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Merck
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重要文件

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SML0572

Sigma-Aldrich

Valspodar

≥98% (HPLC)

同義詞:

6-[(2S,4R,6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic acid]cyclosporin D, Amdray, PSC833, [3′-Desoxy-3′-oxo-MeBmt]1-[Val]2-cyclosporin

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About This Item

經驗公式（希爾表示法）:
C63H111N11O12
CAS號碼:
121584-18-7
分子量：:
1214.62
MDL號碼:
MFCD00907207
分類程式碼代碼:
12161501
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

運輸包裝

wet ice

儲存溫度

−20°C

SMILES 字串

N1([C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C1=O)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C(C)C)C(=O)[C@@H](C\C=C\C)C)C)C(C)C)C

InChI

1S/C63H111N11O12/c1-26-27-28-41(16)53(76)52-57(80)67-49(38(10)11)61(84)68(19)33-48(75)69(20)44(29-34(2)3)56(79)66-50(39(12)13)62(85)70(21)45(30-35(4)5)55(78)64-42(17)54(77)65-43(18)58(81)71(22)46(31-36(6)7)59(82)72(23)47(32-37(8)9)60(83)73(24)51(40(14)15)63(86)74(52)25/h26-27,34-47,49-52H,28-33H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)(H,67,80)/b27-26+/t41-,42+,43-,44+,45+,46+,47+,49+,50+,51+,52+/m1/s1

InChI 密鑰

YJDYDFNKCBANTM-QCWCSKBGSA-N

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應用

Valspodar/ PSC-833 has been used as a ABCB1 (P-glycoprotein) inhibitor.

生化／生理作用

Valspodar is a nonimmunosuppressive cyclosporin analog and potent P-glycoprotein (MDR1) inhibitor.
Valspodar is a nonimmunosuppressive cyclosporin analog and potent P-glycoprotein (MDR1) inhibitor. Valspodar reverses multidrug resistance (MDR) by inhibiting cellular drug efflux mediated by P-glycoprotein.

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

從最近期的版本中選擇一個：

分析證明 (COA)

Lot/Batch Number
106M4727V
026M4775V
125M4727V
025M4708V
123M4733V

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Kohjiro Nagao et al.
Biochimica et biophysica acta, 1831(2), 398-406 (2012-11-17)
ATP-binding cassette protein A1 (ABCA1) plays a key role in generating high-density lipoprotein (HDL). However, the detailed mechanism of HDL formation remains unclear; in order to reveal it, chemicals that specifically block each step of HDL formation would be useful.
Benjamin L Emmink et al.
Gastroenterology, 141(1), 269-278 (2011-04-05)
Stem cells of normal tissues have resistance mechanisms that allow them to survive genotoxic insults. The stem cell-like cells of tumors are defined by their tumor-initiating capacity and may have retained these resistance mechanisms, making them resistant to chemotherapy. We
Lynae M Brayboy et al.
Fertility and sterility, 100(5), 1428-1435 (2013-08-21)
To determine the multidrug-resistant transporter (MDR) activity in oocytes and their potential role in oocyte susceptibility to chemotherapy. Experimental laboratory study. University and academic center for reproductive medicine. Women with eggs retrieved for intracytoplasmic sperm injection cycles and adult female
Ziyad Binkhathlan et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 81(1), 142-148 (2012-03-01)
Co-administration of P-glycoprotein (P-gp) inhibitors such as cyclosporine A (CyA) and its analogue valspodar with doxorubicin (DOX) can result in diminished clearance of DOX, leading to accentuated toxicity. The purpose of this study was to evaluate whether the effect of
Jonathan E Kolitz et al.
Blood, 116(9), 1413-1421 (2010-06-05)
Cancer and Leukemia Group B 19808 (CALGB 19808) is the only randomized trial of a second-generation P-glycoprotein (Pgp) modulator in untreated patients with acute myeloid leukemia (AML) younger than age 60 years. We randomly assigned 302 patients to receive induction
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