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芳维甲酸

芳维甲酸用途

TTNPB 是一种有效的 RAR 激动剂。使用人RARs进行竞争性结合实验中,作用于RARα,RARβ和RARγ,IC50 分别为 5.1 nM,4.5 nM 和 9.3 nM。

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芳维甲酸名称

[ CAS 号 ]:
71441-28-6

[ 中文名 ]:
芳维甲酸

[ 英文名 ]:
TTNPB

[中文别名 ]:

[英文别名 ]:

Ro 13-7410
Arotinoid Acid
MFCD00673917
TTNPB
Tocris-0761
Arotinoic acid
TTNPB (Arotinoid Acid)
Lopac-T-3757

芳维甲酸生物活性

[ 描述 ]:

TTNPB 是一种有效的 RAR 激动剂。使用人RARs进行竞争性结合实验中,作用于RARα,RARβ和RARγ,IC50 分别为 5.1 nM,4.5 nM 和 9.3 nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

研究领域 >> 癌症

[ 靶点 ]

IC50: 5.1 nM (RARα), 4.5 nM (RARβ), 9.3 nM (RARγ)[1]

[体外研究]

对于人RARα,β和γ,TTNPB分别抑制[3H] tRA与3.8nM,4nM和4.5nM的IC50的结合。 TTNPB竞争[3H] tRA与CRABPI的结合,IC50为1800 nM [1]。

[激酶实验]

将标记的和未标记的类视黄醇加入乙醇中的核溶质或胞质级分中，使得所有管中加入的乙醇总量恒定，并且不超过培养体积的2％。将受体制剂与类视黄醇在47℃下孵育4-6小时。 Sephadex PD-10脱盐柱用于在达到平衡后将结合的放射性配体与自由放射性配体分离。对于竞争性结合测定，在固定浓度的[3H] tRA（sp act.49.3 Ci / mmol）或[3H] 9-cis RA（sp）存在下，将不同浓度的未标记的竞争配体与适当的核溶胶或胞质溶胶一起孵育。。动作.24.0 Ci / mmol）。用于核受体结合测定的[3H] tRA和[3H] 9-顺式RA的最终浓度为5nM。 CRABP结合测定的[3H] tRA的最终浓度为30nM。计算IC50。对于饱和动力学，在存在下将增加浓度的放射性标记的配体（[3H] tRA sp。作用49.3Ci / mmol，[3H] TTNPB sp。作用5.5Ci / mmol）加入适当受体亚型的核溶胶中（非特异性结合）或不存在（总结合）100倍摩尔过量的相应未标记的类视黄醇。特异性结合定义为总结合减去非特异性结合。计算饱和动力学[1]。

[参考文献]

[1]. Pignatello MA, et al. Multiple factors contribute to the toxicity of the aromatic retinoid, TTNPB (Ro 13-7410): binding affinities and disposition. Toxicol Appl Pharmacol. 1997 Feb;142(2):319-27.

[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 | 厚朴酚 | AGN 194310 | AGN 193109 | CD 437 | 阿达帕林 | AR7 | 他扎罗汀 | UVI 3003 | (R)-氟比洛芬(Tarenflurbil) | AGN 195183

芳维甲酸物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
486.8±44.0 °C at 760 mmHg

[ 分子式 ]:
C₂₄H₂₈O₂

[ 分子量 ]:
348.478

[ 闪点 ]:
228.6±23.1 °C

[ 精确质量 ]:
348.208923

[ PSA ]:
37.30000

[ LogP ]:
8.62

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.579

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
chloroform/methanol: soluble9.80 - 10.20 mg/mL, clear, colorless to light yellow

芳维甲酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DH6834900

CHEMICAL NAME :: Benzoic acid, 4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphth alenyl)-1-propenyl)-, (E)-

CAS REGISTRY NUMBER :: 71441-28-6

LAST UPDATED :: 199806

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C24-H28-O2

MOLECULAR WEIGHT :: 348.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1040 ug/kg/4D-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 138,169,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1250 ug/kg/25D-I

TOXIC EFFECTS :: Musculoskeletal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 40,3567,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 125 ug/kg/5D-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 138,169,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 392 ug/kg/14D-I

TOXIC EFFECTS :: Musculoskeletal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 34,91,1996 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 ug/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 64,43,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 ug/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 64,43,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 37 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: JJIND8 JNCI, Journal of the National Cancer Institute. (Washington, DC) V.61-79, 1978-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 78,533,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 75 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System

REFERENCE :: JJIND8 JNCI, Journal of the National Cancer Institute. (Washington, DC) V.61-79, 1978-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 78,533,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 290 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: JJIND8 JNCI, Journal of the National Cancer Institute. (Washington, DC) V.61-79, 1978-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 78,533,1987

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芳维甲酸安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H319-H335-H360

[ 警示性声明 ]:
P201-P261-P305 + P351 + P338-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R60

[ 安全声明 (欧洲) ]:
53-26-36/37/39-45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
DH6834900

芳维甲酸合成路线

详细合成路线

芳维甲酸上下游产品

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芳维甲酸文献

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