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抑制劑描述：

產(chǎn)品名稱：FK-506

產(chǎn)品別名：他克莫司

英文別名：FK-506;Fujimycin;FR900506;FK506;FK 506

靶點：FKBP12

CAS：104987-11-3

純度：>99 %

外觀：見愛必信官網(wǎng)

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Tacrolimus (FK506) 是一種23元大環(huán)內(nèi)酯物，通過結(jié)合到抑免蛋白 FKBP12 (FK506結(jié)合蛋白) 產(chǎn)生新的復(fù)合物，從而降低T細(xì)胞中肽酰脯氨酰異構(gòu)酶活性。

FK-506和環(huán)孢霉素A阻斷細(xì)胞質(zhì)成分的移位，而不影響T淋巴細(xì)胞中核亞基的合成。FK-506通過抑制需要白細(xì)胞介素-2轉(zhuǎn)錄誘導(dǎo)的Ca(2+)-依賴過程，阻止T細(xì)胞增殖。FK-506結(jié)合于不同的細(xì)胞內(nèi)蛋白質(zhì)(免疫親和素)家族，學(xué)術(shù)上稱為親環(huán)素類和FK 506結(jié)合蛋白(FKBPs)。FK-506特異性抑制細(xì)胞內(nèi)磷酸酶，在藥物濃度下，抑制活化的T細(xì)胞中白介素2的產(chǎn)生。FK-506和CsA通過抑制早期鈣相關(guān)的涉及淋巴因子表達(dá)，凋亡，和脫粒作用，在細(xì)胞中幾乎發(fā)揮相同的生物學(xué)作用。FK-506與細(xì)胞內(nèi)受體家族結(jié)合，學(xué)術(shù)上稱為FK-506結(jié)合蛋白(FKBPs)。

溶解性：DMSO：94 mg/mL (116.91 mM)
Ethanol：83 mg/mL (103.23 mM)

體外研究：

FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. FK-506 and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs).

體內(nèi)研究：FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in rats. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R).

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