甘珀酸钠

甘珀酸钠用途

Carbenoxolone disodium 是甘草酸 (HY-N0184) 的活性代谢物和人 11β-HSD 和细菌 3α, 20β-HSD 的抑制剂。Carbenoxolone disodium 是一种缝隙连接的解耦剂 (gap junctions) 和并且可以有效抑制牛痘病毒生长。Carbenoxolone disodium 可用于研究消化性、食道和口腔溃疡和炎症的相关研究。

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甘珀酸钠名称

[ CAS 号 ]:
7421-40-1

[ 中文名 ]:
甘珀酸钠

[ 英文名 ]:
Carbenoxolone disodium

[中文别名 ]:

[英文别名 ]:

sodium carbenoxolone
pyrogastrone
CARBENOXOLONE SODIUM
EINECS 231-044-0
ulcus-tablinen
neogel
sanodin
Carbenoxolon-Dinatriumsalz
duogastrone
Carbenoxalone Sodium

甘珀酸钠生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 细胞骨架 >> 间隙连接蛋白

[ 靶点 ]

IC50: human 11β-HSD; bacterial 3α, 20β-HSD[1]; gap junction; Vaccinia virus[2]

[体外研究]

卡宾诺酮二钠(6-150μM；预处理1小时)抑制痘苗病毒(VACV)在一个独立于HaCaT细胞的缝隙连接中的复制,并且在48小时对VACV-A5L-EGFP感染细胞具有毒性作用[2]。卡宾诺酮(30μM；预处理1小时)不上调PP2A的表达,但诱导hacat细胞中晚期蛋白A27的表达[2]。细胞活力测定[2]细胞系：HaCaT细胞浓度：6μM、12μM、30μM、60μM、150μM孵育时间：预处理1小时结果：病毒感染细胞在高剂量下48小时前无毒性。Western Blot分析[2]细胞系：HaCaT细胞浓度：30μM孵育时间：预处理1h结果：A27表达明显上调。

[体内研究]

卡宾索酮(腹腔注射；100、200和300 mg/kg；地西泮前30、60和60 min)不诱导肌肉松弛剂活性,与生理盐水相比显示出肌肉松弛剂活性,并且在牵引试验中这种作用比地西泮更大[3]。在戊四氮(PTZ)癫痫模型中,卡宾诺酮(腹腔注射,100、200和300mg/kg,戊四氮前30、60和60min)显著增加小鼠睡眠时间,降低潜伏期。ED50值为83.3 mg/kg(%95 CL:556.29)[3]。动物模型：雄性BALB/c小鼠[3]剂量：100、200、300mg/kg给药：腹腔注射；戊四唑前30、60、60min结果：小鼠睡眠时间明显延长。

[参考文献]

[1]. W L Duax, et al. Steroid Dehydrogenase Structures, Mechanism of Action, and Disease. Vitam Horm. 2000;58:121-48.

[2]. Hossein Hosseinzadeh, et al. Anticonvulsant, Sedative and Muscle Relaxant Effects of Carbenoxolone in Mice. BMC Pharmacol. 2003 Apr 29;3:3.

[3]. Ismar R Haga, et al. Carbenoxolone-mediated Cytotoxicity Inhibits Vaccinia Virus Replication in a Human Keratinocyte Cell Line. Sci Rep. 2018 Nov 16;8(1):16956.

甘珀酸钠物理化学性质

[ 沸点 ]:
687.4ºC at 760 mmHg

[ 分子式 ]:
C₃₄H₄₈Na₂O₇

[ 分子量 ]:
614.72000

[ 闪点 ]:
211.6ºC

[ 精确质量 ]:
614.32000

[ PSA ]:
123.63000

[ LogP ]:
4.15890

[ 储存条件 ]:
库房低温通风干燥

甘珀酸钠MSDS

详细MSDS(安全技术说明书)

甘珀酸钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RK0250000

CHEMICAL NAME :: Olean-12-en-30-oic acid, 3-beta-hydroxy-11-oxo-, hydrogen succinate, disodium salt

CAS REGISTRY NUMBER :: 7421-40-1

LAST UPDATED :: 199610

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C34-H48-O7.2Na

MOLECULAR WEIGHT :: 614.80

WISWESSER LINE NOTATION :: T F6 E6 B666 DO BUTJ F1 IOV2VQ J1 J1 N1 O1 R1 U1VQ U1 &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 120 mg/kg/6W

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Nutritional and Gross Metabolic - changes in potassium

REFERENCE :: CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 117,1155,1977

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2450 mg/kg

TOXIC EFFECTS :: Cardiac - pulse rate Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 92 mg/kg

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

REFERENCE :: FRMCE8 Farmaco. (Societa Chimica Italiana, Corso Strada Nova, 86, Casella Postale 227, 27100 Pavia, Italy) V.44- 1989- Volume(issue)/page/year: 49,281,1994

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1515 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

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

REFERENCE :: 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 198 mg/kg

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

REFERENCE :: 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3900 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 371 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1060 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 371 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2 gm/kg

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

REFERENCE :: 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 36400 mg/kg/26W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume decreased Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,859,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 12 gm/kg/30D-C

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,831,1976

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甘珀酸钠安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-36

[ 安全声明 (欧洲) ]:
26-36

[ WGK德国 ]:
3

[ RTECS号 ]:
RK0250000