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Adapalene Retinoid Receptor agonist

Name: Adapalene
Brand: Selleck Chemicals
SKU: S1276
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S1276

Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne.

Chemical Structure

Molecular Weight: 412.52

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.85%

99.85

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite Casein Kinase Serine/threonin kinase Lipoxygenase LPL Receptor Phospholipase (e.g. PLA) DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase Glucokinase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase
Related Products	TTNPB AM580 Tamibarotene UVI 3003 Fenretinide SR 11237 BMS493 Palovarotene CD1530 RXRα Antibody [M1G17] AR7 CD3254 RARγ1 Antibody [P15H2] 9-cis-Retinoic acid HX531 All trans-Retinal CD437(AHPN) MSU-42011 Retinoid X Receptorα/RXRA Antibody [C13M7] Ch55

Chemical Information, Storage & Stability

Molecular Weight	412.52	Formula	C₂₈H₂₈O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	106685-40-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CD-271			Smiles	COC1=C(C=C(C=C1)C2=CC3=C(C=C2)C=C(C=C3)C(=O)O)C45CC6CC(C4)CC(C6)C5

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (41.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.	0.850mg/ml (2.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 17 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 clarify; 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.210mg/ml (0.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 4.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

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	RARγ ^[1] RARβ ^[1] RXR ^[1]
In vitro	Adapalene binds to retinoic acid receptors found predominantly in the terminal differentiation zone of epidermis and is more active than tretinoin in modulating cellular differentiation. This compound shows greatest affinity for the subtype PARγ, found predominantly in the epidermis. It is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little activity against cyclo-oxygenase. ^[1] This chemical time- and dose-dependently suppresses DNA synthesis and induces apoptosis in Colon carcinoma cell lines CC-531, HT-29 and LOVO as well as human foreskin fibroblasts. It shows significantly more effective antiproliferative and proapoptotic effects than 9-cis-retinoic acid (CRA), showing remarkable effects even at 10 μM. This compound disrupts DeltaPsi(m) and induces caspase-3 activity in responsive tumor cells. ^[2]
In vivo	Adapalene produces a dose-related reduction in the number of epidermal comedones and an increase in comedo profile and epidermal thickness in the rhino mice. ^[1] This compound results in a decreased expression of TLR-2 and IL-10 in explants of normal skin and explants of acne. It can modulate the epidermal immune system by increasing the CD1d expression and by decreasing the IL-10 expression by keratinocytes, and these modulations can increase the interactions between dendritic cells and T lymphocytes and could strengthen the antimicrobial activity against Propionibacterium acnes. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9074847/ [2] https://pubmed.ncbi.nlm.nih.gov/14506747/ [3] https://pubmed.ncbi.nlm.nih.gov/17518990/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02620813	Completed	Acne Vulgaris	University of California Davis	October 2015	Early Phase 1
NCT02442817	Completed	Schizophrenia	University of Nevada Reno\|Augusta University	March 2 2015	Phase 4
NCT01485367	Unknown status	Senile Purpura	Multispecialty Aesthetic Clinical Research Organization\|Galderma R&D	December 2011	Phase 2

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