Rosiglitazone maleate
Rosiglitazone maleate атрибут
Температура плавления: |
235-240°C |
температура хранения: |
2-8°C |
растворимость: |
Растворим в ДМСО (до 50 мг/мл). |
пка: |
6.1; 6.8(at 25℃) |
форма: |
белый порошок |
цвет: |
белый |
BCS Class: |
1 |
Стабильность:: |
Растворы в ДМСО можно хранить при температуре -20°C до 3 месяцев. |
ИнЧИКей: |
HCDYSWMAMRPMST-NTCAYCPXSA-N |
Справочник по базе данных CAS: |
155141-29-0(CAS DataBase Reference) |
Словарь онкологических терминов NCI: |
rosiglitazone maleate |
FDA UNII: |
KX2339DP44 |
Словарь наркотиков NCI: |
rosiglitazone maleate |
Rosiglitazone maleate химические свойства, назначение, производство
Описание
Rosiglitazone maleate, belongs to a novel class of thiazolidine diones
launched for the treatment of non-insulin-dependent diabetes mellitus (NIDDM),
a disease characterized by a pancreatic β-cell defect and insulin resistance in
the liver and peripheral tissues. The racemic base can be obtained by
KnSvenagel condensation between 2, 4-thiazolidinedione and the corresponding
4-substituted benzaldehyde (itself prepared in 2 steps from 2-chloropyridine),
followed by reduction of the benzylidene. Rosiglitazone was shown to be a
potent agonist of peroxisome proliferator activated receptor-gamma (PPARgamma),
a nuclear receptor involved in the differentiation of adipose tissue,
without activating liver PPAR-alpha receptors. This activation of PPAR-gamma
could mediate the down-regulation of leptin gene expression. In animal models,
Rosiglitazone has been shown to normalize glucose metabolism and reduce the
exogenous dose of insulin needed to achieve glycemic control. In patients with
Type II diabetes, daily doses (4 or 8 mg) of Rosiglitazone significantly improved
blood sugar control without affecting cardiac structure or function.
Химические свойства
White To Off-White Solid
Использование
Insulin sensitizer; binds to peroxisome proliferator activated receptor gamma (PPAR- γ).
Показания
Rosiglitazone maleate is an antihyperglycemic agent in the thiazolidinedione class. It is indicated for the treatment of patients with type 2 diabetes mellitus.
Общее описание
A thiazolidinedione compound that acts as an anti-diabetic agent and serves as a potent and selective agonist of peroxisome proliferator-activated receptor-g (PPARg) (Kd ~40 nM) in fat cells. Shown to reduce fatty acid uptake and ameliorate lipid metabolism and insulin resistance in animal models of type II diabetes. Reported to activate both a1- and a2-containing AMPK complexes. Unlike troglitazone, it does not induce the activity of P4503A4. Significantly improves the differentiation of C3H10T1/2 stem cells into adipocytes. Shown to block estrogen synthesis by interfering with androgen binding to aromatase, but without affecting aromatase mRNA or protein expression.
Rosiglitazone maleate препаратная продукция и сырье
сырьё
препарат
Rosiglitazone maleate поставщик
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