G-28315, also known as SuLfinpyrazone, increases fibrinolytic action [2].

At an oral dose of 30 mg/kg, SuLfinpyrazone (G-28315) was able to dramatically delay the euglobulin clot lysis time in rats that had paw edema caused by kaolin. Apart from these benefits, rabbits were additionally shielded from rapid mortality caused by arachidonic acid by a single oral dose of 10–30 mg/kg SuLfinpyrazone [2].

Absorption, Distribution and Excretion
…Good absorption after oral administration. …Binding to plasma proteins…98-99%. After intravenous injection, the plasma half-life is approximately 3 hours. After oral administration…the uricosuric effect lasts…10 hours. Although a small amount of the drug can be filtered by the glomeruli, it is primarily secreted by the proximal tubules, with minimal passive reflux diffusion… Approximately half of the oral dose appears in the urine within 24 hours. The majority (90%) of the drug in the urine remains unchanged; the remainder is excreted as metabolites. In humans, the drug is rapidly excreted along with its hydroxylated metabolites. The plasma half-life in rats is 16.2 hours, with 18% of the intraperitoneal dose excreted in the urine. The plasma half-life in humans is 1 to 3 hours. The primary route of excretion in rats is feces (68% of the dose). A significant portion is excreted via bile and reabsorbed by the intestines. Only a small amount of sulfinpyrazone is excreted in rat urine. …Primarily cleared from circulation via bile…There is no evidence of enterohepatic circulation.
In mice, the unchanged drug is the main excretory product, with only 28% in urine and 24% in feces. The drug found in bile is p-hydroxysulfinylpyrazol. The low proportion of drug excretion in mouse urine may be related to the lack of uricosuric properties of this drug in this species.
Metabolism/Metabolites

Most of the drug (90%) in urine is unchanged; the remainder is excreted as the N1-p-hydroxyphenyl metabolite…
…/In rats/ 28%…in urine, 24%…in feces, p-hydroxysulfinylpyrazol was found in bile.
Known human metabolites of sulfinylpyrazolone include sulfinylpyrazolone sulfone.
Sulfurylpyrazolone is a known human metabolite of sulfinylpyrazolone sulfide.
Biological half-life
Approximately 4-6 hours

Protein Binding
98-99% Interaction ... The uricosuric effect of sulfinpyrazone is additive with that of probenecid and phenylbutazone, but antagonistic with that of salicylates. ...It can displace other organic anions that are widely bound to plasma proteins... thereby altering their distribution in tissues and their renal excretion... ...Sulpyrazone may enhance the effects of insulin and oral hypoglycemic agents... ...Sulpyrazone may displace sulfonamides from their plasma protein binding sites...

[1]. Margulies EH, White AM, Sherry S. Sulfinpyrazone: a review of its pharmacological properties and therapeutic use. Drugs. 1980;20(3):179‐197.

[2]. Rüegg M. Antithrombotic effects of sulfinpyrazone in animals: influence on fibrinolysis and sodium arachidonate-induced pulmonary embolism. Pharmacology. 1976;14(6):522‐536.

Sulfopyrrolidone is a sulfoxide compound belonging to the pyrazolidine class. It is a uricosuric drug used to lower serum uric acid levels during gout treatment. It does not have anti-inflammatory, analgesic, or diuretic effects. Sulfopyrrolidone is a derivative of phenylbutazone and has uricosuric and antithrombotic effects. Sulfopyrrolidone works by competitively inhibiting the reabsorption of uric acid in the proximal tubules of the kidney. The drug acts on organic anion transport exchangers, thereby increasing uric acid excretion, lowering serum uric acid levels, and preventing uric acid deposition. Sulfopyrrolidone can also block the renal tubular excretion of various acidic drugs, leading to increased serum concentrations of these drugs. Furthermore, sulffopyrrolidone and its active metabolites inhibit the synthesis of thromboxane A2 by competitively inhibiting cyclooxygenase activity, thereby restoring platelet survival time to normal levels and reducing platelet adhesion to subendothelial cells, thus preventing platelet aggregation. It does not possess anti-inflammatory, analgesic, or diuretic effects. Indications: For the treatment of gout and gouty arthritis. Mechanism of Action: Sulfapyridine is an oral uricosuric drug (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfapyridine promotes uric acid excretion by competitively inhibiting the reabsorption of uric acid in the proximal renal tubules, thereby reducing plasma uric acid concentration. This may be achieved by inhibiting uric acid anion transporter 1 (hURAT1) and human organic anion transporter 4 (hOAT4). Sulfapyridine is not suitable for treating acute attacks because it lacks effective analgesic and anti-inflammatory effects. Sulfapyridine and its sulfide metabolites have cyclooxygenase (COX) inhibitory activity. Sulfapyridine has also been shown to be a UDP-glucuronyl transferase inhibitor and a potent CYP2C9 inhibitor. Sulfanilamide is also an inhibitor of cystic fibrosis transmembrane transport regulator (CFTR) and a multidrug resistance protein (MRP) inhibitor. At adequate doses, it potently inhibits renal tubular reabsorption of uric acid. Low doses may reduce uric acid excretion, presumably by inhibiting secretory transport rather than reabsorption transport. It competitively inhibits the secretion of other organic anions by the renal tubules, such as para-aminohippuric acid (PAH) and salicylic acid.

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Therapeutic Uses
Uric Acid Excretory Agents
Example Uses: Sulfanilamide…prolongs platelet survival time in humans.…inhibits platelet aggregation of collagen and antigen-antibody complexes, but has no inhibitory effect on ADP or thrombin aggregation…appearing to be associated with reduced ADP and serotonin release.…its preventative value in thromboembolic diseases is under investigation. Sulfanilamide USP…officially available in 100 mg tablets and 200 mg capsules. For the treatment of… chronic gout, the initial dose is 100-200 mg/day. After the first week, the dose is gradually increased until plasma uric acid levels are reached and maintained at a satisfactory reduction. It may be necessary to take 100-400 mg daily, divided into 2-4 doses, preferably with food. A small number of refractory patients have been successfully treated with doses up to 800 mg daily. Higher doses are poorly tolerated and unlikely to produce further uric acid-lowering effects in refractory patients. For well-responsive patients, a single daily dose of 100 mg may sometimes be sufficient for maintenance therapy. For more complete data on the therapeutic uses of sulfinpyrazone (10 in total), please visit the HSDB record page. Drug Warnings Sulfanilamide lacks the significant clinical anti-inflammatory and analgesic properties of its homologue, phenbuprofen. Gastrointestinal irritation occurs in 10-15% of patients… A small number of patients may require discontinuation of the drug. The frequency and severity of irritation increase with increasing dose… Divided doses with food can reduce discomfort. ...Use with caution only in patients with a history of peptic ulcer disease, and close monitoring is required. ...This drug has been shown to inhibit hematopoiesis...Therefore, regular blood cell counts are recommended during long-term treatment. Adequate precautions must also be taken to prevent urate deposition in the kidneys... ...When using uricosuric drugs clinically, it must be remembered that they can alter the plasma binding, distribution, and renal excretion of other organic acids...whether these organic acids are naturally occurring...or the drug and its metabolites. /Uric Acid/ ...For more complete data on drug warnings for sulfinpyrazone (8 in total), please visit the HSDB record page. ...Pharmacodynamics ...The pharmacological activity of sulfinpyrazone is to enhance uric acid excretion. It can be used to lower serum uric acid levels in patients with chronic tophi and acute intermittent gout, and to promote the absorption of tophi.

C23H20N2O3S

404.4815

404.119

57-96-5

5342

White to off-white solid powder

1.4±0.1 g/cm3

590.8±42.0 °C at 760 mmHg

>300 °C(lit.)

311.1±27.9 °C

0.0±1.7 mmHg at 25°C

1.717

2.3

0

4

6

29

571

0

MBGGBVCUIVRRBF-UHFFFAOYSA-N

InChI=1S/C23H20N2O3S/c26-22-21(16-17-29(28)20-14-8-3-9-15-20)23(27)25(19-12-6-2-7-13-19)24(22)18-10-4-1-5-11-18/h1-15,21H,16-17H2

1,2-diphenyl-4-(2-(phenylsulfinyl)ethyl)pyrazolidine-3,5-dione

G-28315; G28315; G 28315; Sulfinpyrazone; Anturane; Anturanil

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

DMSO : ~33.33 mg/mL (~82.40 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: 2.5 mg/mL (6.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)