| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
SB 204990, the prodrug of the ATP citrate-lyase inhibitor SB-201076, is a potent, orally available and specific inhibitor of ATP citrate lyase (ACLY) enzyme. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. SB-204990 is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.
| ln Vitro |
The ACLY enzyme is specifically inhibited by SB204990 (SB). Acetylation and active β-catenin levels are predicted to decrease as a result of SB204990 therapy, which lowers cytosolic Ac-CoA levels [1].
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|---|---|
| ln Vivo |
Oral administration of SB 204990 to rats results in its absorption into the systemic circulation. Rats given SB 204990 in the diet (0.05-0.25%, w/w) for one week experienced dose-related decreases in plasma cholesterol (up to 46%) and triglyceride levels (up to 80%). By preferentially lowering LDL cholesterol levels over HDL cholesterol levels, SB 204990 (25 mg/kg daily) also lowers triglyceride levels (up to 38%) and plasma cholesterol levels (up to 23%) in dogs [2].
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| References |
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| Molecular Formula |
C18H22CL2O5
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|---|---|
| Molecular Weight |
389.2703
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| Exact Mass |
388.084
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| CAS # |
154566-12-8
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| PubChem CID |
10340264
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| Appearance |
White to off-white solid powder
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| LogP |
4.007
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
25
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| Complexity |
472
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H](OC(=O)[C@]1(CC(=O)O)O)CCCCCCC2=C(C=C(C=C2)Cl)Cl
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| InChi Key |
YTRNLFYTHYWDAU-RDTXWAMCSA-N
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| InChi Code |
InChI=1S/C18H22Cl2O5/c19-13-8-7-12(15(20)9-13)5-3-1-2-4-6-14-10-18(24,11-16(21)22)17(23)25-14/h7-9,14,24H,1-6,10-11H2,(H,21,22)/t14-,18-/m1/s1
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| Chemical Name |
trans-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid
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| Synonyms |
SB-204990; SB 204990; SB204990
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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 |
| 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 : ≥ 100 mg/mL (~256.89 mM)
H2O : ~25 mg/mL (~64.22 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.34 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 20.8 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: ≥ 2.08 mg/mL (5.34 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.56 mg/mL (6.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5689 mL | 12.8446 mL | 25.6891 mL | |
| 5 mM | 0.5138 mL | 2.5689 mL | 5.1378 mL | |
| 10 mM | 0.2569 mL | 1.2845 mL | 2.5689 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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