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Home / Biochemicals / Small Molecules

Zibotentan

SKU : BHB21300383

A Selective Antagonist of Endothelin A Receptors

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Mfr.No.	Z-130, Z-130_10 mg, Z-130_100 mg, Z-130_25 mg, Z-130_5 mg, Z-130_50 mg
Description	Zibotentan (#Z-130) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C19H16N6O4S.
Synonyms	Synthetic
Background	Zibotentan (ZD4054) is an orally active nonpeptide with specificity towards Endothelin A (ET-A) receptors with no activity on Endothelin B (ET-B) receptors. The compound inhibits endothelin-1 radioligand binding to human ET-A receptor with an IC50 value of 21 nM1.Studies show that Zibotentan successfully inhibits growth of tumor xenografts in mice and enhances the cytotoxicity of paclitaxel in ovarian carcinoma in vitro and in vivo1.Endothelin receptors are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several regions of the brain. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-32.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	1 nM - 10 uM.
Reconstitution	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Cas Number	186497-07-4
Molecular Weight	424.43
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Activity	Zibotentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A with IC50 of 21 nM (whilst showing no effect on ET-B at 10 uM). Zibotentan is orally bioavailable and active in vivo.1
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)pyridine-3-sulfonamide.

Purity	>95%
Form	Lyophilized powder.
Storage	Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Morris, C.D. et al. (2005) Br. J. Cancer 92, 2148. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Morris, C.D. et al. (2005) Br. J. Cancer 92, 2148.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300383-1	Z-130_10 mg	10 mg	$202		Add to Cart
BHB21300383-2	Z-130_100 mg	100 mg	$802		Add to Cart
BHB21300383-3	Z-130_25 mg	25 mg	$337		Add to Cart
BHB21300383-4	Z-130_5 mg	5 mg	$117		Add to Cart
BHB21300383-5	Z-130_50 mg	50 mg	$539		Add to Cart

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