1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. TR antagonist 1

TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.

For research use only. We do not sell to patients.

TR antagonist 1 Chemical Structure

TR antagonist 1 Chemical Structure

CAS No. : 500794-88-7

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5 mg USD 550 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.

IC50 & Target

IC50: 36 nM (Thyroid hormone α), 22 nM (Thyroid hormone α)[1]

Cellular Effect
Cell Line Type Value Description References
CHO IC50
32 nM
Compound: 6
Activity at human TR-alpha-1 transfected in CHO K1 cells by alkaline phosphatase reporter gene assay
Activity at human TR-alpha-1 transfected in CHO K1 cells by alkaline phosphatase reporter gene assay
[PMID: 17154490]
CHO IC50
32 nM
Compound: 6
Activity at human TR-beta-1 transfected in CHO K1 cells by alkaline phosphatase reporter gene assay
Activity at human TR-beta-1 transfected in CHO K1 cells by alkaline phosphatase reporter gene assay
[PMID: 17154490]
In Vitro

TR antagonist 1 displays high affinity for both thyroid hormone TRα and TRβ (IC50=36 and 22 nM, respectively). TR antagonist 1 acts as a full antagonist in the TRAFR cell assay and the IC50 32 nM for both TRAFα1 and TRAFβ1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TR antagonist 1 treatment lowers heart rate and shows a possible trend toward an increase of low-density lipoprotein cholesterol (LDL-C) in the cholesterol fed rat model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

561.26

Formula

C25H23Br2NO4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)CCC1=CC(Br)=C(OC2=CC(/C=C/C3=CC=NC=C3)=C(O)C(C(C)C)=C2)C(Br)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (148.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7817 mL 8.9085 mL 17.8171 mL
5 mM 0.3563 mL 1.7817 mL 3.5634 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7817 mL 8.9085 mL 17.8171 mL 44.5426 mL
5 mM 0.3563 mL 1.7817 mL 3.5634 mL 8.9085 mL
10 mM 0.1782 mL 0.8909 mL 1.7817 mL 4.4543 mL
15 mM 0.1188 mL 0.5939 mL 1.1878 mL 2.9695 mL
20 mM 0.0891 mL 0.4454 mL 0.8909 mL 2.2271 mL
25 mM 0.0713 mL 0.3563 mL 0.7127 mL 1.7817 mL
30 mM 0.0594 mL 0.2970 mL 0.5939 mL 1.4848 mL
40 mM 0.0445 mL 0.2227 mL 0.4454 mL 1.1136 mL
50 mM 0.0356 mL 0.1782 mL 0.3563 mL 0.8909 mL
60 mM 0.0297 mL 0.1485 mL 0.2970 mL 0.7424 mL
80 mM 0.0223 mL 0.1114 mL 0.2227 mL 0.5568 mL
100 mM 0.0178 mL 0.0891 mL 0.1782 mL 0.4454 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TR antagonist 1
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HY-111443
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