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化合物简介

Tacrolimus (also FK-506 or fujimycin, trade names Prograf, Advagraf, Protopic) is an immunosuppressive drug used mainly after allogeneic organ transplant to lower the risk of organ rejection. It achieves this by inhibiting the production of interleukin-2, a molecule that promotes the development and proliferation of T cells, which are vital to the body's learned (or adaptive) immune response. Tacrolimus is also used in the treatment of other T cell-mediated diseases such as eczema (for which it is applied to the skin in a medicated ointment), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, Kimura's disease, and the skin condition vitiligo.

基本信息

CAS:104987-11-3
中文别名:藤霉素;
英文别名:fujimycin;Prograf;Advagraf;Protopic;FK-506;3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*-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)-15,19-epoxy-3H-pyrido[2,1-c] [1,4] oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, monohydrate;
分子式:C44H69NO12
分子量:804.018
精确质量:803.482
Psa:178.36
Logp:4.5769

编号系统

PubChem号:24724482
RTECS号:KD4201200

物化性质

外观与性状:白色或灰白色结晶粉末
密度:1.19 g/cm3
沸点:871.7ºC at 760 mmHg
熔点:113-115°C
闪点:481ºC
折射率:1.549
储存条件:-20ºC
蒸汽压:1.73E-35mmHg at 25°C

安全信息

RTECS号:KD4201200
安全说明:45-36-26
WGK Germany:3
危险类别码:R25; R36/37/38
危险品运输编码:UN 2811 6.1/PG 3
危险品标志:Xi; T

生产方法及用途

生产方法
含1%甘油,1%玉米淀粉,0.5%葡萄糖,1%棉子粉,0.5%玉米浸渍液和0.2%碳酸钙,pH=6 治疗肝脏或肾脏移植术后应用其他免疫抑制药物无法控制的移植物排斥反应。现已作为预防、治疗排斥反应以及自身免疫性肝炎的一线药物。
用途
治疗肝脏或肾脏移植术后应用其他免疫抑制药物无法控制的移植物排斥反应。现已作为预防、治疗排斥反应以及自身免疫性肝炎的一线药物。

合成路线

上游原料

下游产品

图谱

Predict 1H proton NMR


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