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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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Rosiglitazone maleate (TDZ01; HSDB-7555; TDZ-01; BRL-49653; trade name Avandia), the maleic acid salt form of rosiglitazone which is an approved anti-diabetic drug, is a thiazolidinedione-based antihyperglycaemic agent with antidiabetic properties and potential antineoplastic activity.
ln Vitro |
Rosiglitazone maleate has an EC50 of 30 nM for PPARγ1 and 100 nM for PPARγ2, respectively, and a Kd of roughly 40 nM for PPARγ, making it a strong and selective PPARγ activator. The development of C3H10T1/2 stem cells into adipocytes is aided by rosiglitazone (BRL49653, 0.1, 1, 10 μM) [1]. With an EC50 of 60 nM, compound 6 (rosiglitazone) activates PPARγ[2]. As PPARγ binds to the NF-κ1 promoter, rosiglitazone (1 μM) promotes gene transcription in neurons. Furthermore, in an NF-κ1-dependent way, rosiglitazone (1 μM) increases BCL-2 expression while shielding Neuro2A cells and hippocampus neurons from oxidative stress [3]. TRPM3 is totally blocked by rosiglitazone against nifedipine- and PregS-induced activity, with IC50 values of 9.5 and 4.6 μM, respectively. However, PPARγ is not involved in this action. An IC50 of roughly 22.5 μM indicates that rosiglitazone inhibits TRPM2 at greater dosages. EC50 of ~30 μM makes rosiglitazone a potent TRPC5 channel stimulant [4].
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ln Vivo |
In diabetic rats, rosiglitazone (5 mg/kg, po) lowers blood glucose levels. Additionally, rosiglitazone decreased the diabetic group's levels of VCAM-1, TNF-α, and IL-6. When rosiglitazone and losartan were combined, blood glucose levels rose in comparison to the diabetes and Los treatment groups. In aortas isolated from diabetic rats, rosiglitazone markedly improves endothelial dysfunction as evidenced by significantly reduced contractile responses to PE and Ang II and increased ACh-induced relaxation [5].
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Animal Protocol |
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References |
[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6.
[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. [3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. [5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220 |
Molecular Formula |
C18H19N3O3S.C4H4O4
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Molecular Weight |
473.5
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CAS # |
155141-29-0
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SMILES |
S1C(N([H])C(C1([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])N(C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=N1)=O)=O.O([H])C(/C(/[H])=C(/[H])\C(=O)O[H])=O
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1119 mL | 10.5597 mL | 21.1193 mL | |
5 mM | 0.4224 mL | 2.1119 mL | 4.2239 mL | |
10 mM | 0.2112 mL | 1.0560 mL | 2.1119 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.