| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
SR12813, a 1,1-bisphosphonate ester, is a novel and potent pan retinoid X receptor (RXR) agonist that is devoid of any RAR activity. SR-12813 exhibits hypocholesterolemic activity by enhancing the degradation of HMG-CoA reductase in various animal models. SR-12813 is also a high affinity ligand for human and rabbit pregnane X receptors (Kd = 41 nM; EC50 = 137 nM for hPXR in vitro) and can induce cytochrome P450 3A expression in human and rabbit hepatocytes.
| ln Vitro |
SR-12813 has no effect on the production of fatty acids, however it inhibits the binding of tritiated water to cholesterol with an IC50 of 1.2 μM. Furthermore, with an IC50 of 0.85 μM, SR-12813 can also lower the activity of the cellular 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase[1]. Because they both prevent cholesterol production, 25-HC and SR-12813 are excellent candidates for fatal selection. At doses ranging from 8 µM to 16 µM, SR-12813 kills HeLa cells. While mutant SL-5 is alive in this situation, SR-12813 kills wild-type cells and mutant cells infected with Ad-Cre (SL-5+Cre). In HeLa cells of the wild type and SL-5 mutant cells, SR-12813 or 25-HC stimulates the breakdown of 95-KDa full-length HMG-CoA reductase [1].
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| References |
[1]. Berkhout TA, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.
[2]. Wei Jiang, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632 |
| Molecular Formula |
C24H42O7P2
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|---|---|
| Molecular Weight |
504.53368
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| CAS # |
126411-39-0
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| SMILES |
OC1=C(C(C)(C)C)C=C(/C=C(P(OCC)(OCC)=O)/P(OCC)(OCC)=O)C=C1C(C)(C)C
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| InChi Key |
YQLJDECYQDRSBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H42O7P2/c1-11-28-32(26,29-12-2)21(33(27,30-13-3)31-14-4)17-18-15-19(23(5,6)7)22(25)20(16-18)24(8,9)10/h15-
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| Synonyms |
GW 485801; GW-485801; GW485801; SR 12813; SR-12813; SR12813
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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 : ≥ 50 mg/mL (~99.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.96 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.96 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9820 mL | 9.9102 mL | 19.8204 mL | |
| 5 mM | 0.3964 mL | 1.9820 mL | 3.9641 mL | |
| 10 mM | 0.1982 mL | 0.9910 mL | 1.9820 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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