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Diclofenac sodium salt

双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)是一种非选择性COX抑制剂,双氯芬酸钠在完整细胞中对COX-1和-2的IC50分别为0.5μg/ ml和0.5μg/ ml。
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中文别名 双氯芬酸钠(15307-79-6);双氯灭痛钠;二氯芬酸;二氯苯胺苯乙酸钠;双氯灭痛双氯胺苯乙酸钠;双氯酸盐;双氯芬酸;2-[((2,6-6-二氯苯基)氨基]-苯乙酸钠盐(1:1);
英文别名 Diclofenac sodium salt, cyclo-oxygenase inhibitor(15307-79-6);Diclofenac Sodium;Dichlofenal;Diclofenac;Diclofenac Potassium;Diclofenac Sodium;Diclofenac, Sodium;Diclonate P;Diclophenac;Dicrofenac;Feloran;GP 45,840;GP-45,840;GP45,840;Novapirina;Orthofen;Orthophen;Ortofen;Sodium Diclofenac;SR 38;SR-38;SR38;Voltaren;Voltarol;
CAS号 15307-79-6
Inchi InChI=1S/C14H11Cl2NO2.Na/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19;/h1-7,17H,8H2,(H,18,19);/q;+1/p-1
InchiKey KPHWPUGNDIVLNH-UHFFFAOYSA-M
分子式 Molecular Weight C14H10Cl2NNaO2
分子量 Formula 318.13
溶解度Solubility DMSO 64 mg / mL(201.17 mM);乙醇64 mg / mL(201.17 mM)Soluble in water (50 mg/ml), PBS pH 7.2 (6 mg/ml), ethanol (~35 mg/ml), DMF (~35 mg/ml), DMSO (~35 mg/ml), methanol (>24 mg/ml), and acetone (6 mg/ml).
性状 灰白色至浅米色固体
储藏条件 Storage conditions 3年-20°C粉末; 6个月-80°C溶剂

双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)毒理性质:
 
生物 测试类型 路线 报告剂量(标准化剂量) 影响 资源
dog LD50 intravenous 42mg/kg (42mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 6, Pg. 1521, 1972.
dog LD50 oral 59mg/kg (59mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 6, Pg. 1521, 1972.
mouse LD50 intraperitoneal 74mg/kg (74mg/kg)   Pharmaceutical Chemistry Journal Vol. 27, Pg. 343, 1993.
mouse LD50 intravenous 116mg/kg (116mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 5, Pg. 106, 1974.
mouse LD50 oral 95mg/kg (95mg/kg)   Pharmaceutical Chemistry Journal Vol. 23, Pg. 579, 1989.
mouse LD50 subcutaneous 390mg/kg (390mg/kg)   Drugs in Japan Vol. 6, Pg. 311, 1982.
mouse LD50 unreported 380mg/kg (380mg/kg)   Pharmaceutical Chemistry Journal Vol. 21, Pg. 275, 1987.
rabbit LD50 intravenous > 100mg/kg (100mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 6, Pg. 1521, 1972.
rabbit LD50 oral 157mg/kg (157mg/kg)   Kiso to Rinsho. Clinical Report. Vol. 6, Pg. 1521, 1972.
rat LD50 intraperitoneal 25mg/kg (25mg/kg)   Drugs in Japan Vol. 6, Pg. 311, 1982.
rat LD50 intravenous 117mg/kg (117mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 5, Pg. 106, 1974.
rat LD50 oral 53mg/kg (53mg/kg) BEHAVIORAL: ATAXIA Toho Igakkai Zasshi. Journal of Medical Society of Toho University. Vol. 28, Pg. 99, 1981.
 
BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)
 
LUNGS, THORAX, OR RESPIRATION: RESPIRATORY STIMULATION
rat LD50 rectal 85400ug/kg (85.4mg/kg)   Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 14, Pg. 2259, 1986.
rat LD50 subcutaneous 83mg/kg (83mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 5, Pg. 106, 1974.
women TDLo intramuscular 9mg/kg/1W-I (9mg/kg) BLOOD: NORMOCYTIC ANEMIA American Journal of Hematology. Vol. 58, Pg. 142, 1998.
 
KIDNEY, URETER, AND BLADDER: "CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)"
women TDLo intramuscular 15mg/kg/5D-I (15mg/kg) KIDNEY, URETER, AND BLADDER: "CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)" Lancet. Vol. 340, Pg. 126, 1992.
 
GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"
 
GASTROINTESTINAL: OTHER CHANGES
women TDLo oral 30mg/kg/10D-I (30mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING Postgraduate Medical Journal. Vol. 69, Pg. 486, 1993.
women TDLo oral 112mg/kg/8W-I (112mg/kg) GASTROINTESTINAL: OTHER CHANGES Archives of Internal Medicine. Vol. 152, Pg. 625, 1992.
 
GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"
 
SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE"
women TDLo oral 180mg/kg/13W- (180mg/kg) SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE" British Medical Journal. Vol. 295, Pg. 182, 1987.
 
BEHAVIORAL: ANOREXIA (HUMAN
 
KIDNEY, URETER, AND BLADDER: PROTEINURIS
women TDLo oral 183mg/kg/26W- (183mg/kg) LIVER: "JAUNDICE, OTHER OR UNCLASSIFIED" British Journal of Clinical Practice. Vol. 43, Pg. 125, 1989.
 
LIVER: "HEPATITIS, FIBROUS (CIRRHOSIS, POST-NECROTIC SCARRING)"
women TDLo oral 270mg/kg/90D- (270mg/kg) BLOOD: CHANGES IN ERYTHROCYTE (RBC) COUNT Archives of Internal Medicine. Vol. 152, Pg. 625, 1992.
 
GASTROINTESTINAL: OTHER CHANGES
 
GASTROINTESTINAL: ULCERATION OR BLEEDING FROM LARGE INTESTINE
women TDLo oral 300mg/kg/17W- (300mg/kg) LIVER: LIVER FUNCTION TESTS IMPAIRED Clinical Rheumatology. Vol. 11, Pg. 120, 1992.
women TDLo oral 2190mg/kg/2Y- (2190mg/kg) GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA" American Journal of Gastroenterology. Vol. 90, Pg. 1871, 1995.
women TDLo unreported 364mg/kg/26W- (364mg/kg) KIDNEY, URETER, AND BLADDER: URINE VOLUME DECREASED Wiener Klinische Wochenschrift. Vol. 111, Pg. 523, 1999.
 
KIDNEY, URETER, AND BLADDER: INTERSTITIAL NEPHRITIS
 
KIDNEY, URETER, AND BLADDER: PROTEINURIS

双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)实验注意事项
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害。
3.取样品的移液枪头需及时更换,必要时为避免交叉污染尽可能选择滤芯吸头。
4.称量药品时选用称量纸,并无风处取药和称量以免扬撒,试剂的容器使用前务必确保干净,并消毒。
5.取药品时尽量采用多个药勺分别使用,使用后清洗干净后,烘干消毒存放。
6.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染。

双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:双氯芬酸钠试剂,双氯芬酸钠杂质,双氯芬酸钠合成,双氯芬酸钠中间体,双氯芬酸钠密度,双氯芬酸钠溶解度,双氯芬酸钠旋光度,双氯芬酸钠闪点,双氯芬酸钠熔点,双氯芬酸钠购买,
产品说明 双氯芬酸钠(15307-79-6)仅做科学研究以及化学合成中间体使用,双氯芬酸钠溶解度,双氯芬酸钠MSDS,双氯芬酸钠结构式其他参数见主页
Introduction双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)used for scientific research and chemical synthesis intermediates
Application1双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)An inhibitor of Cox-1 and Cox-2.
Application2双氯芬酸钠(GP 45840)是一种非选择性COX抑制剂,在完整细胞中对COX-1和-2的IC50分别为0.5μg/ ml和0.5μg/ ml
Application3双氯芬酸钠是具有解热镇痛作用的非甾体类抗炎药(NSAID)。双氯芬酸钠主要以钠盐形式提供。
一、双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)药理学:
1、双氯芬酸钠(GP 45840)是一种有效的,非选择性抗炎剂,为COX的抑制剂,在CHO细胞中,对人COX-1和COX-2的IC50值分别为4和1.3 nM。双氯芬酸钠对绵羊COX-1和COX-2的IC50值分别为5.1μM,0.84μM。双氯芬酸钠通过活化caspase级联反应来诱导神经干细胞凋亡(凋亡)。
2、Diclofenac Sodium (GP 45840) 是一种有效的,非选择性抗炎剂,为 COX 的抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的 IC50 值分别为 4 和 1.3 nM。Diclofenac Sodium 对绵羊 COX-1 和 COX-2 的 IC50 值分别为 5.1 μM,0.84 μM。Diclofenac Sodium 通过活化 caspase 级联反应来诱导神经干细胞凋亡 (apoptosis)。
 
二、双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)物理属性:
 
物理特性 单位 温度(摄氏度) 资源
Melting Point 283-285 deg C   EXP
log P (octanol-water) 0.7 (none)   EXP
Water Solubility 2430 mg/L 25 EST
Vapor Pressure 4.75E-14 mm Hg 25 EST
Atmospheric OH Rate Constant 1.64E-10 cm3/molecule-sec 25 EST

警示图
危险性 warning
危险性警示 No data available
安全声明 H303吞入可能有害+H313皮肤接触可能有害+H333吸入可能对身体有害
安全防护 P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜(如果有)并且易于操作,继续冲洗+P337如果眼睛刺激持续+P313获得医疗建议/护理
备注 实验过程中防止吸入、食入,做好安全防护
双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)危害标识:
象形图
信号 Danger
GHS危险说明 Aggregated GHS information provided by 356 companies from 38 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
H301 (81.18%): Toxic if swallowed [Danger Acute toxicity, oral]
H302 (18.82%): Harmful if swallowed [Warning Acute toxicity, oral]
H315 (10.67%): Causes skin irritation [Warning Skin corrosion/irritation]
H319 (10.39%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]
H361 (37.64%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]
H372 (31.18%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]
H411 (28.93%): Toxic to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]
Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码 P201, P202, P260, P264, P270, P273, P280, P281, P301+P310, P301+P312, P302+P352, P305+P351+P338, P308+P313, P314, P321, P330, P332+P313, P337+P313, P362, P391, P405, and P501
(The corresponding statement to each P-code can be found at the GHS Classification page.)
 
Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80.
Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95.
双氯芬酸钠(15307-79-6,Diclofenac Sodium,GP 45840)参考文献:
1.Simultaneous Determination of Diclofenac Sodium and Rabeprazole Sodium in Bulk and Pharmaceutical Dosage Form by LC
Vora Asfak, Damle Mrinalini, Bhat Leena, Godge Rahul. Chromatographia 2007, 66, December (No. 11/12)

Diclofenac sodium (DCF) possesses analgesic, antipyretic and anti-inflammatory properties. It is official in I.P, B.P and U.S.P while rabeprazole (RAB) is a proton-pump inhibitor that suppresses gastric acid secretion. RAB is not official in I.P, B.P and U.S.P. detailed survey of the literature for DCF revealed several methods based on different techniques, viz-spectrophotometric methods and HPLC methods for either DCF as single component or in combinations with drugs other than RAB. Moreover, the literature survey reveals spectrophotometric methods as well as chromatographic methods for the determination of RAB as single drug and in combination with drugs other than DCF. There is no method reported for the determination of DCF and RAB in combination. In the present investigation a simple, accurate, sensitive and precise RP-HPLC method has been developed for the simultaneous determination of diclofenac sodium and rabeprazole sodium in bulk and marketed formulations.

2.Photocatalytic Degradation of Diclofenac Sodium in Aqueous Solution Using N, S, and C-doped ZnO
M. Giahi. Russian Journal of Applied Chemistry, 2015, Vol. 88, No. 12, pp. 2044−2049

The pH value of the different wastewater is different, and it influences the photocatalytic reactions for degradation of the pollutants. Similarly, the pH plays an important role in the degradation of diclofenac sodium. The effect of the initial pH value on the photodegradation efficiency of diclofenac sodium is shown in Fig. 6. In all cases, the maximum degradation efficiency was obtained in acidic pH 6.0 for diclofenac sodium. In the presence of N, S, C-doped ZnO and in pH 6.0, degradation efficiency was 98.2% was obtained. The interpretation of pH effects on the photocatalytic process is a very difficult task because of its multiple roles such as electrostatic interactions between the semiconductor surface, solvent molecules, substrate and charged radicals formed during the progress of reaction. The pH influences adsorption and dissociation of substrate, catalyst surface charge, oxidation potential of the valence band, and other physicochemical properties of the system.

3.Clinical analysis on the analgesic effect of Methyl Carboprost and Diclofenac Sodium for intracavitary brachytherapy
Guiling Li, Yingqiu Song, Fang Zhu, Tingting Zhang. Chinese-German Journal of Clinical Oncology October 2007, Vol. 6, No. 5, P497–P499

Prostaglandin (PG) is the major factor inducing to pain. Methyl Carboprost is a synthesis of PGF2α analogue, which can be absorbed through mucous membrane quickly and act to PG receptor in the uterine muscle cell membrane directly, and then activate the uterine muscle cell. The activities of collagenase and elastase will be improved. The uterine cervical is softened and loosened. The effective component of Diclofenac Sodium is naphthalene acetic acid, which is a kind of NASID deriving from alphatoluic acid. It can inhibit the activity of epoxidase, and then block the transformation from arachidonic acid to PG. The synthesis and releasing of PG will reduce. So it can control pain and relax the uterine cervical, and then it can relieve the pain induced by putting the intrauterine tube. Besides, it is reported that Diclofenac Sodium can play the role in resisting the perception to the central nerve system and peripheral nerve, too. It can inhibit the inducing reaction of cerebral ganglion to nociceptor of nerve terminal, and then depress the sensitivity of peripheral nerve to noxious stimulation. So it has analgesic effect to patients. Diclofenac Sodium can be absorbed through mucous membrane, but not enter into general circulation through liver. The response of stomach intestine and the first pass effect of liver will be avoided. The drug level in blood receiving by anus is two times of receiving by mouth. The analgesic effect is good and quick. The persistence time is long.


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