| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Stannsoporfin targets heme oxygenase (HO), specifically the HO-1 isoform, by acting as a competitive inhibitor. Heme oxygenase is the rate-limiting enzyme in the catabolism of heme to biliverdin, which is subsequently converted to bilirubin. By inhibiting heme oxygenase, stannsoporfin blocks the conversion of heme into bilirubin, thereby reducing bilirubin production and preventing hyperbilirubinemia. This mechanism of action specifically targets the enzyme responsible for bilirubin formation, making stannsoporfin a targeted approach to managing neonatal jaundice.
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| ln Vitro |
In vitro, stannsoporfin has been shown to effectively inhibit heme oxygenase activity in cell-free systems. As a competitive inhibitor of HO, it binds to the enzyme's active site and prevents the catalysis of heme to biliverdin. The compound's inhibitory activity has been characterized in enzyme assays using purified heme oxygenase or tissue homogenates. Stannsoporfin has also demonstrated activity in enhancing the bactericidal activity of a novel regimen for multidrug-resistant tuberculosis in a murine model.
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| ln Vivo |
In vivo, stannsoporfin has been evaluated for its ability to reduce bilirubin levels in animal models and human infants. As a heme oxygenase inhibitor, it effectively decreases the production of bilirubin, thereby preventing the development of jaundice in at-risk infants. Studies have also investigated stannsoporfin's potential in the treatment of intracerebral hemorrhage. The compound has shown activity in modifying heme-iron levels in the intestine and has been found active against intracerebral trauma.
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| Enzyme Assay |
In non-cell-based enzyme assays, stannsoporfin's inhibition of heme oxygenase is evaluated using spectrophotometric or fluorometric methods. HO activity is typically measured by monitoring the conversion of heme to biliverdin, which can be detected by absorbance at specific wavelengths. The assay mixture contains heme as substrate, NADPH as cofactor, and varying concentrations of stannsoporfin. The rate of biliverdin formation is measured in the presence and absence of the inhibitor to determine the IC50 and inhibition constant (Ki). This approach confirms stannsoporfin's role as a competitive inhibitor of HO.
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| Cell Assay |
In vitro cellular assays for stannsoporfin involve measuring its effects on heme oxygenase activity in cultured cells. Cells such as hepatocytes or macrophages are treated with stannsoporfin, and HO activity is assessed by measuring bilirubin production or carbon monoxide release. The compound's ability to inhibit HO-1 expression or activity in response to oxidative stress or heme stimulation can also be evaluated. These cellular assays complement the non-cell-based enzyme studies and provide information on the compound's activity in a more physiological context.
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| Animal Protocol |
In vivo animal studies for stannsoporfin have been conducted in murine models. The heme oxygenase-1 metalloporphyrin inhibitor stannsoporfin has been shown to enhance the bactericidal activity of a novel regimen for multidrug-resistant tuberculosis in a murine model. Studies have also investigated its effects in models of intracerebral hemorrhage and its ability to modify heme-iron levels. In infant animal models, stannsoporfin has been evaluated for its ability to prevent hyperbilirubinemia by inhibiting heme oxygenase and reducing bilirubin production.
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| ADME/Pharmacokinetics |
Stannsoporfin's pharmacokinetic properties have been characterized in preclinical and clinical studies. As a metalloporphyrin, it is administered intravenously. The compound's distribution, metabolism, and elimination are influenced by its porphyrin structure. Stannsoporfin has been shown to modify heme-iron levels in the intestine. The pharmacokinetic profile supports its use as a single or limited-dose intervention for the prevention of hyperbilirubinemia. Studies have investigated the use of low dosages of stannsoporfin for the treatment of infant hyperbilirubinemia.
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| Toxicity/Toxicokinetics |
The toxicological profile of stannsoporfin has been evaluated in preclinical studies. As with other metalloporphyrins, potential toxicities may include photosensitivity, oxidative stress, and effects on heme-dependent enzymes. However, stannsoporfin has been developed specifically for use in infants, and safety assessments have focused on its risk-benefit profile for the prevention of jaundice. The compound is generally well-tolerated at therapeutic doses. Long-term safety data are limited, and ongoing studies continue to evaluate its safety in the target population.
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| Additional Infomation |
Stannsoporfin has been developed by InfaCare, a subsidiary of WellSpring Pharmaceuticals, for the prevention of hyperbilirubinemia in infants at risk of developing jaundice. Its mechanism of action specifically inhibits the enzyme that blocks the conversion of heme into bilirubin. The compound has been evaluated in clinical trials and is intended for use in neonates. Stannsoporfin represents a targeted approach to managing neonatal jaundice by directly inhibiting the enzyme responsible for bilirubin production, potentially reducing the need for phototherapy or exchange transfusion.
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| Molecular Formula |
C34H36CL2N4O4SN
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|---|---|
| Molecular Weight |
754.29
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| Exact Mass |
754.114
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| CAS # |
106344-20-1
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| PubChem CID |
15978579
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| Appearance |
Brown to reddish brown solid powder
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| Boiling Point |
1096.1ºC at 760mmHg
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| Flash Point |
616.7ºC
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| Vapour Pressure |
0mmHg at 25°C
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| LogP |
1.887
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
45
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| Complexity |
949
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Cl-][Sn+4]123([N-]4C5C(C)=C(CC)C4=CC4C(C)=C(CC)C(=CC6=C(C)C(CCC(=O)[O-])=C(C=C7C(CCC(=O)[O-])=C(C)C(C=5)=N17)[N-]26)N3=4)[Cl-].[H+]
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| Chemical Name |
Stannate(2-), dichloro(7,12-diethyl-3,8,13,17-tetramethyl-21H,23H-porphine-2,18-dipropanato(4-)-N21,N22,N23,N24)-, dihydrogen, (OC-6-13)-
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| Synonyms |
Stannsoporfin. tin (IV) mesoporphyrin IX dichlorideStannsoporfin USAN SNMPP SnMP Sn MesoporphyrinTin mesoporphyrin Stanate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5.56 mg/mL (~7.37 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (0.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 5.6 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3258 mL | 6.6288 mL | 13.2575 mL | |
| 5 mM | 0.2652 mL | 1.3258 mL | 2.6515 mL | |
| 10 mM | 0.1326 mL | 0.6629 mL | 1.3258 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00076960 | NO LONGER AVAILABLE | Drug: Stanate (TM) [stannsoporfin, tin-mesoporphyrin] | Hyperbilirubinemia Neonatal Jaundice |
InfaCare Pharmaceuticals Corporation, a Mallinckrodt Company | ||
| NCT02685137 | COMPLETED | Drug: stannsoporfin Other: Sham Injection |
Nutritional and Metabolic Diseases | InfaCare Pharmaceuticals Corporation, a Mallinckrodt Company | 2002-05-01 | Phase 3 |
| NCT02000830 | COMPLETED | Drug: Stannsoporfin Drug: Placebo |
Hyperbilirubinemia, Neonatal | InfaCare Pharmaceuticals Corporation, a Mallinckrodt Company | 2013-10-17 | |
| NCT00115544 | COMPLETED | Drug: Stanate | Hyperbilirubinemia | InfaCare Pharmaceuticals Corporation, a Mallinckrodt Company | 2005-09 | Phase 2 |
| NCT01887327 | COMPLETEDWITH RESULTS | Procedure: Phototherapy Drug: Stannsoporfin Drug: Placebo |
Hyperbilirubinemia, Neonatal Jaundice, Neonatal |
InfaCare Pharmaceuticals Corporation, a Mallinckrodt Company | 2013-10-16 | Phase 2 |
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