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Purity: ≥98%
SW033291 (SW-033291; SW 033291) is a selective and high affinity inhibitor of the prostaglandin-degrading enzyme 15-PGD (15-hydroxyprostaglandin dehydrogenase) with potential kidney and liver protective effects. It inhibits 15-PGDH with an IC50 and Kiapp of 1.5 nM and 0.1 nM, respectively. Inhibition of 15-PGDH by SW033291 could alleviate lipopolysaccharide (LPS)-induced acute kidney injury (AKI) by regulating the apoptosis, autophagy, and oxidative stress rather than inflammation in mice.
| ln Vitro |
After applying SW033291 to the cells, the activity of the 15-PGDH enzyme is reduced by 85%. Up to 40 μM PGE2, SW033291's inhibition of 15-PGDH was non-competitive when compared to PGE2. PGE2 levels are increased by 3.5 times at 500 nM upon treatment of A549 cells with SW033291, and the EC50 50 is at roughly 75 nM[1].
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| ln Vivo |
Significant advantages are observed in C57BL/6J mice treated with SW033291 (10 mg/kg; intraperitoneal injection; twice daily; for 3 days) for three days in a row. These include a doubling of peripheral neutrophil counts, a 65% increase in marrow SKL cells, and a 71% increase in marrow SLAM cells[1].
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| Animal Protocol |
Animal/Disease Models: C57BL/6J mice[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; twice (two times) daily; for 3 days (for 5 doses) Experimental Results: demonstrated significant benefits, including a doubling of peripheral neutrophil counts, a 65% increase in marrow SKL cells, and a 71% increase in marrow SLAM cells. |
| References |
[1]. Zhang Y, et al. TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015 Jun 12;348(6240):aaa2340.
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| Molecular Formula |
C21H20N2OS3
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| Molecular Weight |
412.59
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| CAS # |
459147-39-8
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| Related CAS # |
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| SMILES |
S(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])(C1=C(C2=C(N=C(C3=C([H])C([H])=C([H])S3)C([H])=C2C2C([H])=C([H])C([H])=C([H])C=2[H])S1)N([H])[H])=O
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| InChi Key |
LCYAYKSMOVLVRL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N2OS3/c1-2-3-12-27(24)21-19(22)18-15(14-8-5-4-6-9-14)13-16(23-20(18)26-21)17-10-7-11-25-17/h4-11,13H,2-3,12,22H2,1H3
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| Chemical Name |
2-(Butylsulfinyl)-4-phenyl-6-(2-thienyl)-thieno[2,3-b]pyridin-3-amine
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: 2.5 mg/mL (6.06 mM) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% 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 EtOH 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. View More
Solubility in Formulation 3: 2.5 mg/mL (6.06 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 900 μL of corn oil and mix well. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4237 mL | 12.1186 mL | 24.2371 mL | |
| 5 mM | 0.4847 mL | 2.4237 mL | 4.8474 mL | |
| 10 mM | 0.2424 mL | 1.2119 mL | 2.4237 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.
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