Molecular Formula | C21H21NO2S |
Molar Mass | 351.46 |
Density | 1.22±0.1 g/cm3(Predicted) |
Melting Point | 95-98°C |
Boling Point | 499.8±45.0 °C(Predicted) |
Flash Point | 256.1°C |
Solubility | DMSO: >15mg/mL |
Vapor Presure | 4.03E-10mmHg at 25°C |
Appearance | powder |
Color | white to very faintly yellow |
Merck | 14,9081 |
pKa | 0.04±0.29(Predicted) |
Storage Condition | 2-8°C |
Refractive Index | 1.624 |
Physical and Chemical Properties | Off-white or light-yellow solid |
In vitro study | In HL-60 human myeloid leukemia cells, Tazarotene causes ERK activation, RB tumor suppressor protein phosphorylation, G0 arrest, and myeloid differentiation. Tazarotene is able to push the early or late part of the period leading to differentiation or G0 arrest and is interchangeable with RARalpha-selective ligands. Tazarotene modulates three important pathogenic factors in psoriasis by interacting with specific nuclear retinoic acid receptors (RARs) to therapeutically regulate gene transcription. Tazarotene inhibits fibroblast proliferation and synthesis of DNA and collagen. Tazarotene down-regulates keratinocyte differentiation, keratinocyte proliferation, and markers of inflammation. Tazarotene also upregulates three novel genes, TIG-1 (tazarotene-induced gene -1),TIG-2, and TIG-3, which may mediate antiproliferative effects. In retinoid-responsive breast cancer cell lines, Tazarotene causes growth inhibition by upregulating tig3. |
In vivo study | In UV-and ionizing radiation-treated Ptch1 /− mice, Tazarotene treatment reduced the number and size of onlookers basal cell carcinomas (BCCs). |
WGK Germany | 3 |
RTECS | US5675100 |
This product is 6 - [( 3, 4-dihydro-4, 4-dimethyl-2-1-benzothian-6-yl) ethynyl]-3-pyridinecarboxylic acid ethyl ester. The content of C21H21NO2S shall be 98.5% to 101.5% calculated as the dried product.
The melting point of this product (General 0612) is 102~105°C.
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.845 ml | 14.226 ml | 28.453 ml |
5 mM | 0.569 ml | 2.845 ml | 5.691 ml |
10 mM | 0.285 ml | 1.423 ml | 2.845 ml |
5 mM | 0.057 ml | 0.285 ml | 0.569 ml |
take this product, add acetonitrile to dissolve and dilute to make a solution containing about 80ug per lml as a test solution; Take lml from precision children and put it in a 100m l measuring flask, as a control solution, it was diluted to the scale with acetonitrile and shaken. According to the chromatographic conditions under the content determination item, 20 u1 of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 2 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
take this product, at 60°C under reduced pressure drying to constant weight, weight loss should not exceed 1.0% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as a filler; Isopropanol-acetonitrile-water (38:27:35) was used as a mobile phase; The detection wavelength was 325nm. The number of theoretical plates shall not be less than 5000 calculated by tazarotene peak, and the separation degree between tazarotene peak and adjacent impurity peaks shall meet the requirements.
take about 16mg of this product, accurately weigh, put it in a 100ml measuring flask, add acetonitrile to dissolve and dilute to the scale, shake well, take 5ml accurately, put it in a 50ml measuring flask, dilute with acetonitrile to scale, shake, as a test solution, accurately take 20u1 injection liquid chromatography, record chromatogram; Tazarotene control, the same method. According to the external standard method to calculate the peak area, that is.
antikeratotic agents.
sealed and stored in a cool and dry place.
This product contains tazarotene (C21H21N02S) should be 90.0% to 110.0% of the label.
This product is colorless to light yellow gel.
take an appropriate amount of this product (about 0.8mg equivalent to tazarotene), weigh it accurately, put it in a 50ml measuring flask, add an appropriate amount of acetonitrile, and fully shake to dissolve tazarotene, dilute with acetonitrile to the scale, shake, centrifuge, take the supernatant as the test solution, take 20 u1 with precision, and measure according to the method under the content determination item of tazarotene.
Same as tazarotene.
(l )15g:7.5mg (2)30g:15mg (3)30g:30mg
sealed and stored in a cool place.