Products

Enzymes for Research, Diagnostic and Industrial Use

Valspodar

Cat No.
CEI-1567
Product Overview
Valspodar is a potent inhibitor of P-glycoprotein (P-gp) widely used in preclinical and clinical studies. P-gp is a transmembrane glycoprotein which is located on cell membrane. P-gp distributes extensively and is expressed in certain cell types primarily containing liver, colon, kidney and pancreas. It also is known as multidrug resistance protein 1 (MDR1) which is pumps foreign substances out of cells. P-gp decreases the net uptake of cytotoxic drugs into the cells and mediats the efflux of these agents out of the cells, which is ATP-dependent. P-gp also overexpress in some cancer cells. P-gp plays an important role in mediating resistance to anticancer drugs and decreasing drug accumulation in multidrug-resistant cancer cells. Valspodar can reverse the resistance to mitoxantrane which is due to the expression of P-gp. The IC50 of mitoxantrane decreased from 1.6 ±0.13 μM to 0.4 ±0.02μM in MDA-MB-435mdr cells pretreated with 3 mg/ml PSC. Valspodar increase the mitoxantrane intracellular accumulation by decreasing drug efflux and increasing mitoxantrone net uptake in cells. The cytotoxicity was significant greater in T47D/TAMR-6 cells treated with doxorubicin and valspodar than doxorubicin only. Co-encapsulation of doxorubicin and valspodar presents a promising anticancer effect. Valspodar was rapid absorpted and reachs the peak within 2 hnafter an oral dose. Valspodar showed properties of wide distribution, low hepatic extraction and mean bioavailability of 42.8% in rat.
CAS No.
121584-18-7
Molecular Weight
1214.62
Purity
0.98
Storage
Store at -20°C
Synonyms
PSC 833; PSC-833; PSC833
Targets
P-glycoprotein
Molecular Formula
C63H111N11O12
Chemical Name
PSC 833; PSC-833; PSC833
Solubility
Limited solubility
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
Download Datasheet:



Inquiry
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: