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甲磺酸加贝酯

甲磺酸加贝酯用途

Gabexate甲磺酸盐是非抗原的类胰蛋白酶丝氨酸蛋白酶抑制剂。

甲磺酸加贝酯名称

[ CAS 号 ]:
56974-61-9

[ 中文名 ]:
甲磺酸加贝酯

[ 英文名 ]:
Gabexate mesylate

[中文别名 ]:

[英文别名 ]:

Gabexate monomethanesulfonate
MFCD00210299
Gabexate mesylate

甲磺酸加贝酯生物活性

[ 描述 ]:

Gabexate甲磺酸盐是非抗原的类胰蛋白酶丝氨酸蛋白酶抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 因子Xa

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Erba, F., et al., Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol, 2001. 61(3): p. 271-6.

[2]. Aosasa, S., et al., Mechanism of the inhibitory effect of protease inhibitor on tumor necrosis factor alpha production of monocytes. Shock, 2001. 15(2): p. 101-5.

[3]. Colasanti, M., et al., Effect of gabexate mesylate (FOY), a drug for serine proteinase-mediated diseases, on the nitric oxide pathway. Biochem Biophys Res Commun, 1998. 246(2): p. 453-6.

[相关活性小分子]

甲磺酸加贝酯物理化学性质

[ 沸点 ]:
508.6ºC at 760 mmHg

[ 熔点 ]:
91 °C

[ 分子式 ]:
C₁₇H₂₇N₃O₇S

[ 分子量 ]:
417.477

[ 闪点 ]:
261.4ºC

[ 精确质量 ]:
417.156982

[ PSA ]:
177.25000

[ LogP ]:
3.58790

[ 外观性状 ]:
白色晶体

[ 储存条件 ]:
-20°C

[ 水溶解性 ]:
水溶性：完全溶解；易溶于：氯仿,乙醇；可溶于：甲醇；微溶：丙酮；不溶：乙醚

甲磺酸加贝酯MSDS

甲磺酸加贝酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DG2800800

CHEMICAL NAME :: Benzoic acid, 4-((6-((aminoiminomethyl)amino)-1-oxohexyl)oxy)-, ethyl ester, monomethanesulfonate

CAS REGISTRY NUMBER :: 56974-61-9

LAST UPDATED :: 199806

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C16-H23-N3-O4.C-H4-O3-S

MOLECULAR WEIGHT :: 417.53

WISWESSER LINE NOTATION :: MUYZM5VOR DVO2 &WSQ1

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 :: 6480 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4020 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 79 mg/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4500 mg/kg

TOXIC EFFECTS :: Skin and Appendages - corrosive (after topical exposure)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 218 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Kidney, Ureter, Bladder - urine volume increased

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,1203,1987

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 71,71,1975

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 71,71,1975 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1120 mg/kg/14D-C

TOXIC EFFECTS :: Blood - normocytic anemia Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 15,1209,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1680 mg/kg/8W-C

TOXIC EFFECTS :: Endocrine - changes in spleen weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,743,1975

甲磺酸加贝酯安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn: Harmful;

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

[ WGK德国 ]:
2

[ RTECS号 ]:
DG2800800

甲磺酸加贝酯合成路线

甲磺酸加贝酯上下游产品

甲磺酸加贝酯上游产品

甲磺酸加贝酯下游产品

甲磺酸加贝酯制备

6-氨基己酸和氢氧化钠反应，生成6-氨基己酸钠。再和甲基异硫脲硫酸盐的水溶液反应，得6-胍基己酸。再和甲磺酸在水中搅拌，过滤去不溶物后，减压浓缩，加人丙酮，放置，过滤，可得6-胍基己酸甲磺酸盐，用甲醇-乙醚重结晶后，熔点116～118℃。6-胍基己酸甲磺酸盐经氯化亚砜氯化为酰氯，再和对羟基苯甲酸乙酯，在四氢呋喃和吡啶中反应，经处理得甲磺酸加贝酯。

甲磺酸加贝酯文献

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