TTNPB

別名：Arotinoid Acid, Ro 13-7410, AGN-191183

製品コード：S4627 純度：99.67%

TTNPB is a potent RAR agonist, and inhibits binding of [³H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively.

CAS No. 71441-28-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 70500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（11）

製品安全説明書

現在のバッチを見る：純度： 99.67%

99.67

TTNPB関連製品

関連ターゲット	RAR RXR	もっと見る
関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

Retinoid Receptor阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報	PMID
HEK293 cells	Function assay	Agonist activity at human RARalpha expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.18 nM	25305688
CV-1 cells	Function assay	Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells, EC50=0.002 Μm	8308867
HL60 cells	Cytotoxicity assay	In vitro cytotoxicity against HL60 cells, IC50=46 μM	11128648
HeLa cells	Function assay	Agonist activity at human RARalpha expressed in human HeLa cells assessed as relative luminescence units at >=10 uM by luciferase assay relative to control	18951029
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生物活性

製品説明

TTNPB is a potent RAR agonist, and inhibits binding of [³H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively.

Targets

RARβ ^[1] (cell-free assay)	RARα ^[1] (cell-free assay)	RARγ ^[1] (cell-free assay)
4.5 nM	5.1 nM	9.3 nM

In Vitro
In vitro	TTNPB binds to nuclear retinoic acid receptors with high affinity, inhibits binding of [³H]tRA with IC50 of 3.8 nM, 4.0 nM, and 4.5 nM for mRARα, β, and γ, respectively. ^[1] TTNPB increases transcriptional activation of Mouse RARs in JEG-3 cells after 72 h using conditioned media with EC50 of 2.0 nM, 1.1 nM and 0.8 nM for mRARα, β, and γ, respectively. ^[2] TTNPB inhibits the growth of normal human mammary epithelial cells (HMECs) and estrogen receptor-positive (ER-positive) breast cancer cells by inducing G1 cell cycle blockade. ^[3] TTNPB causes a concentration-dependent decrease in ES-D3 cell differentiation. ^[4]
Kinase Assay	Binding assays
Kinase Assay	Binding assays are performed as previously described (Allenby et al., 1993, 1994). Briefly, labeled and unlabeled retinoids are added to nucleosol or cytosolic fractions in ethanol so that the total amount of ethanol added is constant in all tubes and did not exceed 2% of the incubation volume. The receptor preparations are incubated with retinoids at 4°C for 4–6 hr. Sephadex PD-10 desalting columns are used to separate bound radioligand from free radioligand after equilib- rium is achieved. For competitive binding assays, varying concentrations of unlabeled competing ligand are incubated with the appropriate nucleosol or cytosol in the presence of a fixed concentration of [³H]tRA (sp. act. 49.3 Ci/mmol) or [³H]9-cis RA (sp. act. 24.0 Ci/mmol). Final concentrations of [³H] tRA and [³H]9-cis RA for nuclear receptor binding assays are 5nM. Final concentrations of [³H] tRA for CRABP binding assays is 30 nM. The IC50s are calculated as described above (DeLean et al., 1978). For saturation kinetics, increasing concentrations of radiolabeled ligand ([³H]tRA sp. act. 49.3 Ci/mmol, [³H]TTNPB sp. act. 5.5 Ci/ mmol) are added to the nucleosol of the appropriate receptor subtype in the presence (nonspecific binding) or absence (total binding) of a 100-fold molar excess of the corresponding unlabeled retinoid. Specific binding is defined as the total binding minus nonspecific binding. Saturation kinetics are calculated as previously described (Scatchard, 1949; Grippo and Gudas, 1987; Levin et al., 1992).
細胞実験	細胞株	T47D cells and 184 cells
	濃度	~1 μM
	反応時間	8-12 days
	実験の流れ	Human mammary epithelial cells are maintained in Mammary Epithelial Basal Medium (MEBM) supplemented with the Mammary Epithelial Growth Media (MEGM) bullet kit. 184 and 184B5 cells are maintained in MEBM sodium-bicarbonate free (MEBM-SBF) supplemented with the MEGM bullet kit, isoproterenol (10 μM), and transferrin (5 μg/ml). MCF10A cell lines are maintained in DME/F12 containing 5% heat inactivated horse serum, penicillin/streptomycin (100 μg/ml and 100 μg/ml), hydrocortisone (1.4μM), insulin (10 μg/ml), choleratoxin (100 ng/ml), and EGF (20 ng/ml). Breast cancer cell lines are maintained in Improved MEM Zinc Option containing 10% fetal bovine serum, 1% glutamine, and 1% penicillin/streptomycin. For growth assays, cells are treated with the different retinoids for the specified number of days with media and treatment changes every other day in T47D cells and every 2 days in 184 cells. Cell proliferation is measured according to the protocol for the CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. This colorimetric assay determines the number of viable cells in a sample. Each point represents samples done in quadruplicate.

In Vivo
In Vivo	TTNPB (0.25 mg/kg) causes growth inhibition in both MXT-HS and MXT-HI models by inducing cell apoptosis. ^[5]
動物実験	動物モデル	Mouse models bearing hormone-sensitive (HS) and hormone-insensitive (HI) strains of the MXT murine mammary carcinoma.
	投与量	~0.25 mg/kg
	投与経路	i.p.

参考
[1] Pignatello MA, et al. Toxicol Appl Pharmacol. 1997, 142(2), 319-327. [2] Pignatello MA, et al. Toxicol Appl Pharmacol. 1999, 159(2), 109-116. [3] Wu K, et al. Breast Cancer Res Treat. 2006, 96(2), 147-157. [4] Louisse J, et al. Toxicol Lett. 2011, 203(1), 1-8. [5] Darro F, et al. Breast Cancer Res Treat. 1998, 51(1), 39-55. + 展開

参考

+ 展開

化学情報

分子量	348.48	化学式	C₂₄H₂₈O₂
CAS No.	71441-28-6	SDF	Download TTNPB SDFをダウンロードする
Smiles	CC(=CC1=CC=C(C=C1)C(=O)O)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 15 mg/mL ( (43.04 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):