他克莫司 - CAS:109581-93-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	他克莫司促销
英文名称:	Tacrolimus
别名:	他克莫司一水合物 FK-506 monohydrate FR900506 LCP-Tacro
CAS No:	109581-93-3	分子式:	C₄₄H₆₉NO₁₂^.H₂O	分子量:	822.03
CAS No:	109581-93-3
分子式:	C₄₄H₆₉NO₁₂^.H₂O
分子量:	822.03
MDL:	MFCD11045918

安全技术说明书(PDF) MSDS(PDF) 点击下载技术规格说明书(PDF) 点击下载产品说明书(PDF)

F10032 他克莫司 ≥98% (psaitong)

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包装规格：

25mg 100mg 1g in glass bottle

溶解性：

溶于DMSO(20mg/mL)

产品描述：

基本信息

产品编号：F10032
产品名称：Tacrolimus
CAS:	109581-93-3	储存条件	粉末	-20℃	四年
分子式：	C44H69NO12.H2O		溶于液体	-80℃	两年
分子量	822.03			-20℃	一个月
化学名：	(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone;hydrate
Solubility (25°C)	体外	DMSO	100mg/mL (124.37mM)
		Ethanol	100mg/mL (124.37mM)
		Water	Insoluble
	体内（现配现用）	5% DMSO+corn oil	15mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.2438mL	6.2188mL	12.4375mL
5mM	0.2488mL	1.2438mL	2.4875mL
10mM	0.1244mL	0.6219mL	1.2438mL
50mM	0.0249mL	0.1244mL	0.2488mL

生物活性

产品描述	一种大环内酯物，可结合到FK506结合蛋白(FKBP)形成复合体，从而降低T细胞中肽酰脯氨酰异构酶活性。
靶点/IC₅₀	FKBP12 (T cells)	calcineurin ()
体外研究	Tacrolimus (FK506) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus. Treatment with a low concentration of Tacrolimus (FK506,10μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus(100-1,000μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased(P<0.01).
体内研究	The therapeutic effect of Tacrolimus is investigated on progression and perpetuation of colitis by administering Tacrolimus to Dextran sulfate sodium (DSS)-treated mice from Days 10 to 16 or to 23. At Days 17 and 24, colon length is significantly shortened, and colon weight is significantly higher in DSS-treated control animals than in normal animals. In addition, colon weight per unit length in the control group is more than twice that in the normal group. While both 7 and 14 d treatment with Tacrolimus significantly suppresses increases in colon weight per unit length in DSS-treated animals compared with the control group, this treatment does not actually restore the colon shortening. In addition, this inhibitory effect of Tacrolimus on increases in colon weight per unit length is more pronounced with 14-d than 7-d treatment, as shown by the inhibitory percentages (59% vs. 28%).

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

Tumor cell proliferation is determined by the MTT assay. Briefly, after MH3924A cells have reached the logarithmic growth phase, a 0.2-mL cell suspension at 1×104 cells/mL is added into each well of a 96-well plate and cultured in DMEM for 24h.When adherent growth is established, different concentrations of Tacrolimus (10, 100 and 1,000μg/L) , AMD3100 (10, 50 and 100μg/L) and Tacrolimus (0 and 100μg/L)+AMD3100 (0, 10, 50 and 100μg/L) are added into the plates. Untreated cells cultured in medium alone are used as controls. After culturing for 48 h, 10μL MTT (5 g/L) are added, and each well is incubated for 6 h; next, 150μL/well DMSO are added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well is measured three times, and each sample is assayed in triplicate.

动物实验:

Animal Administration

Mice

Six-week-old male C57BL/6J mice are maintained in a temperature- and humidity-controlled room with a 12-h light-dark cycle. For the multiple dosing study, colitic mice (n=10) are orally administered Tacrolimus at 30 mg/kg for 7 d (Days 10 to 16) or 14 d (Days 10 to 23). Control (n=10) and normal groups (n=5) are administered placebo using the same regimen.Tacrolimus or placebo is administered at 10mL/kg. Mice are euthanized by CO2 inhalation on the day following the final dosing. For the single dosing study, colitic mice are orally administered Tacrolimus at 30 mg/kg or placebo (n=8) once on Day 7, 10, 17, or 24. Normal mice (n=4) are administered placebo using the same regimen. Mice are euthanized by CO2 inhalation eight hours after dosing.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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