DMOG
DMOG атрибут
Температура плавления: |
46-48°C |
Температура кипения: |
179-182 °C(Press: 12 Torr) |
плотность: |
1.246±0.06 g/cm3(Predicted) |
температура хранения: |
-20°C |
растворимость: |
Н2О: >30мг/мл |
пка: |
10.55±0.46(Predicted) |
форма: |
Твердый |
цвет: |
От белого до не совсем белого |
Растворимость в воде: |
Растворим в воде при концентрации 30 мг/мл. |
Стабильность:: |
Раствор должен быть приготовлен и использован на месте. |
безопасность
- Заявления о рисках и безопасности
- код информации об опасности(GHS)
Коды опасности |
Xi,Xn |
Заявления о рисках |
22 |
WGK Германия |
3 |
кода HS |
2924.19.8000 |
Класс опасности |
IRRITANT |
символ(GHS) |
|
сигнальное слово |
Warning |
Заявление об опасности |
пароль |
Заявление об опасности |
Класс опасности |
категория |
сигнальное слово |
пиктограмма |
предупреждение |
H302 |
Вредно при проглатывании. |
Острая токсичность, пероральная |
Категория 4 |
Предупреждение |
|
P264, P270, P301+P312, P330, P501 |
|
Внимание |
P301+P312+P330 |
ПРИ ПРОГЛАТЫВАНИИ: Обратиться за медицинской помощью
при плохом самочувствии. Прополоскать рот. |
|
DMOG химические свойства, назначение, производство
Описание
The pro-angiogenic factor HIF-1α is targeted for destruction in normoxic environments by the hydroxylation of a specific proline residue, P564, by the oxygen-sensing enzyme HIF-1α prolyl hydroxylase (HIF-PH). DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM. DMOG is therefore expected to act as a pro-angiogenic compound, acting via the HIF-1α system.
Химические свойства
Off-White to Pale Pink Solid
Использование
DMOG is a cell permeable prolyl-4-hydroxylase inhibitor which upregulates HIF activity. HIF activation stimulates angiogenesis in several different models (1nM). DMOG also inhibits FIH (factor inhibiting HIF), an asparaginyl hydroxylase, which enhances the HIF response. It is active in vivo and attenuates myocardial injury in a rabbit ischemia reperfusion model (20mg/Kg).
Ферментативный ингибитор
This iron-binding a-ketoglutarate (2-oxoglutarate) analogue (FW = 147.09
g/mol; also named N-oxaloglycine) competitively inhibits prolyl-4-
hydroxylase (Reaction: Procollagen (L-proline) + a-ketoglutarate + O2 →
Procollagen ( (2S,4R) -4-hydroxyproline) + succinate + CO2). During
catalysis, prolyl-4-hydroxylase forms Fe (III), and the latter most likely
makes an extremely stable metal ion complex with N-oxaloglycine.
Substitution on the glycine moiety alters inhibitor activity stereoselectively
and that, if the w-carboxylate is homologated or replaced, either by
acylsulfonamides or anilide, activity is likewise sharply reduced. Prolyl-
4-Hydroxylase Catalysis: Each catalytic round of this posttranslational
modifying enzyme reaction occurs in two stages. O2 is bound end-on in an
axial position, producing a dioxygen unit. Nucleophilic attack at C-2
generates a tetrahedral intermediate, with loss of the double bond in
dioxygen and bonds to iron and the a-carbon of a-ketoglutarate.
Elimination of CO2 coincides with formation of the Fe (IV) =O species. The
second stage involves the abstraction of the pro-R hydrogen atom from C-4
of proline, followed by radical combination, yielding hydroxyproline. In
the presence of a-ketoglutarate, enzyme-bound Fe2+ is rapidly converted to
Fe3+, resulting in inactivation of the enzyme Ascorbate is utilized as a
cofactor to reduce Fe (III) back to Fe (II). Cell-Permeable Analogue:
Dimethyloxalylglycine (FW = 175.14 g/mol; CAS 89464-63-1; Symbol:
DMOG, also named N- (methoxyoxoacetyl) -glycine methyl ester) is
metabolicaly demethylated to form N-oxaloglycine upon entry to many
cells.
DMOG препаратная продукция и сырье
сырьё
препарат
DMOG поставщик
Global( 123)Suppliers
89464-63-1()подобный поиск: