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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。

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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

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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

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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。

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甲磺酸加贝酯文献

Involvement of proteinase activated receptor-2 in the vascular response to sphingosine 1-phosphate.

Clin. Sci. 126(8) , 545-56, (2014)

S1P (sphingosine 1-phosphate) represents one of the key latest additions to the list of vasoactive substances that modulate vascular tone. PAR-2 (proteinase activated receptor-2) has been shown to be ...

Role of TRPV1 in nociception and edema induced by monosodium urate crystals in rats.

Pain 152(8) , 1777-88, (2011)

Gout is characterized by the deposition of monosodium urate (MSU) crystals. Despite being one of the most painful forms of arthritis, gout and the mechanisms responsible for its acute attacks are poor...

Neonatal amygdala lesions advance pubertal timing in female rhesus macaques.

Psychoneuroendocrinology 51 , 307-17, (2014)

Social context influences the timing of puberty in both humans and nonhuman primates, such as delayed first ovulation in low-ranking rhesus macaques, but the brain region(s) mediating the effects of s...

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甲磺酸加贝酯

甲磺酸加贝酯用途

甲磺酸加贝酯名称

甲磺酸加贝酯生物活性

甲磺酸加贝酯物理化学性质

甲磺酸加贝酯MSDS

详细MSDS(安全技术说明书)

甲磺酸加贝酯毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

甲磺酸加贝酯安全信息

甲磺酸加贝酯合成路线

详细合成路线

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

甲磺酸加贝酯文献

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