製品番号: HY-14531

Talarozole

Name: Talarozole
Brand: MedChemExpress
SKU: HY-14531
Price: 120.00 USD
Availability: InStock
Rating: 5 (22 reviews)

(別名: R115866)

22 Cited Publications

カスタマーレビュー

Based on 22 publication(s) in Google Scholar

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC₅₀s of 5.4 and 0.46 nM, respectively.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度 : 99.75%
CAS 番号: 201410-53-9
分子式: C₂₁H₂₃N₅S
分子量:377.51

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Talarozole 構造式

CAS 番号: 201410-53-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (22)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

CYP26

RAR/RXR アイソフォーム固有の製品をすべて表示 :

Cytochrome P450 アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.0051 μM Compound: 3; R115866	Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
Sf9	IC₅₀	0.00046 μM Compound: 3; R115866	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
Sf9	IC₅₀	0.46 nM Compound: 3; R115866	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]

体外実験

When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased^[2].

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

体内実験

A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) C_max of 80 nM and a K_i of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice^[3].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 201410-53-9
性状 Solid
分子量 377.51
分子式 C₂₁H₂₃N₅S
Color White to off-white
SMILES

CCC(CC)C(C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4
別名

R115866
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (22)

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Cell Stem Cell

Multi-omic analysis reveals retinoic acid molecular drivers for dermal fibrosis and regenerative repair in the skin. [Abstract]

2025 Sep 4;32(9):1421-1437.e6. PMID: 40816279
Dev Cell

Pituicyte Cues Regulate the Development of Permeable Neuro-Vascular Interfaces. [Abstract]

2018 Dec 17;47(6):711-726.e5. PMID: 30449506
Clin Transl Med

Metformin reduces hepatocarcinogenesis by inducing downregulation of Cyp26a1 and CD8+ T cells. [Abstract]

2023 Nov;13(11):e1465. PMID: 37997519
Neurosci Bull

Cytochrome P450 26A1 Contributes to the Maintenance of Neuropathic Pain. [Abstract]

2024 Mar;40(3):293-309. PMID: 37639183
J Enzyme Inhib Med Chem

Comparison of the ligand binding site of CYP2C8 with CYP26A1 and CYP26B1: a structural basis for the identification of new inhibitors of the retinoic acid hydroxylases. [Abstract]

2016;31(sup2):148-161. PMID: 27424662
Toxicology

Exosomes-mediated retinoic acid disruption: A link between gut microbiota depletion and impaired spermatogenesis. [Abstract]

2024 Nov:508:153907. PMID: 39121937
Tissue Eng Regen Med

Wnt/β-Catenin Promotes the Osteoblastic Potential of BMP9 Through Down-Regulating Cyp26b1 in Mesenchymal Stem Cells. [Abstract]

2023 Aug;20(5):705-723. PMID: 37010733
J Biol Chem

A cell-based assay for retinaldehyde dehydrogenase activity: Retinoid quantification as an alternative to current fluorescence-based approaches. [Abstract]

2026 Jan 29;302(3):111211. PMID: 41617028
Development

Differential RA responsiveness directs formation of functionally distinct spermatogonial populations at the initiation of spermatogenesis in the mouse. [Abstract]

2019 May 13;146(12):dev173088. PMID: 31023878
J Cell Physiol

WNT4 acts downstream of BMP2 to mediate the regulation of ATRA signaling on RUNX1 expression: Implications for terminal differentiation of antler chondrocytes. [Abstract]

2018 Feb;233(2):1129-1145. PMID: 28436029
PLoS Genet

In vivo zebrafish morphogenesis shows Cyp26b1 promotes tendon condensation and musculoskeletal patterning in the embryonic jaw. [Abstract]

2017 Dec 11;13(12):e1007112. PMID: 29227993

Talarozole purchased from MedChemExpress. Usage Cited in: PLoS Genet. 2017 Dec 11;13(12):e1007112. [Abstract]

Embryos raised in media containing 0.01% DMSO develop normally. 100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n=64).
Toxicol Appl Pharmacol

In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]

2024 May:486:116945. PMID: 38688424
Biol Reprod

Differential responsiveness of spermatogonia to retinoic acid dictates precocious differentiation but not meiotic entry during steady-state spermatogenesis. [Abstract]

2023 May 10;108(5):822-836. PMID: 36708226
J Cell Biochem

A novel lncRNA LOLA1 may predict malignant progression and promote migration, invasion, and EMT of oral leukoplakia via the AKT/GSK-3β pathway. [Abstract]

2021 Oct;122(10):1302-1312. PMID: 33969929
Mol Pharmacol

CYP26C1 Is a Hydroxylase of Multiple Active Retinoids and Interacts with Cellular Retinoic Acid Binding Proteins. [Abstract]

2018 May;93(5):489-503. PMID: 29476041
Mol Pharmacol

All-Trans-Retinoic Acid Enhances Mitochondrial Function in Models of Human Liver. [Abstract]

2016 May;89(5):560-74. PMID: 26921399

Talarozole purchased from MedChemExpress. Usage Cited in: Mol Pharmacol. 2016 May;89(5):560-74. [Abstract]

Induction of hepatic mitochondrial biogenesis genes in mice after Talarozole (TLZ) treatment compared with vehicle-treated mice. All mRNA data are presented as fold change in mRNA abundance relative to control mice. β-Actin is used as the housekeeping gene. For protein data, results are expressed as ratio of SDHA to β-actin.
Mol Pharmacol

Induction of CYP26A1 by metabolites of retinoic acid: evidence that CYP26A1 is an important enzyme in the elimination of active retinoids. [Abstract]

2015;87(3):430-41. PMID: 25492813
J Exp Zool B Mol Dev Evol

ATRA Signaling Regulates the Expression of COL9A1 through BMP2-WNT4-RUNX1 Pathway in Antler Chondrocytes. [Abstract]

2017 Sep;328(6):575-586. PMID: 28643469

Talarozole purchased from MedChemExpress. Usage Cited in: J Exp Zool B Mol Dev Evol. 2017 Sep;328(6):575-586. [Abstract]

Effect of R115866 on COL9A1 expression. R115866 enhances the effect of ATRA on COL9A1 expression. R115866 (1 μM) is dissolved in DMSO. Control receive the vehicle only.
University of Oxford

2023 Oct.
Mech Dev

The Cdx transcription factors and retinoic acid play parallel roles in antero-posterior position of the pectoral fin field during gastrulation. [Abstract]

2020 Dec:164:103644. PMID: 32911082
University of Texas

August 2017.

Talarozole purchased from MedChemExpress. Usage Cited in: University of Texas. August 2017.

100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n = 64).
Université Nice Sophia Antipolis

5 Oct 2016.

溶剤 & 溶解度

体外:

DMSO : 33.33 mg/mL (88.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6489 mL

13.2447 mL

26.4894 mL

5 mM

0.5298 mL

2.6489 mL

5.2979 mL

10 mM

0.2649 mL

1.3245 mL

2.6489 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (5.30 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (5.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[2]

Human liver microsomes (0.2 mg/mL) are incubated with 4-OH-atRA (500 nM) and NADPH, NADP⁺ or NAD⁺ (each at 2 mM) in 100 mM KPi buffer pH 7.4. In addition, 4-OH-atRA is incubated with human liver microsomes in the presence and absence of Talarozole (1 μM), a CYP26A1 specific inhibitor, and Ketoconazole (10 μM) a pan-P450 inhibitor and with NADPH as a cofactor. Following a 5 min pre-incubation, the reactions are initiated with the addition of cofactor and incubated for 30 minutes. At 30 min the reactions are quenched with equal volume of Acetonitrile and centrifuged at 3,000 g for 15 min. The supernatants are collected and 4-oxo-atRA formation is analyzed by LC-MS/MS. All incubations are normalized to a no cofactor control^[2].

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

Animal Administration^[3]

Mice^[3]
Talarozole is administered to mice as a single dose (2.5 mg/kg) or as multiple doses for three days. Serum Talarozole concentrations and serum, liver and testes atRA concentrations are measured by LC-MS/MS. Inhibition of CYP26 and changes inatRA concentrations in each tissue are predicted based on CYP26 activity in vitro and Talarozole disposition. Markers of fatty acid oxidation in the liver and spermatogonial differentiation in the testes are measured following Talarozole treatment.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
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OR (2659 KB)
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SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Diaz P, et al. Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, theHuman Liver Retinoic Acid Hydroxylase. J Med Chem. 2016 Mar 24;59(6):2579-95. [Content Brief]

[2]. Topletz AR, et al. Induction of CYP26A1 by metabolites of retinoic acid: evidence that CYP26A1 is an important enzyme in theelimination of active retinoids. Mol Pharmacol. 2015;87(3):430-41. [Content Brief]

[3]. Faith Stevison, et al. CYP26 Inhibition Increases Retinoic Acid Concentrations in Target Tissues and Alters Retinoid Signaling

[4]. Tripathy S, et al.All-Trans-Retinoic Acid Enhances Mitochondrial Function in Models of Human Liver. Mol Pharmacol. 2016 May;89(5):560-74. [Content Brief]

[5]. Bovenschen HJ, et al. Oral retinoic acid metabolism blocking agent Rambazole for plaque psoriasis: an immunohistochemical study. Br J Dermatol. 2007 Feb;156(2):263-70. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6489 mL	13.2447 mL	26.4894 mL	66.2234 mL
	5 mM	0.5298 mL	2.6489 mL	5.2979 mL	13.2447 mL
	10 mM	0.2649 mL	1.3245 mL	2.6489 mL	6.6223 mL
	15 mM	0.1766 mL	0.8830 mL	1.7660 mL	4.4149 mL
	20 mM	0.1324 mL	0.6622 mL	1.3245 mL	3.3112 mL
	25 mM	0.1060 mL	0.5298 mL	1.0596 mL	2.6489 mL
	30 mM	0.0883 mL	0.4415 mL	0.8830 mL	2.2074 mL
	40 mM	0.0662 mL	0.3311 mL	0.6622 mL	1.6556 mL
	50 mM	0.0530 mL	0.2649 mL	0.5298 mL	1.3245 mL
	60 mM	0.0441 mL	0.2207 mL	0.4415 mL	1.1037 mL
	80 mM	0.0331 mL	0.1656 mL	0.3311 mL	0.8278 mL

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Talarozole

22 Cited Publications

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Talarozole

MedChemExpress（MCE）の使用を引用している文献 Talarozole

RAR/RXR アイソフォーム固有の製品をすべて表示

Cytochrome P450 アイソフォーム固有の製品をすべて表示

生物活性