Tacrolimus (FK506)

別名: FR900506, Fujimycin 中文名稱：他克莫司

目錄號(hào)：S5003 Purity: 99.97%

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。Tacrolimus 也可抑制calcineurin鈣調(diào)磷酸酶的磷酸酶活性。Tacrolimus 可誘導(dǎo)血管內(nèi)皮細(xì)胞的自噬。

Tacrolimus (FK506) Chemical Structure

CAS: 104987-11-3

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1137.06	現(xiàn)貨
50mg	744.25	現(xiàn)貨
500mg	3538.67	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.97%

99.97

Tacrolimus (FK506)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	FKBP1 FKBP12	點(diǎn)擊展開
相關(guān)產(chǎn)品	Shield-1 AP20187	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細(xì)胞周期化合物庫 NF-κB信號(hào)通路庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
rat RBL2H3 cells	Function assay	15 mins	Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA, IC50=0.25 nM	22410084
rat RBL2H3 cells	Function assay	16 h	Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA, IC50=0.25 nM	23791076
Jurkat T	Immunosuppressive assay	15 to 30 mins	Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA, IC50 = 0.36 μM.	28412204
Jurkat T	Antiinflammatory assay	20 mins	Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA, IC50 = 5.8 μM.	28509552
human T-cell	Proliferation assay		In vitro inhibitory activity against human T-cell proliferation, IC50=0.5 nM	7537331
human WiDr cells	Growth inhibition assay		Inhibition of SAP130 mediated cell growth in human WiDr cells, IC50=10.9 nM	17643112
human U251 cells	Function assay		Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay, IC50=13.8 nM	17643112
PBMCs	Function assay		Inhibitory activity against IFN-gamma production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM.	15369399
PBMCs	Function assay		Inhibitory activity against IL-5 production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM.	15369399
T-cells	Function assay		The compound was tested for its inhibitory activity against T-cell proliferation using murine splenic T-cells, IC50 = 0.0002 μM.	10450987
RBL-2H3	Function assay		Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells, IC50 = 0.00025 μM.	16901696
HEK293	Function assay		TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, IC50 = 3.7 μM.	14530907
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生物活性

產(chǎn)品描述

靶點(diǎn)

FKBP12 ^[1]
(T cells)

calcineurin ^[6]

體外研究(In Vitro)
體外研究活性	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。^[1] 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。^[2] 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。^[3] 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)。^[4]
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 p-S6K(S371) / S6K / p-Erα(S167) / Erα		26455952
	Immunofluorescence	FKBP52 / p23 / hsp90 FKBP51 Tom20 / JC-1 / ROS / NF-κB		20796173
	Growth inhibition assay	Cell viability		23470533

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	大鼠行為疼痛評估中，F(xiàn)K-506導(dǎo)致痛覺過敏和異常疼痛刺激下爪子和尾巴收縮的閾值增加。在大鼠體內(nèi)，F(xiàn)K-506也會(huì)導(dǎo)致血清硝酸鹽和硫代巴比妥酸活性產(chǎn)物(TBARS)水平降低，并伴隨組織髓過氧化物酶(MPO)和總鈣水平降低，然而，會(huì)升高組織中還原型谷胱甘肽的水平。在缺血再灌注損傷(I/R)的大鼠體內(nèi)，F(xiàn)K-506可以改善加重的神經(jīng)水腫和軸突變性。^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05702931	Not yet recruiting	Hyperglycemia\|Renal Transplant Complication Primary Non-Function\|Diabetes	Rigshospitalet Denmark\|Aarhus University Hospital\|Odense University Hospital	April 1 2024	Phase 4
NCT06268769	Recruiting	Immunosuppression	Edward Geissler\|Chiesi Pharmaceuticals GmbH\|University of Regensburg	March 9 2024	Phase 4
NCT06326775	Active not recruiting	Heart Transplant Patients	Nanjing First Hospital Nanjing Medical University\|Wuhan Union Hospital China\|Changhai Hospital\|Shanghai Zhongshan Hospital	March 12 2024	--
NCT06235892	Not yet recruiting	Organ Grafts	Nantes University Hospital	February 10 2024	Phase 3

參考文獻(xiàn)
[1] Flanagan WM, et al. Nature, 1991, 352(6338), 803-807. [2] S J O Keefe, et al. Nature . 1992 Jun 25;357(6380):692-4. [3] Fruman DA, et al. Proc Natl Acad Sci U S A, 1992, 89(9), 3686-3690. [4] Wiederrecht G, et al. Ann N Y Acad Sci, 1993, 696, 9-19. [5] Muthuraman A, et al. J Brachial Plex Peripher Nerve Inj, 2010, 5, 13. [6] Ikuko Yano. Drug Metab Pharmacokinet . 2008;23(3):150-7. [7] X-S Xu, et al. Eur Rev Med Pharmacol Sci . 2018 May;22(10):3199-3206. [8] Okada Y, et al. Biol Pharm Bull.?2011;34(12):1823-7. + 展開

參考文獻(xiàn)

[1] Flanagan WM, et al. Nature, 1991, 352(6338), 803-807.
[2] S J O Keefe, et al. Nature . 1992 Jun 25;357(6380):692-4.
[3] Fruman DA, et al. Proc Natl Acad Sci U S A, 1992, 89(9), 3686-3690.

[4] Wiederrecht G, et al. Ann N Y Acad Sci, 1993, 696, 9-19.
[5] Muthuraman A, et al. J Brachial Plex Peripher Nerve Inj, 2010, 5, 13.
[6] Ikuko Yano. Drug Metab Pharmacokinet . 2008;23(3):150-7.
[7] X-S Xu, et al. Eur Rev Med Pharmacol Sci . 2018 May;22(10):3199-3206.
[8] Okada Y, et al. Biol Pharm Bull.?2011;34(12):1823-7.

+ 展開