GlpBio

TTNPB (Arotinoid Acid)

目录号: GC14273纯度: >99.00%同义词: Ro 13-7410; Arotinoid acid; AGN191183
A potent, selective RAR agonist
TTNPB (Arotinoid Acid)
Cas No.: 71441-28-6
规格价格库存数量操作
1mg¥192.00现货
1
5mg¥560.00现货
1
10mg¥735.00现货
1
25mg¥1,250.00现货
1
50mg¥1,974.00现货
1
100mg¥2,912.00现货
1
10mM (in 1mL DMSO)¥616.00现货
1
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产品描述 Description

TTNPB (Arotinoid Acid) is an agonist of RAR with IC50 values of 3.8nM, 4nM and 4.5nM for RARα, RARβ and RARγ, respectively [1].

TTNPB is a teratogen with 1000-fold higher potency than tRA. TTNPB inhibits chondrogenesis with IC50 value of 0.14nM when using mouse limb bud cell cultures. The action of TTNPB results from binding to nuclear receptors. TTNPB can competes with [3H]tRA and prevent them from binding to mRARα, mRARβ and mRARγ with IC50 values of 3.8nM, 4nM and 4.5nM, respectively. Besides that, TTNPB also directly binds to mRARs with high potency. The Kd values are 2.5nM, 2.7nM and 1.8nM for mRARα, mRARβ and mRARγ, respectively. Moreover, TTNPB is reported to bind to mCRABPI and mCRABPII with 27-fold and 3.5-fold lower affinity than tRA [1].

References:
[1] Pignatello M A, Kauffman F C, Levin A A. Multiple factors contribute to the toxicity of the aromatic retinoid, TTNPB (Ro 13-7410): Binding affinities and disposition. Toxicology and applied pharmacology, 1997, 142(2): 319-327.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human mammary epithelial cell line 184 and T47D breast cancer cells

Preparation method

The solubility of this compound in DMSO is > 17.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 μM

Applications

In the normal human mammary epithelial cell line 184, TTNPB inhibited cell growth. In T47D cells, TTNPB arrested the cell cycle in the G0/G1 phase and induced apoptosis. Further study showed that TTNPB induced cell cycle blockade mainly by suppressing Cyclin D1 and Cyclin D3 protein activity. But TTNPB did not change the expression of Cyclin D1 protein in a biologically relevant manner.
Animal experiment [2]:

Animal models

Mice bearing hormone-sensitive (HS) and hormone-insensitive (HI) strains of the MXT murine mammary carcinoma

Dosage form

0.25 mg/kg; i.p.

Applications

In both MXT-HS and MXT-HI models, TTNPB exhibited equal inhibition on tumor growth. Comparing with Tamoxifen, TTNPB was markedly more efficient in inhibiting cell proliferation and triggering apoptosis. TTNPB inhibited MXT-HS growth rate by inducing apoptosis rather than inhibiting cell proliferation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wu K, DuPré E, Kim H, Tin-U CK, Bissonnette RP, Lamph WW, Brown PH. Receptor-selective retinoids inhibit the growth of normal and malignant breast cells by inducing G1 cell cycle blockade. Breast Cancer Res Treat. 2006 Mar;96(2):147-57.

[2]. Darro F, Cahen P, Vianna A, Decaestecker C, Nogaret JM, Leblond B, Chaboteaux C, Ramos C, Pétein M, Budel V, Schoofs A, Pourrias B, Kiss R. Growth inhibition of human in vitro and mouse in vitro and in vivo mammary tumor models by retinoids in comparison with tamoxifen and the RU-486 anti-progestagen. Breast Cancer Res Treat. 1998 Sep;51(1):39-55.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
71441-28-6
同义词
Ro 13-7410; Arotinoid acid; AGN191183
化学名
4-[(E)-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)prop-1-enyl]benzoic acid
SMILES
CC(=CC1=CC=C(C=C1)C(=O)O)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C
分子式
C24H28O2
分子量
348.48 g/mol
溶解性
≥ 17.4mg/mL in DMSO
保存条件
4°C, protect from light
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol