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53910-25-1

53910-25-1结构式
53910-25-1结构式

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中文名 喷司他丁
英文名 pentostatin
中文别名 脱氧助间型霉素
英文别名 Nipent
DCF
yk-176
(R)-3-(2-Deoxy-b-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydro-, (R)-
Imidazo[4,5-d][1,3]diazepin-8-ol, 3- (2-deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydro-, (R)-
(8R)-3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)-
deoxycoformycin
2'-deoxy-D-coformycin
Pentostatin
2'-deoxycoformycin
(R)-3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo(4,5-d)(1,3)diazepin-8-ol
Cl 825
CO-Vidarabine
Co-V
ci-825
Imidazo[4,5-d][1,3]diazepin-8-ol, 3- (2-deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8- tetrahydro-, (R)-
(8R)-3-[(2R,4S,5R)-4-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydro-, (8R)-
PD-ADI
Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)-
(8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxyméthyl)tétrahydrofuran-2-yl]-3,6,7,8-tétrahydroimidazo[4,5-d][1,3]diazépin-8-ol
Coforin
描述 Pentostatin 是一种高效,不可逆的腺苷脱氨酶抑制剂,Ki 值为 2.5 pM。
相关类别
靶点

Ki: 2.5 pM (adenosine deaminase)

体内研究 在ECP和Pentostatin(4 mg/m2,iv)治疗中,所有狗从第4天开始出现<500粒细胞/μL的粒细胞减少症。血小板减少症(<20,000血小板/μL)从HCT后第7天发生,最低点为3000至14000个血小板/ μL[1]。 Pentostatin(2 mg/kg)与虫草素(2 mg/kg)组合在感染T. evansi的小鼠中100%有效。一些生化参数的水平增加,尤其是肝酶,其伴随着肝脏和肾脏中的组织学损伤。 Pentostatin单独对感染组没有疗效[2]。
动物实验 使用线性加速器以7cGy /分钟通过920cGy TBI对所有受体狗进行移植。组A1中的狗接受ECP在第-2天和第-1天施用,第0天施用TBI,第A2组中的狗在第-6和第5天接受ECP,静脉内(IV)以4mg / m 2的剂量静脉注射戊糖素 - 天数 - 在第0天,来自DLA-非同一供体的供体骨髓细胞在全身麻醉下通过插入肱骨和股骨的针吸出,并在4℃下储存在肝素化组织培养基中不超过6小时。在TBI的4小时内,将收获的骨髓细胞IV输注到受体,中位剂量为2.9(范围,1.9至6.1)×108总有核细胞(TNC)/ kg。骨髓移植的日期被指定为第0天。除了骨髓移植之外,在第1天和第2天,通过白细胞分离术从骨髓供体获得的外周血血沉棕黄层细胞的IV输注,中位剂量为2.3(范围, 1.2至6.9)×108 TNC / kg,以确保一致的造血植入。静脉注射0.4mg / kg剂量的MTX用作移植后免疫抑制,并在第+1天,+ 3天,+ 6天和+11天施用,然后每周一次直至第102天。
参考文献

[1]. Bethge WA, et al. Extracorporeal photopheresis combined with pentostatin in the conditioning regimen for canine hematopoietic cell transplantation does not prevent GVHD. Bone Marrow Transplant. 2014 Sep;49(9):1198-204.

[2]. Dalla Rosa L, et al. Cordycepin (3'-deoxyadenosine) pentostatin (deoxycoformycin) combination treatment of mice experimentally infected with Trypanosoma evansi. Parasitology. 2013 Apr;140(5):663-71.

密度 1.8±0.1 g/cm3
沸点 673.1±65.0 °C at 760 mmHg
熔点 220-225ºC
分子式 C11H16N4O4
分子量 268.269
闪点 360.9±34.3 °C
精确质量 268.117157
PSA 112.13000
LogP -2.16
外观性状 白色晶体
蒸汽压 0.0±2.2 mmHg at 25°C
折射率 1.793
储存条件 -20°C
分子结构

1、 摩尔折射率:62.65

2、 摩尔体积(cm3/mol):147.4

3、 等张比容(90.2K):444.2

4、 表面张力(dyne/cm):82.3

5、 极化率(10-24cm3):24.83

更多

1.性状:从甲醇-水得白色结晶

2.熔点(ºC):220~225

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NI2931000
CHEMICAL NAME :
Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-beta-D-pentofuranosyl)-3,6,7,8-tetrahydro- , (R)-
CAS REGISTRY NUMBER :
53910-25-1
LAST UPDATED :
199703
DATA ITEMS CITED :
23
MOLECULAR FORMULA :
C11-H16-N4-O4
MOLECULAR WEIGHT :
268.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
390 mg/kg/3D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - thrombocytopenia Blood - other hemolysis with or without anemia
REFERENCE :
IEDIEP Internal Medicine. (The Japanese Society of Internal Medicine, 34-3, 3-chome, Hongo, Bunkyo-ku, Tokyo 113, Japan) V.31- 1992- Volume(issue)/page/year: 34,593,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
227 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - hematuria Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,7888,1990
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
122 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB84-211424
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
360 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,7888,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
650 mg/kg/26W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Endocrine - other changes Blood - changes in bone marrow (not otherwise specified)
REFERENCE :
TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 22,519,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
80 mg/kg/4W-I
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - changes in lung weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
CCPHDZ Cancer Chemotherapy and Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1978- Volume(issue)/page/year: 5,83,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
18200 ug/kg/26W-C
TOXIC EFFECTS :
Blood - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4277,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
28 mg/kg/4W-I
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in leukocyte (WBC) count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,1271,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
91 ug/kg/26W-C
TOXIC EFFECTS :
Blood - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4277,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
14 mg/kg/4W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,1271,1991 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
7500 ug/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 44,325,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
7500 ug/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - sex ratio
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 44,325,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
500 ug/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow) Reproductive - Specific Developmental Abnormalities - immune and reticuloendothelial system
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 25(2),36A,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
5 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 40,615,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
1 mg/kg
SEX/DURATION :
female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 45,91,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
5 mg/kg
SEX/DURATION :
female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 47,17,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
5 mg/kg
SEX/DURATION :
female 7 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 47,17,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
5 mg/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3977,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
8300 ug/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3965,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
8300 ug/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 6 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3965,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
28 ug/kg
SEX/DURATION :
female 15-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4329,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
28 ug/kg
SEX/DURATION :
female 15-21 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4329,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
1300 ug/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Fertility - abortion Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,4319,1991

符号 GHS06
GHS06
信号词 Danger
危害声明 H301
警示性声明 P301 + P310
危害码 (欧洲) Xn
风险声明 (欧洲) 22
危险品运输编码 UN 2811 6.1 / PGIII
海关编码 2934999090
上游产品  4

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大规模生产以喷妥司汀的产生菌Streptomyces antibioticus进行浸入或深层培养来制备:
一、发酵
经选择的培养基植入灭过菌的水溶性营养液,在无菌条件下,于20~45℃(最好是33~40℃),充气和搅拌培育,直至培养液中出现喷妥司汀。影响获得最大收率的时间的长短的因素是所用设备的类型和大小、搅拌的速度,充气的速度,微生物培养基和其它因素。在罐形发酵器中进行的大
规模工业发酵,进行3~7d最大收率。也可采用较短的发酵时间,但收率较低。当在振荡瓶进行发酵时,所需的时间比用大容积的发酵罐的时间要长。
在浸入培养时,微生物生长成分布于整个营养液的不连续的颗粒;而在表面培养时,是在营养液的表面形成连续的薄膜。由于微生物分布在整个营养液中,因而在采用发酵工业中使用的罐和缸进行微生物培养时,可以采用大容积的接种营养液。装有搅拌和充气装置的连续缸形发酵器特别适合大规模生产,但也可以使用其它发酵设备。在小量生产或制备用于大规模发酵的微生物培养基时,浸入培养可在小烧瓶中进行,可以采用适合的方法进行振荡或搅拌。在浸入培养时,培养液的充气和搅拌可用许多方式来完成。搅拌可用涡轮机、桨状搅拌器、叶轮推进器等其它机械搅拌设备,也可旋转或振荡发酵器本
身,或用各种泵设备往营养液中注入空气或氧气而获得。充气可采用开口管、多孔管或带有分配器的管子来注入空气或氧气,或可将营养液喷、泼或溢到氧气气氛中。浸入培养外的另一选择方法是表面培养。此时使用2CM以下薄层的灭过菌的水溶性培养液,植入喷妥司汀的产生菌犛狋狉犲狆狋狅犿狔犲狊犪狀狋犻犫犻狅狋犻犮狌狊,在20~45℃和充氧下进行培育。和浸入培养相似可得产品。
二、分离和提纯
分离可采用压滤或离心分离。滤饼用水彻底洗涤,洗液和滤液合并后,用氢氧化钠、三乙胺或氢氧化铵等碱性水溶液调狆犎值至约9.2。减压浓缩至约剩1/10的体积。浓缩液冷至5℃,时间可在数小时或数天(依据体积大小而定)。
析出的沉淀是9-(B-D-阿拉伯糖基呋喃糖基)腺嘌呤,可用硅藻土作助滤剂过除去。滤液用水稀释至其浓缩前的体积,然后用盐酸或硫酸等水溶性酸调狆犎值至约8.3。用活性炭或其它吸附剂(最好是Darco G-60)来吸附。吸附过程可分批进行,也可通过柱子连续进行。
在批量方法中,把0.5%~10%,最好是约3%(W/V)的活性炭加入滤液,并搅拌1~3h。过滤,滤饼用水洗后,再用丙酮水溶液等量的丙酮和水洗脱。洗脱液浓缩至剩约1%~3%的体积。往浓缩液中加入甲醇,以获得80%甲醇溶液。过滤除去产生的沉淀,滤液浓缩以除去甲醇。浓缩液用5%丙酮的水溶液稀释至其2.5倍的体积,通过一活性炭柱子。该活性炭柱先用5%丙酮水溶液洗,再用10%丙酮水溶
液洗。然后用25%丙酮水溶液洗脱。洗脱液减压浓缩后冻干。将干燥固体溶于小量水中,通过用水制备的装有Sephadex G-10的柱子进行渗滤。用水洗柱子,收集含产品的流出液,干燥,用甲醇水溶液结晶,可得喷司他丁。


海关编码 2934999090
中文概述 2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素 品名, 成分含量, 用途
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%