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109581-93-3

中文名稱 他克莫司一水合物
英文名稱 TACROLIMUS
CAS 109581-93-3
分子式 C44H69NO12
分子量 822.04
MOL 文件 109581-93-3.mol
更新日期 2024/12/23 11:22:48
109581-93-3 結(jié)構(gòu)式 109581-93-3 結(jié)構(gòu)式

基本信息

中文別名
他克莫司水合物
他克莫司,一水
他克莫司一水合物
FK-506一水合物
他克莫司 USP標(biāo)準(zhǔn)品
英文別名
FK-506
135175
CS-1308
Tacarolimus
[3R[E(1S,3S,4S)
tacrolimushydrate
FK-506 MONOHYDRATE
Tacrolimus (150 mg)
FR900506 monohydrate
tsukubaenolidehydrate
所屬類別
生物化工:免疫抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)127-129°
比旋光度D23 -84.4° (c = 1.02 in chloroform)
儲(chǔ)存條件−20°C
溶解度DMSO:可溶,20mg/mL
形態(tài)粉末
顏色白色到近乎白色
Merck14,9025
InChIKeyNWJQLQGQZSIBAF-MLAUYUEBSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301
防范說明P301+P310+P330
危險(xiǎn)品標(biāo)志T
危險(xiǎn)類別碼25
安全說明45
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1/PG 3
WGK Germany3
RTECS號(hào)KD4201200
危險(xiǎn)等級(jí)6.1
包裝類別III
海關(guān)編碼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)

常見問題列表

生物活性
Tacrolimus monohydrate (FK506 monohydrate) 是大環(huán)內(nèi)酯類化合物,Tacrolimus monohydrate 與 FK506 結(jié)合蛋白 (FKBP) 結(jié)合形成復(fù)合物并抑制鈣調(diào)神經(jīng)磷酸酶 (calcineurin phosphatase),從而抑制 T 淋巴細(xì)胞信號(hào)轉(zhuǎn)導(dǎo)和 IL-2 轉(zhuǎn)錄。具有強(qiáng)免疫抑制特性。
靶點(diǎn)

PP2B (calcineurin phosphatase)
Autophagy inducer

體外研究

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).

體內(nèi)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%).

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