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野百合碱

野百合碱用途

Monocrotaline是从猪屎豆植物的种子提取的吡咯里西啶生物碱,用于在啮齿动物中诱导肺动脉高血压。
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野百合碱名称

[ CAS 号 ]:
315-22-0

[ 中文名 ]:
野百合碱

[ 英文名 ]:
Monocrotaline

[中文别名 ]:

[英文别名 ]:

野百合碱生物活性

[ 描述 ]:

Monocrotaline是从猪屎豆植物的种子提取的吡咯里西啶生物碱,用于在啮齿动物中诱导肺动脉高血压。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他
天然产物 >> 其他
研究领域 >> 代谢疾病

[体外研究]

野百合碱(MCT)是一种11元大环吡咯里西啶生物碱(PA),来源于猪屎豆(Crotalaria spectabilis)植物的种子[1]。野甘露碱是一种天然配体,具有剂量依赖性细胞毒性,具有强大的抗肿瘤活性。野百合碱的体外细胞毒性证实为IC50为24.966μg/ mL,2 X IC50对HepG2细胞的遗传毒性[2]。

[体内研究]

MCT引起大鼠肺血管综合征,其特征为增殖性肺血管炎,肺动脉高压(PH)和肺心病[3]。在肺动脉高压(PAH)的临床前模型中,野百合碱动物模型提供了模拟人PAH几个关键方面的优势,包括血管重塑,平滑肌细胞增殖,内皮功能障碍,炎性细胞因子上调和右心室衰竭,需要单次注射药物[4]。通过注射野百合碱观察到与PH发展相关的多种途径的变化,包括活化的糖酵解,增加的增殖标记,肉毒碱稳态的破坏,炎症和纤维化生物标志物的增加以及谷胱甘肽生物合成的减少[5]。

[溶解度]

体外:

DMSO:37.5 mg / mL(115.26 mM;需要超声波)

体内:1。逐个添加每种溶剂:10%DMSO 90%玉米油溶解度:≥2.5mg / mL(7.68 mM);澄清溶液2.逐个添加每种溶剂:10%DMSO 90%(20%SBE-β-CD在盐水中)溶解度:≥2.5mg/ mL(7.68mM);澄清溶液3.逐个添加每种溶剂:10%DMSO 40%PEG300 5%吐温-80 45%盐水溶解度:≥2.5mg/ mL(7.68mM);明确解决方案

[储备液]

1 mM 3.0735 mL 15.3676 mL 30.7352 mL
5 mM 0.6147 mL 3.0735 mL 6.1470 mL
10 mM 0.3074 mL 1.5368 mL 3.0735 mL

[动物实验]

大鼠:在该研究中使用总共20只雄性Sprague Dawley大鼠(SD; 220-270g)(每组n = 10)。对照组接受野百合碱(MCT)的载体。肺动脉高压前期(PH)组单次注射MCT(60 mg / kg ip)诱导并在14天后处死[5]。

[存储]

粉末 -20°C 3年
  4°C 2年
在溶剂中 -80°C 6月
  -20°C 1月

[运输]

室温;可能会有所不同

[SMILES]

O=C(O[C@]1([H])CCN2[C@]1([H])C(CO3)=CC2)[C@H](C)[C@@](C)(O)[C@@](C)(O)C3=O

[参考文献]

[1]. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012 Feb 15;302(4):L363-9.

[2]. Kusuma SS, et al. Antineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem. 2014;14(9):1237-48.

[3]. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22(5-6):307-25.

[4]. Nogueira-Ferreira R, et al. Exploring the monocrotaline animal model for the study of pulmonary arterial hypertension: A network approach. Pulm Pharmacol Ther. 2015 Dec;35:8-16.

[5]. Rafikova O,et al. Metabolic Changes Precede the Development of Pulmonary Hypertension in the Monocrotaline Exposed RatLung. PLoS One. 2016 Mar 3;11(3):e0150480.


[相关活性小分子]

磺丁基-β-环糊精 | 环孢菌素A | 2',7'-二氯荧光素二乙酸酯 | 1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐 | 4',4''-双-2-咪唑啉-2-基对苯二丙烯酰苯胺二盐酸盐 | 乙莫克舍 | TD139 | Mitoquinone甲磺酸盐 | GSK2795039 | JC-1 | 胞内钙荧光探针 BAPTA-AM | AP20187 | GKT137831 | D-荧光素 | BPTES

[相关文档]

*以上文档由Medchemexpress提供,仅用于科学研究参考。

野百合碱物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
537.3±50.0 °C at 760 mmHg

[ 熔点 ]:
204ºC (dec.)(lit.)

[ 分子式 ]:
C16H23NO6

[ 分子量 ]:
325.357

[ 闪点 ]:
278.7±30.1 °C

[ 精确质量 ]:
325.152527

[ PSA ]:
96.30000

[ LogP ]:
-0.37

[ 外观性状 ]:
白色至淡黄褐色的粉末

[ 蒸汽压 ]:
0.0±3.2 mmHg at 25°C

[ 折射率 ]:
1.586

野百合碱MSDS

野百合碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QB3140000
CHEMICAL NAME :
Monocrotaline
CAS REGISTRY NUMBER :
315-22-0
BEILSTEIN REFERENCE NO. :
0048732
LAST UPDATED :
199612
DATA ITEMS CITED :
44
MOLECULAR FORMULA :
C16-H23-N-O6
MOLECULAR WEIGHT :
325.40
WISWESSER LINE NOTATION :
T55 AN CUTJ FQ D1OV1- ET5OVTJ C1 D1 EQ

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 :
66 mg/kg
TOXIC EFFECTS :
Liver - hepatitis (hepatocellular necrosis), diffuse
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
130 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - other changes Liver - other changes
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
60 mg/kg
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
92 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
60 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
259 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
261 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Mammal - species unspecified
DOSE/DURATION :
60 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 :
61600 ug/kg/28D-C
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - changes in lung weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other oxidoreductases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
18 mg/kg/10D-C
TOXIC EFFECTS :
Cardiac - changes in heart weight Lungs, Thorax, or Respiration - changes in lung weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
75600 ug/kg/3W-C
TOXIC EFFECTS :
Vascular - BP elevation not characterized in autonomic section Lungs, Thorax, or Respiration - changes in lung weight Cardiac - changes in heart weight
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
288 mg/kg/48W-I
TOXIC EFFECTS :
Vascular - thrombosis distant from injection site Blood - hemorrhage Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1050 mg/kg/14D-I
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in spleen weight Blood - changes in leukocyte (WBC) count
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
130 mg/kg/1Y-I
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Lungs, Thorax, or Respiration - tumors Liver - tumors
TYPE OF TEST :
Specific locus test
TYPE OF TEST :
Sex chromosome loss and nondisjunction
TYPE OF TEST :
Heritable translocation test
TYPE OF TEST :
DNA damage
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Micronucleus test

MUTATION DATA

TYPE OF TEST :
Cytogenetic analysis
TEST SYSTEM :
Mammal - species unspecified Leukocyte
DOSE/DURATION :
25 umol/L
REFERENCE :
CYTBAI Cytobios. (Faculty Press, 88 Regent St., Cambridge, UK) V.1- 1969- Volume(issue)/page/year: 14,151,1975 *** REVIEWS *** IARC Cancer Review:Animal Sufficient Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,291,1976 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,291,1976 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 35,89,1976 TOXICOLOGY REVIEW CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,1171,1976
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野百合碱安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H351

[ 警示性声明 ]:
P281-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 危险品运输编码 ]:
UN 1544 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
QB3140000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29399990

野百合碱上下游产品

野百合碱文献

The Japanese toxicogenomics project: application of toxicogenomics.

Mol. Nutr. Food. Res. 54 , 218-27, (2010)

Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted appr...

Developing structure-activity relationships for the prediction of hepatotoxicity.

Chem. Res. Toxicol. 23 , 1215-22, (2010)

Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...


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相关化工产品/化学物质:

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¥需询单/20mg

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产品详情:野百合碱


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¥需询单/1mg

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¥588.0/50mg ¥398.0/20mg

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价格:
¥500.0/25mg ¥900.0/50mg ¥1450.0/100mg ¥2500.0/200mg

联系人:周女士

产品详情:Monocrotaline


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产品详情:Monocrotaline


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相关化合物

【野百合碱】化源网提供野百合碱CAS号315-22-0,野百合碱MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询野百合碱上化源网,专业又轻松。>>电脑版:野百合碱

标题:野百合碱_MSDS_用途_密度_野百合碱CAS号【315-22-0】_化源网 地址:https://m.chemsrc.com/mip/cas/315-22-0_894703.html