溴匹立明

溴匹立明用途

Bropirimine 是 toll 样受体 7 (TLR7) 的合成激动剂。Bropirimine 通过 TLR7 介导 IFN-β 的产生抑制破骨细胞前体细胞向破骨细胞分化。Bropirimine 是一种口服活性免疫调节剂,在膀胱和上尿路的原位移行细胞癌 (CIS) 中具有抗癌活性。

溴匹立明名称

[ CAS 号 ]:
56741-95-8

[ 中文名 ]:
2-氨基-5-溴-6-苯基嘧啶-4-醇

[ 英文名 ]:
Bropirimine

[中文别名 ]:

[英文别名 ]:

4(1H)-pyrimidinone, 2-amino-5-bromo-6-phenyl-
2-Amino-5-bromo-6-phenyl-4(1H)-pyrimidinone
2-Amino-5-bromo-6-phenylpyrimidin-4(1H)-one
4(3H)-pyrimidinone, 2-amino-5-bromo-6-phenyl-
Bropirimine
2-Amino-5-bromo-6-phenylpyrimidin-4-ol
4-Pyrimidinol, 2-amino-5-bromo-6-phenyl-
ABPP
2-amino-5-bromo-6-phenyl-1H-pyrimidin-4-one

溴匹立明生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> Toll样受体(TLR)

研究领域 >> 癌症

[参考文献]

[1]. Suzuki H, et al. Bropirimine inhibits osteoclast differentiation through production of interferon-β. Biochem Biophys Res Commun. 2015;467(1):146‐151.

[2]. Sarosdy MF, et al. Oral bropirimine immunotherapy of bladder carcinoma in situ after prior intravesical bacille Calmette-Guérin. Urology. 1998;51(2):226‐231.

溴匹立明物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
473.2±55.0 °C at 760 mmHg

[ 分子式 ]:
C₁₀H₈BrN₃O

[ 分子量 ]:
266.094

[ 闪点 ]:
240.0±31.5 °C

[ 精确质量 ]:
264.985077

[ PSA ]:
72.03000

[ LogP ]:
1.90

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.696

[ 储存条件 ]:
库房通风低温干燥

溴匹立明MSDS

溴匹立明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UW7351300

CHEMICAL NAME :: 4(1H)-Pyrimidinone, 2-amino-5-bromo-6-phenyl-

CAS REGISTRY NUMBER :: 56741-95-8

BEILSTEIN REFERENCE NO. :: 0651807

LAST UPDATED :: 199703

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C10-H8-Br-N3-O

MOLECULAR WEIGHT :: 266.12

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 910 mg/kg/52W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - hematuria Kidney, Ureter, Bladder - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 7280 mg/kg/52W-I

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Related to Chronic Data - changes in prostate weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2900 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1450 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 200 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 200 mg/kg

SEX/DURATION :: female 5 day(s) after conception

TOXIC 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) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 300 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 252,221,1991

溴匹立明安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H361

[ 警示性声明 ]:
P281

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UW7351300

[ 海关编码 ]:
2933599090

溴匹立明合成路线

溴匹立明海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

溴匹立明文献

CMV specific cytokine release assay in whole blood is optimized by combining synthetic CMV peptides and toll like receptor agonists.

J. Immunol. Methods 414 , 82-90, (2014)

Interferon gamma release assays (IGRAs) are widely used to detect pathogen specific cellular immunity. Cytomegalovirus (CMV) is the foremost problematic viral infection in immunocompromised patients s...

Bropirimine, an orally active anticancer agent for superficial bladder cancer.

Eur. Urol. 34(2) , 107-10, (1998)

To investigate efficacy and safety of bropirimine, a new orally active interferon inducer, in patients with superficial bladder cancer.Twenty patients with histologically confirmed recurrent superfici...

Current and new strategies in immunotherapy for superficial bladder cancer.

Urology 64(3) , 409-21, (2004)

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