| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
RAR-α[1]
YCT529 targets the Retinoic Acid Receptor alpha (RARalpha). It functions as a selective antagonist, potently inhibiting RARalpha with an IC50 of 1.2 nM. It shows greater than 300-fold selectivity over RARbeta and RARgamma, making it a highly specific tool for blocking RARalpha activity. |
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| ln Vitro |
In cell-free assays, YCT529 potently inhibits RARalpha with an IC50 of 1.2 nM. It demonstrates over 300-fold selectivity for RARalpha compared to RARbeta and RARgamma, indicating that its effects on spermatogenesis are primarily mediated through blocking this specific receptor subtype without interfering with other retinoid signaling pathways.
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| ln Vivo |
After four weeks of oral given to male mice, YCT529 was 99% successful in preventing conception and greatly reduced the number of sperm. There were no evident negative effects. After discontinuing to receive YCT529, mice can give birth to pups once again in 4-6 weeks [1].
YCT529 effectively reduces sperm counts in mice and non-human primates (NHPs) via oral administration. By blocking retinoic acid signaling necessary for spermatogenesis, it induces temporary infertility. This in vivo efficacy in two species supports its potential as a promising candidate for a reversible, non-hormonal male contraceptive. |
| Enzyme Assay |
Cell-free binding assays are performed using radioligand competition. Purified RARalpha, RARbeta, and RARgamma receptors are each incubated with a radiolabeled retinoic acid ligand and varying concentrations of YCT529. After incubation, the mixture is filtered to separate bound and free ligand, and the half-maximal inhibitory concentration (IC50) for each receptor is calculated.
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| Cell Assay |
Cellular assays for RAR antagonism are conducted in COS-1 cells transfected with an RARalpha expression plasmid and a luciferase reporter plasmid containing a retinoic acid response element (RARE). Cells are co-treated with a fixed concentration of an RARalpha agonist and varying doses of YCT529 to evaluate its ability to block agonist-induced transcription.
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| Animal Protocol |
In vivo efficacy is evaluated in adult male mice and non-human primates (NHPs). YCT529 is administered orally (gavage) daily for several weeks. The primary endpoint is sperm count in the epididymis or ejaculate, measured via microscopy. Other endpoints include testicular histology to assess the progression of spermatogenesis and the reversibility of the effect after stopping treatment.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties have been evaluated in preclinical species. YCT529 is orally active, achieving sufficient systemic exposure to reach the testes and effectively inhibit RARalpha. Its absorption, distribution, metabolism, and excretion (ADME) profile is favorable for a once-daily oral contraceptive candidate.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies have been conducted to support its development as a male contraceptive. YCT529 has been shown to be well-tolerated at effective doses in both mice and NHPs, with no significant adverse effects reported beyond the intended on-target pharmacological effect of reversible infertility.
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| References | |
| Additional Infomation |
YCT-529 is being investigated in the clinical trial NCT06542237 (an open-label, repeated-dose study designed to evaluate the efficacy of YCT-529 in healthy men).
YCT529 represents a first-in-class, non-hormonal male contraceptive that targets a specific nuclear receptor rather than hormones. Its selectivity for RARalpha over other RAR isoforms is key to its safety profile. Although it is a research compound, its discovery has been presented at major scientific meetings, highlighting a new paradigm for contraception that does not involve hormones. |
| Molecular Formula |
C29H25NNAO3
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|---|---|
| Molecular Weight |
458.50
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| Exact Mass |
457.165
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| CAS # |
2863670-67-9
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| Related CAS # |
YCT529 free acid;2863670-66-8
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| PubChem CID |
166055298
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| Appearance |
Light yellow to green yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
736
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(OC2=CC=C(C3=CC=C(C4C=CC(=CC=4)C(=O)O)N3)C=C2C(C2C=CC(=CC=2)C)=C1)C.[Na]
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| InChi Key |
NNFWFHLHNJSJTH-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C29H25NO3.Na/c1-18-4-6-19(7-5-18)24-17-29(2,3)33-27-15-12-22(16-23(24)27)26-14-13-25(30-26)20-8-10-21(11-9-20)28(31)32;/h4-17,30H,1-3H3,(H,31,32);/q;+1/p-1
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| Chemical Name |
sodium;4-[5-[2,2-dimethyl-4-(4-methylphenyl)chromen-6-yl]-1H-pyrrol-2-yl]benzoate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 2.1810 mL | 10.9051 mL | 21.8103 mL | |
| 5 mM | 0.4362 mL | 2.1810 mL | 4.3621 mL | |
| 10 mM | 0.2181 mL | 1.0905 mL | 2.1810 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06542237
Conditions:Male ContraceptionLink: https://clinicaltrials.gov/ct2/show/NCT06094283
Conditions:Male ContraceptionProducts are for research use only; We do not sell to patients
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