Tazarotene

Tazarotene
Tazarotene
Tazarotene

Tazarotene

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1 Kilogram

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  • Min.Order :1 Kilogram
  • Purity: 99（%）
  • Payment Terms : L/C,D/A,D/P,T/T,Other

Keywords

Tazarotene 118292-40-3 C21H21NO2S

Quick Details

  • Appearance:powder
  • Application:as medicine material
  • PackAge:25KG/Cardboard bucket or as required
  • ProductionCapacity:5|Metric Ton|Month
  • Storage:Store in dry, dark and ventilated place
  • Transportation:by sea or by air

Superiority:

Tazarotene Basic information
Description Dermatology drugs Adverse reactions and precautions Chemical Properties References
Product Name: Tazarotene
Synonyms: Tazarotene 99% Min SynonyMs Ethyl 6-[2-(4,4-diMethylthiochroMan-6-yl)ethynyl]pyridine-3-carboxylate;Avage;6-[(3,4-Dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl]-3-pyridinecarboxylic acid ethyl ester;ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinate;Tazarotene, >=98%;3-pyridinecarboxylicacid,6-((3,4-dihydro-4,4-dimethyl-2h-1-benzothiopyran-6-y;agn190168;ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate
CAS: 118292-40-3
MF: C21H21NO2S
MW: 351.46
EINECS: 601-516-4
Product Categories: Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Retinoids;Sulfur & Selenium Compounds;Heterocycles;API;Tazorac, Avage, Zora
Mol File: 118292-40-3.mol
Tazarotene Structure
 
Tazarotene Chemical Properties
Melting point  95-98°C
storage temp.  Store at +4°C
solubility  DMSO: >15mg/mL
form  powder
color  white to very faintly yellow
Merck  14,9081
CAS DataBase Reference 118292-40-3(CAS DataBase Reference)
 
Safety Information
WGK Germany  3
RTECS  US5675100
MSDS Information
 
 
Tazarotene Usage And Synthesis
Description Tazarotene belongs to a third generation prescription topical retinoid. It is marketed in different forms including cream (brand name: Avage), foam (brand name: Fabuir) and gel (brand name: Tazorac). It is mainly used for the treatment of psoriasis, acne, and sun damaged skin. The detailed mechanisms of action of Tazarotene are still unclear. It is converted to its active form, the cognate carboxylic acid of tazarotene (AGN 190299) in vivo through rapid de-esterification in animals and man. AGN 190299 is capable of binding to all the three members of the retinoic acid receptor (RAR) family: RARα, RARβ, and RARγ with relative selectivity for RARβ, and RARγ. This process may further modify gene expression. However, it is unclear whether this is related to its mode of action. Common side effects associated with it include worsening of acne, desquamation, burning/stinging, erythema and pruritus increased sensitivity to sunlight, dry skin, itchiness, redness, skin pain rash and skin discoloration. In most cases, these side effects are mild and can remarkable decrease after the first 2–4 weeks. Tazarotene should not be used in the following cases: patients are allergic to it; patients are pregnant; patients have a sunburn; patients are taking photo-sensitive drugs such as thiazides and tetracycline.
Dermatology drugs Tazarotene belongs to the third generation retinoid dermatology drug and is also the retinoid A-like prototype for skin tropical administration and has regulatory effect on epidermal cell differentiation and proliferation. It is mainly used for the treatment of plaque psoriasis vulgaris. Tazarotene cream can also be used for the treatment of facial acne. The clinical administrated product contains an active ingredient of this product being 15mg/30g with its gel being subject to tropical administration. At half an hour before sleep every night, apply appropriate amount of this product into the wounded part. Before treatment, first clean the affected area and apply the drug evenly to the skin lesion part after the dry of the skin for forming a thin film; after applying the drug, the patients should gently rub in order to promote the absorption of drugs. Pea-sized gel can cover a palm-size area of skin lesions. The application area should not exceed 20% of body surface area. Wash hands with soap after rubbing the drug. 
Psoriasis is a common benign, acute or chronic inflammatory skin disease. It occurred on the basis of genetic predisposition. Trauma or irritation of normal skin can induce the occurrence of psoriasis lesions (Koebner phenomenon): There are several different manifestations of psoriasis-the most common is plaque type. Rash type (guttate) psoriasis includes a lot of 3~10mm skin lesions. It may occasionally occur after mental stress or streptococcal pharyngitis. Seriously, there may be occasionally life-threatening forms such as generalized pustular and erythrodermic psoriasis. Sudden onset of plaque type or generalized erythrodermic psoriasis may be associated with HIV infection. 
Tazarotene gel belongs to the topical formulations of formic acid and can be used for the treatment of psoriasis. Early research has shown that: twice daily for topical administration of eight weeks with about 50% patients with mild to moderate psoriasis having at least 75% of their lesions be alleviated. But the completely eliminated plaque number accounts for less than 10%. Tazarotene gel accounts for concentrations of 0.05% and 0.1%. There is no difference on the efficacy of topical administration of 0.1% gel once per day or twice per day. However, tropical administration of the 0.5% gel once per day gives a poor efficacy. 
Tazarotene, as a synthetic ethylene retinal, after topical application, it can be quickly converted to tazarotene acid and plays the pharmacological effects. Tazarotene acid, after binding to the skin retinoid acid receptor-γ (RAR-γ), it can achieve the purpose of alleviating the clinical symptoms through restoring to normal skin differentiation and reducing the inflammation of the skin.
Adverse reactions and precautions Adverse reactions of tazarotene mainly include skin reactions, manifested as itching, burning, stinging, redness, irritation, skin irritation, scaling, dermatitis, chapped, edema, bleaching, drying and bleeding. 
Precautions:
1. For women of childbearing age, within the first 2 weeks before the start of tazarotene gel treatment, we need to perform serum or urine pregnancy test to confirm that the pregnancy test is negative. Start the treatment at the secondary day or third day in the next normal menstrual cycle. Before treatment, during treatment and for some time after cessation of treatment, the patients must use effective contraceptive methods.
2. Avoid contact between drug and eyes, mouth and mucous membrane; try to avoid the contact between skin and the drug. In case of contact with eyes, rinse thoroughly with water.
3. In cases of skin irritation such as itching, try not to scratch and can apply with a small amount of emollient; in severe case, you should stop using this drug or administer at the next day.
4. This product is not recommended for treating acute eczema.
5. During the treatment, avoid excessive exposure to the sun. You should also avoid simultaneously administration of taking photosensitive drug.
6. After application of the drug, avoid using clothing and bandaging for affected area. You should avoid using pharmaceuticals and cosmetics which can dry the skin. Safety information regarding to the applied area should not exceed 20% of the body surface area has not been established.
7. It should be contraindicated in pregnant and lactating women. For this drug, patients allergic to other aldehydes retinol or vitamin A derivative should be tabooed.
8. Safety and efficacy regarding to the children under age 12 for using tazarotene has not been established.
The above information is edited by the chemicalbook of Dai Xiongfeng.
Chemical Properties It is as white-like or pale yellow solid.
References #;
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Chemical Properties White Solid
Uses An acetylenic retinoid prodrug converted to the active metabolite, Tazarotenic acid, with selective affinity for retinoic acid receptors RAR and RAR. Antiacne; antipsoriatic. Used in treatment of photodamaged skin
Uses An acetylenic retinoid prodrug converted to the active metabolite, Tazarotenic acid, with selective affinity for retinoic acid receptors RARβ and RARγ. Antiacne; antipsoriatic. Used in treatment of photodamaged skin.
Uses Tazarotene is a prescription topical retinoid sold as a cream or gel. This medication is approved for treatment of psoriasis, acne, and sun damaged skin (photodamage). It is commonly sold in two concentrations: 0.05% and 0.1%. In addition to tretinoin, wh
Uses anticholelithic
Uses Used to treat psoriasis, acne and sun damaged skin.
Definition ChEBI: The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.
Indications Like other retinoids, tazarotene (Tazorac) acts by binding to RARs and altering gene expression. Tazarotene appears to be particularly selective for the retinoid receptors RAR-β and RAR-γ, but the clinical significance of this observation is unknown.
Brand name Avage (Allergan); Tazorac (Allergan).
Clinical Use In the United States, tazarotene has been approved for topical treatment of psoriasis (involving up to 20% body surface area) and mild to moderate facial acne. Application site burning, stinging, and desquamation are common side effects, especially with acne. Tazarotene is contraindicated in women who are pregnant.

 

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