Sulfobromophthalein disodium salt (Bromosulfophthalein disodium salt)   中文名称: 四溴磺酚钠

一种称为磺溴酞二钠盐的合成染料于 1925 年首次出现，作为评估肝功能的治疗工具[1]。 pH 指示剂染料磺溴酞 (BSP) 表现出快速（17 秒，质子依赖性醌基-酚互变异构，pK = 8.5）[1]。有机阴离子转运多肽 1B1 (OATP1B1)、OATP1B3、OATP1A2 和 OATP2B1 以及多药耐药蛋白 2 (MDR2) 均已被证明是溴磺胺的底物和抑制剂 [2]。

Absorption, Distribution and Excretion
WHEN HEPATIC FUNCTION IS SEVERELY IMPAIRED, UP TO 10-25%...MAY BE EXCRETED IN URINE. NORMALLY...LESS THAN 2% OF DOSE IS EXCRETED IN THIS WAY, & EXTRAHEPATIC REMOVAL OF SULFOBROMOPTHALEIN CAN BE DISREGARDED.
NORMAL METABOLISM & EXCRETION OF SULFOBROMOPHTHALEIN DEPEND ON HEPATIC BLOOD FLOW, ABILITY OF LIVER CELLS TO TAKE UP & CONCN THE DYE, & INTAKE BILIARY EXCRETION.
...METABOLIZED IN LIVER BY CONJUGATION WITH GLUTATHIONE, & BOTH FREE & CONJUGATED...ARE EXCRETED INTO BILE. ... DYE DOES NOT UNDERGO ENTEROHEPATIC CIRCULATION...& IS EXCRETED PRIMARILY IN FECES. ... EXCRETION OF DYE IS USUALLY COMPLETE WITHIN 24 HR.
FOLLOWING IV ADMIN...ALMOST COMPLETELY BOUND TO PLASMA PROTEINS IN BLOOD, MAINLY ALBUMIN & ALPHA1 LIPOPROTEINS. DYE IS RAPIDLY TAKEN UP & BRIEFLY STORED BY HEPATIC PARENCHYMAL CELLS. ... SMALL AMT...MAY BE TAKEN UP BY SKELETAL MUSCLE, BUT EXTRA-HEPATIC TISSUE UPTAKE IS MINIMAL. ...DOES NOT CROSS PLACENTA.
For more Absorption, Distribution and Excretion (Complete) data for SODIUM SULFOBROMOPHTHALEIN (6 total), please visit the HSDB record page.

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Metabolism / Metabolites
S-ARYLTRANSFERASE IS THOUGHT TO BE INVOLVED IN METABOLISM OF SULFOBROMOPHTHALEIN...
IT IS EXCRETED IN BILE OF RATS AS BSP-GLUTATHIONE & OTHER AMINOACYL CONJUGATES, FORMED BY CONDENSATION OF BSP WITH GLUTATHIONE, PROBABLY WITHOUT ELIMINATION OF ANY OF BROMINE ATOMS.
SULFOBROMOPHTHALEIN /WAS METABOLIZED TO THE FOLLOWING/ S-(3,3-BIS(4-HYDROXY-3-SULFOPHENYL) TRIBROMOPHTHALIDYL)GLUTATHIONE IN DOG; JAVITT NB, ET AL, J CLIN INVEST, 39, 1570 (1960). SULFOBROMOPHTHALEIN-BETA-D-GLUCURONIDE IN LIVER; HIRAYAMA C, ET AL, SAISHIN IGAKU, 17, 2520 (1962).

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Biological Half-Life
IN ONE STUDY IN SMALL NUMBER OF NORMAL SUBJECTS, PLASMA HALF-LIFE AVG ABOUT 4 MIN. LIVER HAS STORAGE CAPACITY...WHICH IS PROPORTIONAL TO PLASMA CONCN OF DYE, & RANGES FROM 50-75 MG OF SULFOBROMOPHTHALEIN...PER MG OF DYE PER 100 ML OF PLASMA IN PT WITH NORMAL LIVER FUNCTION.

Interactions
DEHYDROCHOLIC ACID, CHLORTETRACYCLINE, SULFONAMIDES, NOVOBIOCIN, & MONOAMINE OXIDASE INHIBITORS MAY ALSO INCR SULFOBROMOPHTHALEIN RETENTION, ALTHOUGH POSSIBILITY OF ACTUAL LIVER DAMAGE SHOULD BE CONSIDERED IN PT RECEIVING CHLORTETRACYCLINE, SULFONAMIDES, OR NOVOBIOCIN.
SIMULTANEOUS ADMIN OF INDOCYANINE GREEN...MAY RESULT IN IMPAIRMENT OF HEPATIC EXCRETION...
CHOLECYSTOGRAPHIC AGENTS...REPORTED TO COMPETITIVELY INTERFERE WITH SULFOBROMOPHTHALEIN CLEARANCE & EXCRETION... ETHOXAZENE, PHENAZOPYRIDINE, PHENOLPHTHALEIN, & PHENOLSULFONPHTHALEIN (PSP) MAY PRODUCE APPARENT DECR EXCRETION OF SULFOBROMOPHTHALEIN BY INTERFERING WITH COLORIMETRIC MEASUREMENT...
BILIARY EXCRETION RATE & RATE OF PLASMA DISAPPEARANCE OF SULFOBROMOPHTHALEIN... WERE SHOWN...TO INCR AFTER PRE-TREATMENT WITH PHENOBARBITAL & OTHER MICROSOMAL-ENZYME INDUCERS IN RATS, & INCR EXCRETION CORRELATED WELL WITH INCR IN BILE FLOW RATES.
For more Interactions (Complete) data for SODIUM SULFOBROMOPHTHALEIN (7 total), please visit the HSDB record page.

[1]. Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: comparative analysis with prototypical probe substrates estradiol-17β-glucuronide, estrone-3-sulfate, and sulfobromophthalein. Drug Metab Dispos. 2013 Oct;41(10):1859-66.

Bromosulfophthalein sodium is an organic sodium salt that is the disodium salt of bromosulfophthalein. It has a role as a dye. It contains a bromosulfophthalein(2-). It is functionally related to a 2-benzofuran-1(3H)-one.
A phenolphthalein that is used as a diagnostic aid in hepatic function determination.

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Mechanism of Action
SULFOBROMOPHTHALEIN TEST FOR LIVER FUNCTION IS BASED ON THE FACT THAT IN PT WITH HEPATIC DYSFUNCTION, PERCENTAGE DISAPPEARANCE RATE & EST STORAGE CAPACITY...ARE DECR & PLASMA HALF-LIFE & EST EXCRETORY TIME OF DYE ARE INCR.

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Therapeutic Uses
Indicators and Reagents; Phthalein Dyes
FORTY-FIVE MIN AFTER INJECTION...4-5 ML OF BLOOD IS WITHDRAWN FROM OPPOSITE ARM TO AVOID CONTAMINATION OF SAMPLE. ...SOME CLINICIANS TAKE SINGLE SAMPLE @ 30 MIN & OTHERS @ 60 MIN. AMT OF DYE RETAINED IN THE SERUM IS DETERMINED COLORIMETRICALLY.
USE...IN HEPATIC FUNCTION DETERMINATION IS NOT BASED ON ITS PHARMACOLOGIC EFFECTS BUT ON ITS DISTRIBUTION, METABOLISM, & EXCRETION FROM BODY.
...HELPFUL IN DETECTING HEPATIC DAMAGE IN PT WHO HAVE BEEN EXPOSED TO HEPATOTOXINS & IN RECOGNIZING METASTATIC CARCINOMA. ...ALSO BEEN USED TO DISTINGUISH UPPER GI HEMORRHAGE DUE TO PEPTIC ULCER FROM THAT DUE TO ESOPHAGEAL VARICES & FOR DIAGNOSIS OF DUBIN-JOHNSON OR ROTOR SYNDROMES. ...USED TO EST HEPATIC BLOOD FLOW...
For more Therapeutic Uses (Complete) data for SODIUM SULFOBROMOPHTHALEIN (8 total), please visit the HSDB record page.

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Drug Warnings
HIGH BLOOD LEVELS OF BILIRUBIN MAY INTERFERE WITH MEASUREMENT OF SULFOBROMOPHTHALEIN... HEPARIN...INCR COLOR INTENSITY...IN SERUM & CAUSES SHIFT IN ABSORPTION... ... SULFOBROMOPHTHALEIN MAY PRODUCE...INCR IN OTHER LABORATORY TEST RESULTS...SERUM CALCIUM, SERUM CREATINE & CREATININE, UROBILINOGEN, BLOOD PROTEIN...
PARENTERAL CHOLECYSTOGRAPHIC AGENTS ARE SATURATED SOLN, & PT ALMOST INVARIABLY EXPERIENCE THROMBOPHLEBITIS IF SULFOBROMOPHTHALEIN IS INJECTED INTO SAME ARM WITHIN FEW DAYS FOLLOWING INJECTION OF RADIOPAQUE SUBSTANCE.
VET WARNING: IRRITANT TO VEINS. USE DILUTE SOLN VIA SMALL GAUGE NEEDLES OR CANNULAS. ... ICTERIC STATES PREVENT INTERPRETATION OF TEST.
...USED WITH EXTREME CAUTION, IF @ ALL, IN PT WHO HAVE HAD PREVIOUS SULFOBROMOPHTHALEIN TESTS & IN PT WITH HISTORY OF ALLERGY OR ASTHMA... COMPLETE MEDICAL HISTORY...SHOULD BE OBTAINED BEFORE DYE IS ADMIN.
For more Drug Warnings (Complete) data for SODIUM SULFOBROMOPHTHALEIN (7 total), please visit the HSDB record page.

C20H8BR4NA2O10S2

838.00

833.609

71-67-0

297-83-6 (Parent)

6282

White to off-white solid powder

6.576

205.76

2

10

2

38

994

0

GHAFORRTMVIXHS-UHFFFAOYSA-L

InChI=1S/C20H10Br4O10S2.2Na/c21-15-13-14(16(22)18(24)17(15)23)20(34-19(13)27,7-1-3-9(25)11(5-7)35(28,29)30)8-2-4-10(26)12(6-8)36(31,32)33;;/h1-6,25-26H,(H,28,29,30)(H,31,32,33);;/q;2*+1/p-2

disodium;2-hydroxy-5-[4,5,6,7-tetrabromo-1-(4-hydroxy-3-sulfonatophenyl)-3-oxo-2-benzofuran-1-yl]benzenesulfonate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 500 mg/mL (596.66 mM)

配方 1 中的溶解度: ≥ 4.17 mg/mL (4.98 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 41.7 mg/mL澄清的DMSO储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 4.17 mg/mL (4.98 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 41.7 mg/mL 澄清 DMSO 储备液加入 900 μL 20% SBE-β-CD 生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 4.17 mg/mL (4.98 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 41.7 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。