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[CAS NO. 465-16-7]??Oleandrin

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PRODUCTS SPECIFICATIONS [465-16-7]

Catalog
HY-13719
Brand
MCE
CAS
465-16-7

DESCRIPTION [465-16-7]

Overview

MDLMFCD00079204
Molecular Weight576.72
Molecular FormulaC32H48O9
SMILESO=C1OCC([C@H]2[C@@H](OC(C)=O)C[C@]3(O)[C@]4([H])CC[C@]5([H])C[C@@H](O[C@H]6C[C@@H]([C@H]([C@H](C)O6)O)OC)CC[C@]5(C)[C@@]4([H])CC[C@]23C)=C1

For research use only. We do not sell to patients.


Summary

Oleandrin (PBI-05204) inhibits the Na + , K + -ATPase activity with an IC 50 of 620 nM.


IC50 & Target

IC50: 620 nM (Na + , K + -ATPase) [1] .


In Vitro

Study of Na,K-ATPase inhibition shows an IC 50 (nM) of 620 for Oleandrin. The inhibition of Na,K-ATPase by Oleandrin confirms that it likely exert its toxic effect through inhibition of sodium pump activity [1] . When treated with a series of concentrations of Oleandrin (0.2-25 nM), the undifferentiated CaCO-2 cells are sensitive as evidenced by an IC 50 of 8.25 nM. In contrast, a maximum growth inhibition of only 20% is reached in differentiated CaCO-2 cells even though they are treated with Oleandrin concentrations as high as 25 nM [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

The effect of Oleandrin is investigated on glioma growth in vivo. To this aim, SCID or C57BL/6 mice are transplanted, respectively, with human U87MG (5×10 4 ), U251, GBM19 (5×10 5 ), or murine (syngeneic) GL261 (7.5×10 4 ) cells into the right striatum and, after 10 d, treated daily with intraperitoneal Oleandrin for an additional 7 d. Oleandrin significantly reduces tumor sizes in human and murine glioma cell models in vivo in a dose-dependent way. High concentrations of Oleandrin (3 mg/kg) are fatal in both models, as expected from the known lethal dose for rodents. Doses of Oleandrin below the lethal dose (0.3 mg/kg) significantly increase the survival time from 32.6±1.4 d to 53.8±9.6 d in mice injected with U87MG cells (n=5-11; p<0.01, log-rank test) and from 23.37±1.2 d to 34.38±3.3 d (n=5-11; p<0.01, log rank test) in mice injected with GL261 cells [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02329717 Phoenix Biotechnology, Inc
Pancreatic Cancer
April 2015 Phase 2
NCT00554268 M.D. Anderson Cancer Center
Solid Tumors
October 2007 Phase 1

Appearance

Solid



Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 173.39 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7339 mL 8.6697 mL 17.3394 mL
5 mM 0.3468 mL 1.7339 mL 3.4679 mL
10 mM 0.1734 mL 0.8670 mL 1.7339 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Card-20(22)-enolide, 16-(acetyloxy)-3-[(2,6-dideoxy-3-O-methyl-α-L-arabino-hexopyranosyl)oxy]-14-hydroxy-, (3β,5β,16β)-
Oleandrin
(3β,5β,16β)-16-(Acetyloxy)-3-[(2,6-dideoxy-3-O-methyl-α-L-arabino-hexopyranosyl)oxy]-14-hydroxycard-20(22)-enolide
Corrigen
Foliandrin
Folinerin
Oleandrine
Neriol
Neriostene
Neriolin
Oleandrigenin 3-O-α-L-oleandroside

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