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他克莫司一水合物

他克莫司一水合物 更多供应商
公司名称: 北京迈索化学技术有限公司  黄金产品
联系电话: 18811083386
产品介绍: 中文名称:他克莫司一水合物
英文名称:Tacrolimus monohydrate
CAS:109581-93-3
纯度:99% 备注:铝箔袋/西林瓶/纸板桶
公司名称: 上海默凯医药科技有限公司  黄金产品
联系电话: 18601606476 021-60951261
产品介绍: 中文名称:他克莫司(一水)
英文名称:TACROLIMUS
CAS:109581-93-3
纯度:99% 包装信息:2kg
公司名称: 上海慧风生物科技有限公司  黄金产品
联系电话: 18116461626 021-54285032
产品介绍: 中文名称:他克莫司
英文名称:Tacrolimus
CAS:109581-93-3
纯度:>98% 包装信息:1g;10g;100g; 1kg;10kg;100kg
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 中文名称:他克莫司
英文名称:TACROLIMUS
CAS:109581-93-3
公司名称: 北京百灵威科技有限公司  
联系电话: 400-666-7788 010-82848833
产品介绍: 中文名称:他克莫司一水合物
英文名称:Tacrolimus monohydrate, 98%
CAS:109581-93-3
纯度:98% 包装信息:100MG;25MG 备注:化学试剂、精细化学品、医药中间体、材料中间体
他克莫司一水合物生产厂家及价格列表
他克莫司一水合物_沭阳羽清医药科技有限公司
价格:询价
2021/08/02 15:30:08
他克莫司一水合物_湖北威德利化学科技有限公司
价格:询价
2021/08/02 14:36:07
他克莫司一水合物
生物活性靶点体外研究体内研究 MSDS 用途与合成方法 他克莫司一水合物价格(试剂级) 上下游产品信息
中文名称:他克莫司一水合物
中文同义词:他克莫司一水合物;FK-506一水合物;他克莫司,一水;他克莫司水合物;他克莫司 USP标准品
英文名称:TACROLIMUS
英文同义词:FK-506;15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-, monohydrate, [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-;TACROLIMUS HYDRATE/TSUKUBAENOLIDE HYDRATE;(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone;Tacrolimus (150 mg);(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-Methoxycyclohexyl]-1-Methylethenyl]-14,16-diMethoxy-4,10,12,18-tetraMethyl-8-(2-propen-1-yl)-;Tacrolimus monohydrate;FK-506 monohydrate, >=98%
CAS号:109581-93-3
分子式:C44H69NO12
分子量:822.04
EINECS号:
相关类别:他克莫司杂质;医用原料;发酵类;医药原料;化学连接;原料药;抗生素;Signalling
Mol文件:109581-93-3.mol
他克莫司一水合物
他克莫司一水合物 性质
熔点 127-129°
比旋光度 D23 -84.4° (c = 1.02 in chloroform)
储存条件 −20°C
溶解度 DMSO: soluble20mg/mL
形态powder
Merck 14,9025
InChIKeyNWJQLQGQZSIBAF-MLAUYUEBSA-N
他克莫司一水合物 用途与合成方法
生物活性Tacrolimus monohydrate (FK506 monohydrate) 是大环内酯类化合物,Tacrolimus monohydrate 与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶 (calcineurin phosphatase),从而抑制 T 淋巴细胞信号转导和 IL-2 转录。具有强免疫抑制特性。
靶点

PP2B (calcineurin phosphatase)
Autophagy inducer

体外研究

Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) 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 (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/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%).

安全信息
危险品标志 T
危险类别码 25
安全说明 45
危险品运输编号 UN 2811 6.1/PG 3
WGK Germany 3
RTECS号KD4201200
HazardClass 6.1
PackingGroup III
海关编码 2934990002
毒性LD50 i.p. in mice: >200 mg/kg (Kino); LD50 in male, female rats (mg/kg): 57.0, 23.6 i.v.; 134, 194 orally (Ohara)
他克莫司一水合物 价格(试剂级)
更新日期产品编号产品名称CAS编号包装价格
2021/01/25M2258他克莫司 一水合物
Tacrolimus Monohydrate
109581-93-310mg1320元
2021/01/25M2258他克莫司 一水合物
Tacrolimus Monohydrate
109581-93-350mg4740元
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