| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
HPR targets the retinoic acid receptors (RARs), specifically binding to RAR-alpha, RAR-beta, and RAR-gamma subtypes. It is a direct agonist of the RAR nuclear receptors. Unlike retinol (which must be converted to retinoic acid via two oxidation steps) and retinyl esters (which must be hydrolyzed to retinol and then oxidized), HPR directly binds to RARs without requiring metabolic activation in the skin. Upon binding, the ligand-activated receptor forms a heterodimer with the retinoid X receptor (RXR) and binds to retinoic acid response elements (RAREs) in the DNA. This regulates the transcription of genes involved in cell proliferation, differentiation, and sebum production. This results in the normalization of keratinocyte differentiation, reduction of sebum output, and stimulation of collagen synthesis, providing anti-aging and anti-acne effects.
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| ln Vitro |
In vitro, HPR (0.1-10 uM) acts as a full agonist of RARalpha, RARbeta, and RARgamma in luciferase reporter gene assays. It is more potent than retinol and retinyl esters, with an EC₅0 in the low nanomolar to micromolar range. In primary human keratinocytes, HPR (1-10 uM) reduces the expression of genes involved in inflammation and increases the expression of genes involved in epidermal differentiation. It also inhibits the proliferation of sebocytes (human sebaceous gland cells) and reduces the production of sebum. Compared to all-trans retinoic acid, HPR has a significantly lower irritation potential in reconstituted human epidermis (RHE) models as measured by ET-50 (time to reduce tissue viability by 50% in the MTT assay). It also stimulates collagen type I and type III synthesis in human dermal fibroblasts. HPR does not undergo significant isomerization under UV light, making it photostable.
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| ln Vivo |
In vivo, HPR is used as an ingredient in topical cosmetic formulations at concentrations of 0.1-1%. Clinical studies have shown that the topical application of HPR (0.5%) for 8-12 weeks significantly reduces the signs of photoaging (fine lines, wrinkles, hyperpigmentation) and improves skin firmness. It also reduces acne lesions (comedones, papules) in subjects with mild to moderate facial acne. In a double-blind, vehicle-controlled study, HPR (0.5%) demonstrated comparable anti-aging efficacy to retinol (0.5%) with significantly less skin irritation (dryness, redness, peeling). It is not used as an oral drug. HPR is approved only for topical use in cosmetics, not for systemic administration.
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| Enzyme Assay |
Dose-response curves for RAR activation are generated using a cell-based luciferase reporter assay. Human embryonic kidney (HEK293T) cells are co-transfected with a plasmid expressing the RARalpha, RARbeta, or RARgamma receptor, and a reporter plasmid containing a luciferase gene under the control of a retinoic acid response element (RARE). After 24 h, the cells are treated with HPR (0.1 pM to 10 uM) for 24 h. The cells are then lysed, and luciferase activity is measured. The EC₅0 is calculated from the dose-response curve. The relative binding affinity for the RAR subtypes is determined by competitive binding assays using [3H]-all-trans retinoic acid as the radioligand.
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| Cell Assay |
For anti-aging activity, human dermal fibroblasts (HDFs) are seeded in 6-well plates and treated with HPR (0.1-10 uM) for 48-72 h. The culture supernatant is collected, and the concentration of type I procollagen (PIP) is measured using an ELISA kit. For anti-acne activity, human primary sebocytes are seeded in 24-well plates and treated with HPR (0.1-10 uM) for 7-14 days. The neutral lipid content is measured by Oil Red O staining, and the lipid is extracted with isopropanol, and the absorbance is measured at 520 nm. The reduction in lipid content (expressed as a percentage of control) is calculated. For irritation potential, the reconstructed human epidermis (RHE) model (e.g., EpiDerm) is used. RHE tissues are treated topically with HPR (0.1-1%) for 0.5-24 h. Tissue viability is measured by MTT assay. The ET-50 (the time required to reduce viability by 50%) is calculated.
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| Animal Protocol |
In vivo anti-aging efficacy is assessed using a randomized, double-blind, vehicle-controlled clinical trial. 40 healthy female volunteers (aged 40-65 years) with mild to moderate photoaging are enrolled. The test formulation (containing 0.5% HPR) and the vehicle control are randomly assigned to the left and right sides of the face. The products are applied once daily at night for 8-12 weeks. The study is conducted at a certified testing laboratory under Good Clinical Practice (GCP) standards. Skin parameters are assessed at baseline and at weeks 2, 4, 8, and 12. The primary endpoint is the improvement in wrinkle depth (measured by Visioscan or Primos) and skin roughness (Ra). Secondary endpoints include hydration (Corneometer), transepidermal water loss (TEWL), and skin elasticity (Cutometer). The incidence of adverse events (erythema, scaling, stinging) is recorded. The study is conducted on human volunteers; no animal studies are required.
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| ADME/Pharmacokinetics |
HPR (MW 398.58) is a lipophilic ester (LogP ~ 6). It is designed for topical application. Systemic absorption is negligible following topical application; in a pharmacokinetic study in humans, plasma concentrations of HPR were below the lower limit of quantitation (LLOQ) after 4 weeks of daily application of 0.5% HPR. The compound is not intended for systemic delivery. The compound is photostable and does not decompose under UV light, unlike all-trans retinoic acid. For research use, it is supplied as a solid powder. It is soluble in DMSO, ethanol, and oils. The compound is stored at -20degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
HPR is a cosmetic ingredient and is considered safe for topical use at concentrations up to 1%. Clinical studies have reported no serious adverse events. Mild skin irritation (transient erythema, peeling) occurs in a small percentage of users, but at a significantly lower rate than that observed with retinol or tretinoin. It is not a drug. It is non-genotoxic, non-mutagenic, and non-carcinogenic. As a cosmetic ingredient, it is not required to undergo the same toxicological testing as pharmaceuticals. There is no risk of teratogenicity when used topically, as systemic absorption is negligible. However, oral administration is contraindicated during pregnancy. HPR is not approved by the FDA as a drug; it is listed in the INCI (International Nomenclature of Cosmetic Ingredients) database.
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| References | |
| Additional Infomation |
Hydroxypinacolone retinoate (HPR; CAS# 893412-73-2) is a research-grade third-generation retinoid and direct RAR agonist. It is not an FDA-approved drug. It is used in anti-aging and anti-acne research as an alternative to retinol and tretinoin. It is an active cosmetic ingredient. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C26H38O3
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| Molecular Weight |
398.58
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| Exact Mass |
398.282
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| CAS # |
893412-73-2
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| PubChem CID |
25054592
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
0
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
762
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(CCC1)(C)C)/C=C/C(=C/C=C/C(=C/C(=O)OCC(=O)C(C)(C)C)/C)/C
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| InChi Key |
XLPLFRLIWKRQFT-XUJYDZMUSA-N
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| InChi Code |
InChI=1S/C26H38O3/c1-19(14-15-22-21(3)13-10-16-26(22,7)8)11-9-12-20(2)17-24(28)29-18-23(27)25(4,5)6/h9,11-12,14-15,17H,10,13,16,18H2,1-8H3/b12-9+,15-14+,19-11+,20-17+
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| Chemical Name |
(3,3-dimethyl-2-oxobutyl) (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoate
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| Synonyms |
HPR
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5089 mL | 12.5445 mL | 25.0891 mL | |
| 5 mM | 0.5018 mL | 2.5089 mL | 5.0178 mL | |
| 10 mM | 0.2509 mL | 1.2545 mL | 2.5089 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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