[CAS NO. 201410-53-9] Talarozole

Name: Talarozole
Brand: Arctom Scientific
SKU: AS208592

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PRODUCTS SPECIFICATIONS [201410-53-9]

Fulfillment

Catalog

AS208592

Brand

Arctom Scientific

CAS

201410-53-9

DESCRIPTION [201410-53-9]

Overview

MDL	MFCD17166995
Molecular Weight	377.51
Molecular Formula	C21H23N5S
SMILES	CCC(CC)C(C1=CC=C(NC2=NC3=CC=CC=C3S2)C=C1)N4N=CN=C4

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

14 Publications Citing Use of MCE

Summary

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 IC ₅₀ s of 5.4 and 0.46 nM, respectively.

IC50 & Target

CYP26

In Vitro

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

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

In Vivo

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, at RA 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 at RA concentrations. In agreement, at RA concentrations are elevated in serum and liver at all timepoints measured. This increase in at RA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice ^[3] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00719121	Stiefel, a GSK Company\|GlaxoSmithKline	Cutaneous Inflammation	November 2006	Phase 1
NCT00725348	Stiefel, a GSK Company\|GlaxoSmithKline	Psoriasis	April 2004	Phase 2
NCT00716144	Stiefel, a GSK Company\|GlaxoSmithKline	Psoriasis	June 1, 2006	Phase 2
NCT00725439	Stiefel, a GSK Company\|GlaxoSmithKline	Acne	September 2004	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL ( 88.29 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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.

In Vivo:

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
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.

References

Synonyms

2-Benzothiazolamine, N-[4-[2-ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-

N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine

R 115866

Talarozole

Rambazole