TTNPB (Arotinoid Acid)
(Synonyms: Ro 13-7410; Arotinoid acid; AGN191183) 目录号 : GC14273
A potent, selective RAR agonist
Cas No.:71441-28-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Human mammary epithelial cell line 184 and T47D breast cancer cells |
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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. |
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Reacting condition |
1 μM |
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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]: | |
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Animal models |
Mice bearing hormone-sensitive (HS) and hormone-insensitive (HI) strains of the MXT murine mammary carcinoma |
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Dosage form |
0.25 mg/kg; i.p. |
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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. |
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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. |
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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. | |
| Cas No. | 71441-28-6 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | ≥ 17.4mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8696 mL | 14.348 mL | 28.6961 mL |
| 5 mM | 0.5739 mL | 2.8696 mL | 5.7392 mL |
| 10 mM | 0.287 mL | 1.4348 mL | 2.8696 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet