer metastatic to bone. ,Cancer [5]. Tomkinson H, Kemp J, Oliver S, Swaisland H, Taboada M, Morris T.,Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies.,BMC Clin Pharmacol. 2011 Mar 17;11:3.

Density	1.4±0.1 g/cm3
Boiling Point	637.0±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₆N₆O₄S
Molecular Weight	424.433
Flash Point	339.0±34.3 °C
Exact Mass	424.095367
PSA	141.37000
LogP	2.38
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.628
Storage condition	-20°C

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
RIDADR	NONH for all modes of transport
RTECS	UT7937700