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丙磺舒

丙磺舒用途

Probenecid 是一种有效的选择性瞬时受体电位香草酸受体通道 2 (TRPV2) 激动剂。
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丙磺舒名称

[ CAS 号 ]:
57-66-9

[ 中文名 ]:
丙磺舒

[ 英文名 ]:
probenecid

[中文别名 ]:

[英文别名 ]:

丙磺舒生物活性

[ 描述 ]:

Probenecid 是一种有效的选择性瞬时受体电位香草酸受体通道 2 (TRPV2) 激动剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> TRP频道
研究领域 >> 代谢疾病

[ 靶点 ]

TRPV2[1]


[体外研究]

Probenecid有效抑制MRP1和MRP2对ATP依赖性活性囊泡N-乙基马来酰亚胺谷胱甘肽(NEM-GS)的摄取。在较高的有机阴离子浓度下观察到MRP1-ATP酶的显着抑制。相反,MRP2的ATP酶活性受到Probenecid(近似KACT =250μM),磺吡酮(KACT =300μM)和吲哚美辛(KACT =150μM)的强烈刺激,并且ATP酶活化甚至强于NEM-GS。 MRP2-ATP酶的有机阴离子活化遵循钟形曲线,对于Probenecid,最大值为约2mM,对于磺吡酮为800μM,对于吲哚美辛为400μM[2]。 Probenecid是hTAS2R16,hTAS2R38和hTAS2R43苦味受体的抑制剂。 Probenecid作用于TAS2R的一个子集,并通过一种新颖的变构作用机制进行抑制。 Probenecid还常用于增强GPCR钙动员测定中的细胞信号。 Probenecid特异性地抑制由苦味受体hTAS2R16介导的细胞反应,并提供使用非竞争性(变构)机制与该GPCR直接相互作用的分子和药理学证据[3]。

[体内研究]

在给予盐水的对照小鼠中,对WT小鼠施用丙磺舒导致收缩性增加,如通过相对于EF的射血分数(EF)测量的。注射后5分钟内注意到收缩力增加,所有剂量均为75 mg/kg或以上(峰值变化为5.26±3.35,8.40±2.80,7.32±2.52为75mg/kg,100mg/kg和200mg/kg,分别)。以5分钟间隔(总共30分钟)测量的测量的收缩性变化显示出收缩性的剂量依赖性增加,估计的EC50为49.33mg/kg。 EF对受试者(n = 5,剂量为200 mg/kg IV)保持升高状态至少1小时,评估时间较长(EF相对于基线平均增加8.9±2.57)[1] ]。

[细胞实验]

使用Lipofectamine 2000在具有透明底部的聚赖氨酸包被的黑色384孔板中用hTAS2R表达构建体转染HEK-293T细胞，并在37℃温育22小时。除去生长培养基，用含有20mM HEPES的HBSS洗涤细胞两次，然后在含有20mM HEPES（钙4测定试剂盒）的HBSS中加载钙指示剂染料，含有或不含1mM丙磺舒。在染料和丙磺舒的存在下，将细胞在37℃下孵育1小时，然后移至设定为32℃的Flexstation II-384。在15分钟的温度平衡（没有洗出）后，注射指定的化合物（在t = ~25秒）并测量荧光100至180秒，每3秒读取一次。使用Prism 5.0软件分析数据集并表示为基线信号的％。对于Schild图，原始钙通量值的重复表示为相对于基线信号的％。将指定浓度的Probenecid存在下每种浓度的TAS2R配体在36秒（对应于最大通量信号）的平均值相对于配体浓度的对数作图。使用GraphPad Prism [1]中的非线性回归拟合数据点。

[动物实验]

小鼠[1]为了获得剂量反应曲线，用异氟烷麻醉12-16周龄的雄性C57 WT（n = 39）小鼠，同时在显微镜下获得静脉内颈静脉通路（IV）。随后，如下所述，在胸骨旁长轴（PSLAX）中获得具有M模式和B模式的超声心动图研究。对于WT小鼠中的初始收缩性研究，注射生理盐水或不同剂量的丙磺舒（增加2至200mg / kg）（推注IV）。

[参考文献]

[1]. Koch SE, et al. Probenecid: novel use as a non-injurious positive inotrope acting via cardiac TRPV2 stimulation. J Mol Cell Cardiol. 2012 Jul;53(1):134-44.

[2]. Bakos E, et al. Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8.

[3]. Greene TA, et al. Probenecid inhibits the human bitter taste receptor TAS2R16 and suppresses bitter perception of salicin. PLoS One. 2011;6(5):e20123.


[相关活性小分子]

辣椒碱 | 辣椒平 | 5-(N-乙基-N-异丙基)阿米洛利 | 氯化二亚苯基碘鎓 | 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺 | 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑 | HC-067047 | AMG9810 | GSK1016790A | SAR7334 | PF-4840154 | RN-1734 | AMG 517 | 3-(4-氯苯基)-N-(3-甲氧基苯基)-2-丙烯酰胺 | 冰素

丙磺舒物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
438.0±47.0 °C at 760 mmHg

[ 熔点 ]:
194-196°C

[ 分子式 ]:
C13H19NO4S

[ 分子量 ]:
285.359

[ 闪点 ]:
218.7±29.3 °C

[ 精确质量 ]:
285.103485

[ PSA ]:
83.06000

[ LogP ]:
3.30

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.542

[ 储存条件 ]:
Store at RT

[ 稳定性 ]:
Stable, but may be light sensitive. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
<0.1 g/100 mL at 20 ºC

丙磺舒MSDS

详细MSDS(安全技术说明书)

丙磺舒毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DG9400000
CHEMICAL NAME :
Benzoic acid, p-(dipropylsulfamoyl)-
CAS REGISTRY NUMBER :
57-66-9
BEILSTEIN REFERENCE NO. :
2815775
LAST UPDATED :
199710
DATA ITEMS CITED :
23
MOLECULAR FORMULA :
C13-H19-N-O4-S
MOLECULAR WEIGHT :
285.39
WISWESSER LINE NOTATION :
QVR DSWN3&3

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
50 mg/kg/1W-I
TOXIC EFFECTS :
Blood - other hemolysis with or without anemia
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1600 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
394 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
611 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1666 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1156 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
458 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
230 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
304 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 :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9600 mg/kg/14D-C
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
52 gm/kg/13W-I
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
38400 mg/kg/14D-C
TOXIC EFFECTS :
Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
52 gm/kg/13W-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
206 gm/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - neoplastic by RTECS criteria Liver - tumors

MUTATION DATA

TYPE OF TEST :
Sister chromatid exchange
TEST SYSTEM :
Rodent - hamster Ovary
DOSE/DURATION :
5 mg/L
REFERENCE :
NTPTR* National Toxicology Program Technical Report Series. (Research Triangle Park, NC 27709) No.206- Volume(issue)/page/year: NTP-TR-395,1991 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4171 No. of Facilities: 66 (estimated) No. of Industries: 2 No. of Occupations: 9 No. of Employees: 4059 (estimated) No. of Female Employees: 1675 (estimated)
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丙磺舒安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 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;R40

[ 安全声明 (欧洲) ]:
S36/37

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
DG9400000

[ 海关编码 ]:
2935009090

丙磺舒上下游产品

丙磺舒上游产品

丙磺舒下游产品

丙磺舒制备

对甲苯磺酰胺经重铬酸钠氧化为对羧苯磺酰胺，再用溴丙烷进行烷基化反应，所得丙磺舒钠用乙酸酸化即得丙磺舒。
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丙磺舒海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无 最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

丙磺舒文献

Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.

PLoS ONE 10 , e0127919, (2015)

Extracellular nucleotides, such as ATP, are released from cells in response to various stimuli and act as intercellular signaling molecules through activation of P2 receptors. Exposure to the ultravio...

Flavonoids are inhibitors of human organic anion transporter 1 (OAT1)-mediated transport.

Drug Metab. Dispos. 42(9) , 1357-66, (2014)

Organic anion transporter 1 (OAT1) has been reported to be involved in the nephrotoxicity of many anionic xenobiotics. As current clinically used OAT1 inhibitors are often associated with safety issue...

TRPA1 agonist activity of probenecid desensitizes channel responses: consequences for screening.

Assay Drug Dev. Technol. 10(6) , 533-41, (2012)

The transient receptor potential channel subtype A member 1 (TRPA1) is a nonselective cation channel widely viewed as having therapeutic potential, particularly for pain-related indications. Realizati...


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价格：
￥128.0/5g ￥458.0/25g ￥138.0/100mg

联系人：刘佳

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￥需询单/1g

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