Darusentan | Alomone Labs D-265 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

Darusentan

catalog :

D-265

more info or order :

Alomone Labs product webpage

image

image 1 :

Expression of Mitochondrial uncoupling protein 2 (UCP2) in mouse C2C12 cells. - Immunocytochemical staining of mouse muscle myoblast (C2C12) fixed permeabilized cells. Intracellular staining of cells with Anti-UCP2 Antibody(#ANT-128) (green) (1:50-1:200) followed by goat anti-rabbit-AlexaFluor-488 secondary antibody. A. Magnitude 1x40 (1:50). B-C. Magnitude 1x100 (1:200). DAPI is used as the counterstain (blue).

image 2 :

product information

CAT :

D-265

SKU :

D-265_10 mg

Product Name :

Darusentan

Group Type :

Non Antibodies

Product Type :

S. Molecules

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Storage before Reconstitution :

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

Shipping and storage :

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

Product Page - Scientific background :

Darusentan, (LU 135252), is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. Darusentan is orally bioavailable and is a potent inhibitor of vasoconstriction in large and small arteries. The compound is a propanoic acid based antagonist that consist of two enantiomers - (R) and (S). The (R) enantiomer shows no binding activity, indicating that the (S) enantiomer is the active drug1,2.in vitro, Darusentan inhibits endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 value of 8.11,2.Endothelin receptors include two subtypes: ET-A and ET-B. They 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 detected in several different regions of the brain3.

Supplier :

Alomone Labs

Target :

ET-A receptors

Long Description :

Darusentan (#D-265) is a highly pure, synthetic, and biologically active compound.

Short Description :

A Selective Antagonist of Endothelin A Receptors

MW :

410.43

Synonyms :

LU 135252

Source :

Synthetic

Molecular formula :

C22H22N2O6.

Effective Concentration :

1 nM - 1 µM.

Activity :

Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 6 nM and 371 nM, respectively1. in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 of 8.12. Darusentan is orally bioavailable and active in vivo3.

Reconstitution and Solubility :

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Solubility :

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Storage of solutions :

Up to three months at -20°C.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>99%

CAS No :

171714-84-4

Form :

Lyophilized powder.

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Chemical Name :

(2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid.

more info or order :

Alomone Labs product webpage