Oligomycin A 化学構造
分子量: 791.06

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製品説明

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製品の説明

生物活性

製品説明 Oligomycin Aは、 複雑なV (ATP シンターゼ)の特定の 電子伝達チェーンの阻害剤です。
ターゲット ATP synthase
IC50 [1]
In vitro試験 Oligomycin A is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.Oligomycin A inhibits ATP synthase by blocking its proton channel (Fo subunit), which is necessary for oxidative phosphorylation of ADP to ATP. The inhibition of ATP synthesis by oligomycin A will significantly reduce electron flow through the electron transport chain; however, electron flow is not stopped completely due to a process known as proton leak or mitochondrial uncoupling. [1] In a group of cancer cells, Oligomycin at 100 ng/ml completely inhibits oxidative phosphorylation activity in 1 h and induces various levels of glycolysis gains by 6 h. [2] Oligomycin, inhibitor of the F0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis. [3] Oligomycin inhibits mitochondrial respiration in melanoma, sensitizes melanoma cells to therapy, blocks the emergence of the slow-cycling, long-term tumor-maintaining melanoma cells. [4]
In vivo試験
臨床試験
特集

プロトコル (参考用のみ)

細胞アッセイ: [2]

細胞株 H1229
濃度 100 ng/ml
反応時間 1 h
実験の流れ ATP and Oligomycin Dose-Response Growth Measurement. Cellular ATP changes are measured by CellTiter-Glo reagent. To measure oligomycin dose-response curves, the cells are plated in 96-well plates at about 400–500 cells/well in 100 μl of culture, dosed the next day, and grown for 4 additional days followed by assaying with Cell-Titer-Glo reagent. The dose-response curves are plotted with nonlinear regression analysis of GraphPad Prism.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Oligomycin A SDF
分子量 791.06
化学式

C45H74O11

CAS No. 579-13-5
保管 2年-20℃
6月-80℃in solvent
別名 MCH 32
溶解度 (25°C) * In vitro DMSO 10 mg/mL (12.64 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 15 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 Spiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2'-[2H]pyran]-3,9,13-trione, 22-ethyl-3',4',5',6'-tetrahydro-7,11,14,15-tetrahydroxy-6'-[(2R)-2-hydroxypropyl]-5',6,8,10,12,14,16,28,29-nonamethyl-, (1R,2'R,4E,5'S,6S,6'S,7R,8S,10R,11R,12S,14R,15S,16R,18E,20E,22R,25S,28S,29R)-

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