[CAS NO. 895542-09-3] Trifarotene

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PRODUCTS SPECIFICATIONS [895542-09-3]

Catalog

HY-100256

Brand

MCE

CAS

895542-09-3

DESCRIPTION [895542-09-3]

Overview

MDL	MFCD30481310
Molecular Weight	459.58
Molecular Formula	C29H33NO4
SMILES	O=C(C1=CC=C(C2=CC=C(OCCO)C(C3=CC=C(N4CCCC4)C(C(C)(C)C)=C3)=C2)C=C1)O

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

Summary

Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ ( EC ₅₀ =7.7 nM) over RARα ( EC ₅₀ =500 nM) and RARβ ( EC ₅₀ =125 nM), respectively ^[1] .

In Vitro

Trifarotene (CD5789) (3.3 µL 0.33 cm ² ; 24 hours) involves in keratinization, desquamation, cornification and cell adhesion in reconstructed human epidermis (RHE). The mean EC ₅₀ on the combined target genes is 0.0048% for Trifarotene ^[2] .

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

In Vivo

Trifarotene (0.001%-0.01% in a cream at 25 mg/mouse) shows dose-dependent comedolytic activity, being fully efficacious at 0.01% (98% reduction) ^[2] .

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

Animal Model:	Rhino mice ^[2]
Dosage:	0.001%, 0.0025%, 0.005% and 0.01% in a cream at 25 mg/mouse (5 cm ² surface on the back skin on a 5 mg/cm ² basis)
Administration:	Topical application; once a day; 11 days
Result:	Increased the epidermis thickness by 275% (66 μm) and the transepidermal water loss (TEWL) by 285% (26 g/h/m ² ).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02556788	Galderma R&D	Acne Vulgaris	November 2015	Phase 3
NCT04856904	Galderma R&D	Acne Vulgaris	May 28, 2021	Phase 4
NCT05089708	Galderma R&D	Acne Vulgaris	December 27, 2021	Phase 4
NCT04451330	Galderma R&D	Acne Vulgaris	July 29, 2020	Phase 4
NCT01616654	Galderma R&D	Acne Vulgaris	June 20, 2012	Phase 2
NCT05550337	Teva Pharmaceuticals USA\|Teva Pharmaceuticals, Inc.	Acne Vulgaris	September 19, 2022	Phase 3
NCT01804335	M.D. Anderson Cancer Center\|Galderma R&D	Lymphoma	February 2013	Phase 1
NCT03738800	Mayne Pharma International Pty Ltd	Lamellar Ichthyosis	May 1, 2019	Phase 2
NCT02566369	Galderma R&D	Acne Vulgaris	November 30, 2015	Phase 3
NCT03915860	Galderma R&D	Acne Vulgaris	March 27, 2019	Phase 3
NCT02189629	Galderma R&D	Acne Vulgaris	February 23, 2015	Phase 3

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 : 250 mg/mL ( 543.97 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1759 mL	10.8795 mL	21.7590 mL
5 mM	0.4352 mL	2.1759 mL	4.3518 mL
10 mM	0.2176 mL	1.0879 mL	2.1759 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: ≥ 2.08 mg/mL (4.53 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

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

References

Synonyms

[1,1′:3′,1′′-Terphenyl]-4-carboxylic acid, 3′′-(1,1-dimethylethyl)-4′-(2-hydroxyethoxy)-4′′-(1-pyrrolidinyl)-

3′′-(1,1-Dimethylethyl)-4′-(2-hydroxyethoxy)-4′′-(1-pyrrolidinyl)[1,1′:3′,1′′-terphenyl]-4-carboxylic acid

3′′-tert-Butyl-4′-(2-hydroxyethoxy)-4′′-(pyrrolidin-1-yl)[1,1′:3′,1′′]terphenyl-4-carboxylic acid

Trifarotene

CD 5789

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