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硫前列酮

硫前列酮用途

Sulprostone (SHB 286) 是一种前列腺素 E2 (PGE2) 类似物,是一种有效且选择性的 EP3 受体激动剂。Sulprostone 是具有抗溃疡和非甾体类抗流产作用,有潜力用于终止妊娠和分娩时的出血。

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硫前列酮名称

[ CAS 号 ]:
60325-46-4

[ 中文名 ]:
硫前列酮

[ 英文名 ]:
Sulprostone

[中文别名 ]:

素普罗斯顿

[英文别名 ]:

Sulprostonum
N-Acetyl-N-acetoxy-4-chlorobenzenesulfonamide
Nalador
Sulprostone
SHB-286
Sulprostona
SHB 286
EINECS 262-173-0

硫前列酮生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 炎症/免疫

[ 靶点 ]

EP3 Receptor

[体外研究]

舒前列酮(shb286)对体外培养的中国仓鼠卵巢细胞EP1和EP3的Ki值分别为21nm和0.6nm[1]。舒前列酮(1、1.5或2mg/mL)对树突状细胞(dc)的活性和纯度无明显影响。舒前列酮损害自发和定向的直流电迁移独立于其浓度。舒前列酮降低CCR7的表达,并损害树突状细胞的迁移[2]。

[体内研究]

舒前列酮(0.5 mg/kg；IV)的T1/2为0.451小时,CL为56 mL/min•kg,Vss为0.583 L/kg,AUC为149 ng•h/mL[3]。动物模型：雄性食蟹猴[3]剂量：0.5mg/kg(药代动力学分析)给药：IV结果：T1/2为0.451h,CL为56ml/min•kg,Vss为0.583l/kg,AUC为149ng•h/mL。

[参考文献]

[1]. S Narumiya, et al. Prostanoid receptors: structures, properties, and functions. Physiol Rev. 1999 Oct;79(4):1193-226.

[2]. Jenny Bulgarelli, et al. Skewing effect of sulprostone on dendritic cell maturation compared with dinoprostone. Cytotherapy. 2018 Jun;20(6):851-860.

[3]. Yifan Shi, et al. Bioanalysis of sulprostone, a prostaglandin E 2 analogue and selective EP 3 agonist, in monkey plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Aug 15;1092:51-57.

硫前列酮物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 熔点 ]:
78.5-80ºC

[ 分子式 ]:
C₂₃H₃₁NO₇S

[ 分子量 ]:
465.560

[ 精确质量 ]:
465.182129

[ PSA ]:
138.38000

[ LogP ]:
0.26

[ 外观性状 ]:
白色至灰白色固体

[ 折射率 ]:
1.589

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
DMSO: >5 mg/mL

硫前列酮MSDS

硫前列酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MJ8810000

CHEMICAL NAME :: 5-Heptenamide, 7-(3-hydroxy-2-(3-hydroxy-4-phenoxy-1-butenyl)-5-oxoc yclopentyl)- N-(methylsulfonyl)-, (1R-(1-alpha(Z),2-beta(1E,3R*),3-alpha))-

CAS REGISTRY NUMBER :: 60325-46-4

LAST UPDATED :: 199803

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C23-H31-N-O7-S

MOLECULAR WEIGHT :: 465.61

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 12 mg/kg

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

REFERENCE :: EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992- Volume(issue)/page/year: 56(4),37,1993

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18 mg/kg

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

REFERENCE :: EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992- Volume(issue)/page/year: 56(4),37,1993

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3 mg/kg

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

REFERENCE :: EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992- Volume(issue)/page/year: 56(4),37,1993 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 17 ug/kg

SEX/DURATION :: female 23 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 137,8,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 10 ug/kg

SEX/DURATION :: female 9 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 19,29,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 20 ug/kg

SEX/DURATION :: female 49 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 22,471,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 30 ug/kg

SEX/DURATION :: female 15 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 26,279,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 15 ug/kg

SEX/DURATION :: female 7 week(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - abortion

REFERENCE :: GOBIDS Gynecologic and Obstetric Investigation. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.9- 1978- Volume(issue)/page/year: 29,10,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 5 ug/kg

SEX/DURATION :: female 10 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 27,51,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraplacental

DOSE :: 500 ng/kg

SEX/DURATION :: female 15 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 26,279,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intracervical

DOSE :: 1 ug/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 16,377,1977

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 550 mg/kg

SEX/DURATION :: female 6-16 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 - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: EKFAE9 Eksperimental'naya i Klinicheskaya Farmakologiya. Experimental and Clinical Pharmacology. (Mezhdunarodnaya Kniga, ul. B. Yakimanka, 39, 117049 Moscow, Russia) V.55- 1992- Volume(issue)/page/year: 56(4),37,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 900 ug/kg

SEX/DURATION :: female 21-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: 44LQAF "International Sulprostone Symposium, Papers, Vienna, 1978," Friebel, K., et al., eds., Berlin, Fed. Rep. Ger., Schering AG, 1979 Volume(issue)/page/year: -,39,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 120 ug/kg

SEX/DURATION :: female 63-64 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: ACEDAB Acta Endocrinologica, Supplementum (Copenhagen). (Periodica, Skolegade 12 E, DK-2500 Valby, Denmark) No.1- 1948- Volume(issue)/page/year: 253,148,1983

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硫前列酮安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H319-H335-H360

[ 警示性声明 ]:
P201-P261-P305 + P351 + P338-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R60;R36/37/38

[ 安全声明 (欧洲) ]:
53-22-36/37-45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
MJ8810000

硫前列酮合成路线

硫前列酮上下游产品

硫前列酮上游产品

硫前列酮下游产品

硫前列酮文献

Quantitative phosphoproteomic analysis of signaling downstream of the prostaglandin e2/g-protein coupled receptor in human synovial fibroblasts: potential antifibrotic networks.

J. Proteome Res. 13(11) , 5262-80, (2014)

The Prostaglandin E2 (PGE2) signaling mechanism within fibroblasts is of growing interest as it has been shown to prevent numerous fibrotic features of fibroblast activation with limited evidence of d...

Angiogenesis in the primate ovulatory follicle is stimulated by luteinizing hormone via prostaglandin E2.

Biol. Reprod. 92(1) , 15, (2015)

Rapid angiogenesis occurs as the ovulatory follicle is transformed into the corpus luteum. To determine if luteinizing hormone (LH)-stimulated prostaglandin E2 (PGE2) regulates angiogenesis in the ovu...

PGE2 reduces MMP-14 and increases plasminogen activator inhibitor-1 in cardiac fibroblasts.

Prostaglandins Other Lipid Mediat. 113-115 , 62-8, (2014)

Prostaglandin E2 (PGE2) is elevated during cardiac injury and we have previously shown that mice lacking the PGE2 EP4 receptor display dilated cardiomyopathy (DCM) with increased expression of the mem...

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