Cyclooxygenase-1 (COX-1) [] [1][2]
- Cyclooxygenase-2 (COX-2) [] [1][2]

The NSAID Suprofen (TN-762) is used. Suprofen (TN-762) is an antipyretic and anti-inflammatory analgesic that works similarly to ibuprofen. It has been suggested that it possesses anti-arthritic properties and inhibits prostaglandin synthesis. 200 mg of prostanoids is preferred, saving 6-keto PGF1a[1].

Suprofen combined with PGF2 alpha blocks induction of uterine contractions, suggesting the possibility that Suprofen also antagonizes PGF2 alpha receptor binding. Suprofen are effective at preventing BAB disruption after paracentesis in dogs, indicating their potential usefulness for treatment of prostaglandin-mediated ocular disease. Suprofen (3.7 mg/kg, i.v.) induces a marked decrease in the firing evoked in arthritic rats by ankle mobilization.

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In women with primary dysmenorrhea, oral administration of Suprofen (TN-762) (400 mg three times daily during menstruation) differentially suppressed menstrual fluid prostaglandins. It inhibited prostaglandin F2α (PGF2α) by 68%, prostaglandin E2 (PGE2) by 72%, 6-keto-prostaglandin F1α (6-keto-PGF1α) by 55%, and thromboxane B2 (TXB2) by 42% compared to baseline levels [2]
- The suppression of prostaglandins was associated with a significant reduction in dysmenorrheal pain intensity, with 75% of patients reporting moderate to marked pain relief [2]

Metabolism / Metabolites
Primarily metabolized in the liver (mainly via cytochrome P450 isoenzyme 2C9). Known human metabolites of sulprofen include thiophene-4,5-epoxide, (2S,3S,4S,5R)-3,4,5-trihydroxy-6-[2-[4-(thiophene-2-carbonyl)phenyl]propionyloxy]oxacyclohexane-2-carboxylic acid, and sulprofen sulfoxide.

Protein binding
20%
In long-term animal studies (6 months), sulprofen did not cause significant changes in body weight, hematological parameters (erythrocytes, leukocytes, platelets) or serum biochemical parameters (ALT, AST, creatinine, urea nitrogen) in rats at doses up to 100 mg/kg/day and in dogs at doses up to 45 mg/kg/day[1]
-Mild gastrointestinal irritation (gastric mucosal congestion) was observed in rats at the highest dose (100 mg/kg/day) and dogs at 45 mg/kg/day, but no ulcers or serious lesions were found[1]
-In clinical use for the treatment of primary dysmenorrhea, sulprofen showed mild and transient side effects, mainly gastrointestinal discomfort (nausea, abdominal cramps, diarrhea)[2]

[1]. Suprofen. An overview of long-term safety. Pharmacology, 1983. 27 Suppl 1: p. 87-94.

[2]. Dawood, M.Y. and F.S. Khan-Dawood, Differential suppression of menstrual fluid prostaglandin F2a, prostaglandin E2, 6-keto prostaglandin F1a and thromboxane B2 by suprofen in women with primary dysmenorrhea. Prostaglandins Other Lipid Mediat, 2007. 83(1-2): p. 146-53.

Suprofen is an aromatic ketone with a thiophene ring structure, where the C-2 position is substituted with a 4-(1-carboxyethyl)benzoyl group. It is a nonsteroidal anti-inflammatory drug (NSAID), a non-narcotic analgesic, an EC 1.14.99.1 (prostaglandin intraperoxidase) inhibitor, an antirheumatic drug, a peripheral nervous system drug, and a drug allergen. It belongs to the thiophene class of compounds, monocarboxylic acids, and aromatic ketones. Suprofen is an ibuprofen-based anti-inflammatory, analgesic, and antipyretic drug. It inhibits prostaglandin synthesis and was once considered to have potential anti-arthritis properties. Currently, suprofen is no longer approved for use in the United States. Suprofen is an ibuprofen-based anti-inflammatory, analgesic, and antipyretic drug. It inhibits prostaglandin synthesis and was considered to have potential anti-arthritis properties. Drug Indications Used as eye drops to inhibit pupillary constriction that may occur during ophthalmic surgery. Mechanism of Action Suprofen binds to cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes, inhibiting prostaglandin synthesis and reducing inflammation. Cyclooxygenases catalyze the conversion of arachidonic acid (which itself is derived from the phospholipid bilayer of cells by phospholipase A2) into prostaglandins and thromboxanes. Prostaglandins (among other functions) act as messenger molecules in the inflammatory process. The end result is reduced eye pain and inflammation, and prevention of pupillary constriction during surgery. Typically, trauma to the anterior segment of the eye (especially the iris) increases the synthesis of endogenous prostaglandins, leading to iris sphincter contraction. Pharmacodynamics Suprofen is a nonsteroidal anti-inflammatory drug (NSAID). Ocular anti-inflammatory drugs are used to alleviate problems that may occur during or after certain ophthalmic surgeries. Sometimes, pupillary constriction (pupil vasoconstriction) occurs during surgery, making it difficult for surgeons to access certain areas of the eye. Suprofen is used to help prevent this condition. Suprofen (TN-762) is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory effects, primarily used to treat primary dysmenorrhea[1][2]. Its mechanism of action is to inhibit cyclooxygenases (COX-1 and COX-2), thereby reducing the biosynthesis of prostaglandins that mediate pain and inflammation[1][2]. Animals have shown good tolerability after long-term administration (up to 6 months), with no cumulative toxicity or organ damage observed at therapeutic doses[1]. The drug exhibits varying inhibitory effects on various prostaglandins in menstrual fluid, with stronger inhibition of PGE2 and PGF2α than on 6-keto-PGF1α and TXB2[2].

C14H12O3S

260.31

260.05

40828-46-4

5359

White to off-white solid powder

1.3±0.1 g/cm3

442.6±30.0 °C at 760 mmHg

278ºC

221.5±24.6 °C

0.0±1.1 mmHg at 25°C

1.613

2.42

1

4

4

18

321

0

MDKGKXOCJGEUJW-UHFFFAOYSA-N

InChI=1S/C14H12O3S/c1-9(14(16)17)10-4-6-11(7-5-10)13(15)12-3-2-8-18-12/h2-9H,1H3,(H,16,17)

2-[4-(thiophene-2-carbonyl)phenyl]propanoic acid

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)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.60 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 (9.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (9.60 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.)