Valspodar 是一種 p-糖蛋白 (
P-gp) 抑制劑,被廣泛用作克服多藥耐藥性調節劑。
Valspodar產品描述:Valspodar is a P-glycoprotein (
P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
In Vitro:Valspodar (PSC 833) has no cytotoxicity effects at up to the
co
ncentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and
DOX-L are added to the DOX resistant cells, and cell kill efficacy of
MDR cell type increases significantly when valspodar is administered
alo
ngside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all
co
ncentrations of DOX, are most toxic and kill more than 70% of the
resistant cells
[1]. Pretreatment with PSC833 decreases the IC
50 value of mitoxantrone in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR
cells and almost completely reverses the resistance of MDR cells to
mitoxantrone
[3].
In Vivo:valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitio
ning as
reflected in its low mean blood-to-plasma ratio of approximately 0.52.
Valspodar displays properties of slow clearance and a large volume of
distribution. Valspodar shows properties of low hepatic extraction and
wide distribution, similar to that of its structural analogue
cyclosporine A
[2].
Preadministration of PSC833 to mice increases mitoxantrone fluorescent
intensity in MDR tumor to 94% of that in the wild-type tumors
[3].
公司介紹:MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫,總部位于美國新澤西,分別在瑞典和上海設有歐洲區子公司和區總代理,營銷網點遍及20多個地區。MCE經過多年努力已成為生物活性小分子領域的供應商,
產品涵蓋癌癥、神經科學、抗感染、表觀遺傳學等20個熱門研究領域,PI3K、MAPK等近千個細分靶點,超過4000個活性小分子化合物現貨,以及GPCR、API、離子通道等超過20種不同類型的化合物庫,同時提供從毫克到千克的專業定制合成服務。
MCE 對每批產品都進行嚴格的LCMS和NMR檢驗,其產品已被近萬名客戶廣泛使用并發表大量文章、;
MCE 定期增加各領域熱門抑制劑、激動劑,不斷擴增已有化合物庫,以滿足新的科研需求;
數千種產品在上海有充足備貨,24-48小時內送達客戶;
大量產品提供試用裝; 已為多個知名企業、院校構建各種定制型化合物庫。
Purity:98%
MWt:1214.6220
Formula:C63H111N11O12
SMILES:O=C([C@H](C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N(C)C([C@H](C(C)C)NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[C@@H](C([C@H](C)C/C=C/C)=O)C1=O
Pathway:Membrane Transporter/Ion Channel;
Mechanisms:P-glycoprotein;
Research Area:Cancer
本頁產品地址:http://www.lgsztm.com/sell/show-8005633.html