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他扎罗汀

他扎罗汀用途

Tazarotene是选择性视黄酸受体 (RAR) 激动剂,用于治疗斑块状银屑病和寻常痤疮。

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他扎罗汀名称

[ CAS 号 ]:
118292-40-3

[ 中文名 ]:
他扎罗汀

[ 英文名 ]:
Tazarotene

[中文别名 ]:

[英文别名 ]:

Avage
Tazorac
Tazarotene
Zorac
MFCD00867628

他扎罗汀生物活性

[ 描述 ]:

Tazarotene是选择性视黄酸受体 (RAR) 激动剂,用于治疗斑块状银屑病和寻常痤疮。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

研究领域 >> 炎症/免疫

[体外研究]

凝胶和乳膏制剂中的他扎罗汀既可用作单一疗法,也可用作辅助疗法。对于牛皮癣,它已经与类固醇,卡泊三烯和光疗法以及痤疮,抗生素联合使用。他扎罗汀已被证明可上调肿瘤抑制因子,他扎罗汀诱导的基因3,该基因在牛皮癣和皮肤癌中过度表达[1]。在人表皮细胞培养物中,他扎罗汀抑制2种标志物蛋白MRP-8(钙粒蛋白A)和SKALP(皮肤衍生的抗白细胞蛋白酶)的基因表达,在银屑病表皮中高度升高[2]。

[体内研究]

局部凝胶应用提供了他扎罗汀直接递送到皮肤中。在向健康个体和患有银屑病的患者的皮肤局部施用0.1％他扎罗汀凝胶后10小时,约4至6％的剂量存在于角质层中,2％的剂量分布至活表皮和真皮。他扎罗汀被设计为对其活性代谢物他扎罗汀酸进行快速和完全的代谢。 Tazarotenic acid具有较短的全身停留时间和有限的动物组织分布[3]。当局部应用时,他扎罗汀通过肿瘤促进剂12-O-十四烷基佛波醇13-乙酸酯(TPA)阻断鸟氨酸脱羧酶(ODC)活性的诱导。无毛小鼠的表皮[3]。

[参考文献]

[1]. Talpur R, et al. Efficacy and safety of topical tazarotene: a review. Expert Opin Drug Metab Toxicol. 2009 Feb;5(2):195-210.

[2]. Nagpal S, et al. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acidreceptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ. 1996 Dec;7(12):1783-91.

[3]. Tang-Liu DD, et al. Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis. Clin Pharmacokinet. 1999 Oct;37(4):273-87.

[相关活性小分子]

维生素A酸；视黄酸 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 | 他米巴罗汀 | 4-[(1E)-2-[5,6,7,8-四氢-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸 | 芬维A胺 | 芳维甲酸 | 厚朴酚 | AGN 194310 | AGN 193109 | CD 437 | 阿达帕林 | AR7 | UVI 3003 | (R)-氟比洛芬(Tarenflurbil) | AGN 195183

他扎罗汀物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
499.8±45.0 °C at 760 mmHg

[ 熔点 ]:
97-98ºC

[ 分子式 ]:
C₂₁H₂₁NO₂S

[ 分子量 ]:
351.462

[ 闪点 ]:
256.1±28.7 °C

[ 精确质量 ]:
351.129303

[ PSA ]:
64.49000

[ LogP ]:
6.22

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.625

[ 储存条件 ]:
Store at +4°C

他扎罗汀MSDS

详细MSDS(安全技术说明书)

他扎罗汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US5675100

CHEMICAL NAME :: 3-Pyridinecarboxylic acid, 6-((3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl )ethynyl)-, ethyl ester

CAS REGISTRY NUMBER :: 118292-40-3

LAST UPDATED :: 199801

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H21-N-O2-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JAADDB Journal of the American Academy of Dermatology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) 1979- Volume(issue)/page/year: 37(Suppl),S25,1997 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22750 ug/kg/13W-I

TOXIC EFFECTS :: Musculoskeletal - other changes

REFERENCE :: JAADDB Journal of the American Academy of Dermatology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) 1979- Volume(issue)/page/year: 37(Suppl),S25,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 35 mg/kg/26W-I

TOXIC EFFECTS :: Musculoskeletal - other changes

REFERENCE :: JAADDB Journal of the American Academy of Dermatology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) 1979- Volume(issue)/page/year: 37(Suppl),S25,1997

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他扎罗汀安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2942000000

他扎罗汀合成路线

详细合成路线

他扎罗汀上下游产品

他扎罗汀上游产品

他扎罗汀下游产品

他扎罗汀海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

他扎罗汀文献

A custom tailored model to investigate skin penetration in porcine skin and its comparison with human skin.

Eur. J. Pharm. Biopharm. 95 , 99-109, (2015)

Reliable models for the determination of skin penetration and permeation are important for the development of new drugs and formulations. The intention of our study was to develop a skin penetration m...

Tazarotene versus tretinoin or adapalene in the treatment of acne vulgaris.

J. Am. Acad. Dermatol. 43(2 Pt 3) , S51-4, (2000)

The efficacy and tolerability of tazarotene 0.1% gel in the treatment of acne vulgaris have been compared with those of tretinoin 0.025% gel and adapalene 0.1% gel in multicenter, double-blind, random...

Retinoic acid receptor signaling preserves tendon stem cell characteristics and prevents spontaneous differentiation in vitrox.

Stem Cell Res. Ther. 7 , 45, (2016)

Previous studies have reported that adult mesenchymal stem cells (MSCs) tend to gradually lose their stem cell characteristics in vitro when placed outside their niche environment. They subsequently u...

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