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坎利酸钾

坎利酸钾用途

坎利酮酸(醛二烯)钾是一种释放坎利酮的前药,是一种有效的竞争性盐皮质激素受体(醛固酮受体)拮抗剂。卡诺酸钾作为利尿剂,用于高血压研究[1][2][3]。

坎利酸钾名称

[ CAS 号 ]:
2181-04-6

[ 中文名 ]:
坎利酸钾

[ 英文名 ]:
Potassium canrenoate

[中文别名 ]:

[英文别名 ]:

Potassium canrenoate
Canrenoic acid potassium salt
MFCD05662375
EINECS 218-554-9

坎利酸钾生物活性

[ 描述 ]:

坎利酮酸(醛二烯)钾是一种释放坎利酮的前药,是一种有效的竞争性盐皮质激素受体(醛固酮受体)拮抗剂。卡诺酸钾作为利尿剂,用于高血压研究[1][2][3]。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 代谢酶/蛋白酶 >> 盐皮质激素受体

[体内研究]

已经证明,在大鼠中,坎肾酸钾可导致粒细胞白血病的剂量依赖性增加,而在肝脏、甲状腺、大脑和乳腺的恶性肿瘤中,坎肾酸钾的剂量依赖性增加具有统计学意义[2][3]。卡雷诺酸钾(20mg/kg/天；饮用水)减少异丙肾上腺素诱导的大鼠心脏纤维化[4]。

[参考文献]

[1]. Iqbal J, Andrew R, et al. Displacement of cortisol from human heart by acute administration of a mineralocorticoid receptor antagonist. J Clin Endocrinol Metab. 2014;99(3):915-922.

坎利酸钾物理化学性质

[ 分子式 ]:
C₂₂H₂₉KO₄

[ 分子量 ]:
396.56200

[ 精确质量 ]:
396.17000

[ PSA ]:
77.43000

[ LogP ]:
2.55550

[ 外观性状 ]:
淡黄色至黄褐色的粉末

[ 储存条件 ]:
2-8°C

坎利酸钾MSDS

详细MSDS(安全技术说明书)

坎利酸钾毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU3500000

CHEMICAL NAME :: 17-alpha-Pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, monopotassium salt

CAS REGISTRY NUMBER :: 2181-04-6

LAST UPDATED :: 199512

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C22-H30-O4.K

MOLECULAR WEIGHT :: 397.62

WISWESSER LINE NOTATION :: L E5 B666 OV KU MUTJ A1 E1 FQ F2VQ &-KA-

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 :: 650 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 - rat

DOSE/DURATION :: 183 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 160 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 - rat

DOSE/DURATION :: 112 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 740 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 :: 140 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 165 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 :: 125 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 gm/kg/30D-I

TOXIC EFFECTS :: Behavioral - tremor Lungs, Thorax, or Respiration - respiratory stimulation Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14560 mg/kg/26W-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1350 mg/kg/30D-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 560 mg/kg

SEX/DURATION :: female 7-13 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 - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 420 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Rodent - mouse Lymphocyte

DOSE/DURATION :: 150 mg/L

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 61,201,1988

坎利酸钾安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
TU3500000

[ 海关编码 ]:
2916209090

坎利酸钾海关

[ 海关编码 ]: 2916209090

[ 中文概述 ]:
2916209090 其他（环烷、环烯、环萜烯）一元羧酸（包括酸酐、酰卤化物，过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙烯酸、丙烯酸盐或酯应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
2916209090 other cyclanic, cyclenic or cyclotherpenic monocarboxylic acids, their anhydrides, halides, peroxides, peroxyacids and their derivatives VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

坎利酸钾文献

Effect of the steroid K-canrenoate on hsp70 expression and tissue damage in transgenic Drosophila melanogaster (hsp70-lacZ) Bg9.

J. Insect Sci. 12 , 92, (2012)

In the present study the effect of 0.1, 0.2, 0.4, 0.8, and 1.0 µL/mL of the steroid K-canrenoate was evaluated in the third instar larvae of transgenic Drosophila melanogaster (hsp70-lacZ) Bg(9) for 6...

Mineralocorticoids participate in the reduced vascular reactivity of pregnant rats.

Am. J. Physiol. Heart Circ. Physiol. 302(5) , H1195-201, (2012)

The renin-angiotensin-aldosterone (RAA) system is markedly activated in pregnancy. We evaluated if mineralocorticoid receptors (MR), a major component of the RAA system, are involved in the reduced va...

Akt-mediated cardioprotective effects of aldosterone in type 2 diabetic mice.

FASEB J. 28(6) , 2430-40, (2014)

Studies have shown that aldosterone would have angiogenic effects and therefore would be beneficial in the context of cardiovascular diseases. We thus investigated the potential involvement of aldoste...

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