Name: TTNPB (Arotinoid acid)
Brand: Selleck Chemicals
SKU: S4627
Rating: 5 (16 reviews)

Jump to

Quality Control

Batch: Purity: 99.67%

99.67

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Retinoid Receptor Inhibitors	Tamibarotene AM580 Fenretinide UVI 3003 SR 11237 AR7 BMS493 All trans-Retinal MSU-42011 Palovarotene

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
HEK293 cells	Function assay	Agonist activity at human RARalpha expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.18 nM
CV-1 cells	Function assay	Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells, EC50=0.002 Μm
HL60 cells	Cytotoxicity assay	In vitro cytotoxicity against HL60 cells, IC50=46 μM
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	348.48	Formula	C₂₄H₂₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	71441-28-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Arotinoid Acid, Ro 13-7410, AGN-191183			Smiles	CC(=CC1=CC=C(C=C1)C(=O)O)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C

Solubility

In vitro
Batch:

DMSO : 15 mg/mL (43.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (14.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	RARβ (cell-free assay) 4.5 nM RARα (cell-free assay) 5.1 nM RARγ (cell-free assay) 9.3 nM
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. This compound 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. It 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. This chemical causes a concentration-dependent decrease in ES-D3 cell differentiation.
Kinase Assay	Binding assays
Kinase Assay	Binding assays are performed as previously described (Allenby et al., 1993, 1994). Briefly, labelled and unlabelled 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 equilibrium is achieved. For competitive binding assays, varying concentrations of unlabelled 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 radiolabelled ligand ([³H]tRA sp. act. 49.3 Ci/mmol, [³H]this compound sp. act. 5.5 Ci/ mmol) are added to the nucleosol of the appropriate receptor subtype in the presence (non-specific binding) or absence (total binding) of a 100-fold molar excess of the corresponding unlabelled retinoid. Specific binding is defined as the total binding minus non-specific binding. Saturation kinetics are calculated as previously described (Scatchard, 1949; Grippo and Gudas, 1987; Levin et al., 1992).
In vivo	TTNPB (0.25 mg/kg) causes growth inhibition in both MXT-HS and MXT-HI models by inducing cell apoptosis.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9070355/ [2] https://pubmed.ncbi.nlm.nih.gov/10495774/ [3] https://pubmed.ncbi.nlm.nih.gov/16273314/ [4] https://pubmed.ncbi.nlm.nih.gov/21362465/ [5] https://pubmed.ncbi.nlm.nih.gov/9877028/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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):

TTNPB (Arotinoid acid) RAR Agonist

Chemical Structure

Molecular Weight: 348.48