| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
| Targets |
KX‑826 targets the androgen receptor (AR) as a potent antagonist. By topical application, it blocks AR activation in scalp hair follicles and sebaceous glands, thereby counteracting the effects of dihydrotestosterone (DHT) that cause follicle shrinkage and excessive sebum.
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|---|---|
| ln Vitro |
In vitro, KX‑826 binds to AR and inhibits its transcriptional activity, as confirmed by AR‑responsive reporter assays in prostate cancer cell lines. It shows antagonistic activity without agonist effects, making it suitable for topical use to suppress androgen signalling locally.
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| ln Vivo |
In vivo, topical application of KX‑826 (0.2% and 1%, 20 µL/mouse, twice daily for 4 weeks) promotes hair growth in mouse models. This effect supports its potential for treating androgenetic alopecia, with local action avoiding systemic anti‑androgenic side effects.
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| Enzyme Assay |
AR binding affinity is determined by radioligand displacement using [³H]methyltrienolone (R1881) and recombinant AR; non‑specific binding is defined with excess unlabelled ligand, and Ki is calculated from competition curves.
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| Cell Assay |
Cell‑based assays use AR‑expressing cells transfected with an AR‑responsive luciferase reporter; cells are treated with DHT (agonist) with or without KX‑826, and inhibition of luciferase activity is measured to quantify antagonism.
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| Animal Protocol |
In vivo mouse hair growth model: topical administration of KX‑826 at specified concentrations; hair growth is assessed by visual scoring and histology. Efficacy is compared with vehicle control to demonstrate local AR blockade.
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| ADME/Pharmacokinetics |
KX‑826 (MW 482.43, C₂₁H₁₅F₅N₄O₂S) is a topical drug; systemic absorption is expected to be low, which is a key safety feature. Detailed PK data (plasma levels, half‑life) are not fully disclosed, but minimal systemic exposure is a design goal.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available; however, topical administration minimises systemic side effects associated with AR antagonists (e.g., sexual dysfunction, hepatotoxicity). Local skin irritation and sensitisation are potential risks that would be evaluated in dermatological safety studies.
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| Additional Infomation |
KX‑826 is an investigational drug not yet approved; it is a first‑in‑class topical AR antagonist for hair loss and acne. Its unique local mechanism offers a new approach to androgen‑driven skin conditions, and clinical trials are ongoing to establish its efficacy and safety.
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| Molecular Formula |
C21H15F5N4O2S
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|---|---|
| Molecular Weight |
482.429
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| Exact Mass |
482.08
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| Elemental Analysis |
C, 52.28; H, 3.13; F, 19.69; N, 11.61; O, 6.63; S, 6.65
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| CAS # |
1272719-00-2
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| Related CAS # |
1272719-00-2
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| PubChem CID |
50940514
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| Appearance |
Solid powder
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| Density |
1.53±0.1 g/cm3(Predicted)
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
33
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| Complexity |
873
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=C(C(=C(C=C3)C#N)C(F)(F)F)F)C
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| InChi Key |
CGRMNGGGSWLDDC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H15F5N4O2S/c1-20(2)18(32)29(14-7-4-10(9-27)15(16(14)23)21(24,25)26)19(33)30(20)11-5-6-12(13(22)8-11)17(31)28-3/h4-8H,1-3H3,(H,28,31)
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| Chemical Name |
4-[3-[4-cyano-2-fluoro-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide
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| Synonyms |
Pyrilutamide; KX826; KX 826;KX-826
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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 | 2.0728 mL | 10.3642 mL | 20.7284 mL | |
| 5 mM | 0.4146 mL | 2.0728 mL | 4.1457 mL | |
| 10 mM | 0.2073 mL | 1.0364 mL | 2.0728 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/NCT06409650
Conditions:AlopeciaLink: https://clinicaltrials.gov/ct2/show/NCT05218642
Conditions:Alopecia|Male Pattern Hair LossProducts are for research use only; We do not sell to patients
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