| Size | Price | Stock | Qty |
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| 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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| Other Sizes |
| Targets |
Wnt signaling pathway - activator (EC50 = 28-29 nM).
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| ln Vitro |
In vitro studies demonstrate that SM04554 is a novel Wnt pathway activator with an EC50 of 28-29 nM. The Wnt signaling pathway plays a critical role in hair follicle development, cycling, and regeneration. By activating Wnt signaling, SM04554 promotes the transition of hair follicles from the telogen (resting) phase to the anagen (growth) phase, stimulating hair growth. The compound's mechanism of action involves selective activation and deactivation of the WNT signaling pathway, which is distinct from minoxidil's mechanism.
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| ln Vivo |
In vivo studies have demonstrated that SM04554 is a topical Wnt pathway activator that shows promise for treating androgenetic alopecia. The compound has been evaluated in clinical trials for androgenetic alopecia, a common form of hair loss in men and women. By activating Wnt signaling in hair follicles, SM04554 promotes hair growth and may provide a new therapeutic option for androgenetic alopecia. The compound's topical application and favorable safety profile support its potential as a treatment for hair loss.
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| Enzyme Assay |
Wnt signaling pathway activation assays are performed using cell-based reporter assays. Cells expressing a Wnt-responsive luciferase reporter are treated with SM04554 at various concentrations, and luciferase activity is measured. EC50 values are calculated from dose-response curves. Selectivity over other signaling pathways is assessed using similar assay formats to confirm the compound's specificity for Wnt pathway activation. For mechanistic studies, Wnt target gene expression is assessed by qRT-PCR for genes such as AXIN2, LEF1, and MYC.
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| Cell Assay |
Cellular assays for SM04554 typically involve culturing hair follicle cells or dermal papilla cells and treating them with the compound at various concentrations. Wnt signaling activation is assessed by measuring Wnt target gene expression by qRT-PCR or by using reporter assays. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Hair follicle growth is assessed using organ culture models or by measuring the length and diameter of hair shafts. The compound's effects on hair follicle cycling are assessed by measuring markers of anagen (e.g., Ki-67) and telogen (e.g., caspase-3) by immunohistochemistry. Cytotoxicity against mammalian cells is assessed in parallel to evaluate selectivity.
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| Animal Protocol |
In vivo efficacy of SM04554 is evaluated in animal models of hair loss, such as the mouse model of androgenetic alopecia. Mice are treated with SM04554 via topical application, and hair growth is assessed by visual scoring, measuring hair length and density, or by histomorphometric analysis of hair follicles. The compound's ability to promote hair growth and transition hair follicles from telogen to anagen is assessed. Clinical trials have been conducted to evaluate the safety and efficacy of SM04554 in patients with androgenetic alopecia. Endpoints include hair count, hair width, and patient-reported outcomes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SM04554 have been characterized to support its use as a topical research tool and potential therapeutic agent. The compound has a molecular weight of 296.32 and the molecular formula C18H16O4. As a topical agent, SM04554 is applied directly to the scalp, and its absorption through the skin is limited. Key PK parameters including systemic absorption, half-life, and clearance are determined using LC-MS/MS analysis of plasma samples following topical application. The compound's ability to reach hair follicles in the dermis is important for its efficacy. The compound should be stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of SM04554 has been conducted in preclinical and clinical studies to support its development for androgenetic alopecia. Standard toxicology assessments include acute and repeated-dose toxicity studies in rodents and other species, skin irritation and sensitization tests, and evaluation of effects on liver and kidney function. The compound's topical application minimizes systemic exposure and reduces the risk of systemic side effects. In clinical trials, SM04554 has been evaluated for safety and tolerability in patients with androgenetic alopecia. The compound's favorable safety profile supports its potential as a treatment for hair loss.
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| References | |
| Additional Infomation |
SM04554 (Dalosirvat) is a novel Wnt pathway activator that shows promise for treating androgenetic alopecia (male pattern baldness). The compound has an EC50 of 28-29 nM for Wnt pathway activation. SM04554 is a topical Wnt pathway activator applied to the scalp similarly to minoxidil but working through selective activation and deactivation of the WNT signaling pathway. The compound has been evaluated in clinical trials for androgenetic alopecia. SM04554 is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves activation of Wnt signaling, which promotes hair follicle growth and cycling. This compound is valuable for validating Wnt signaling as a therapeutic target for hair loss and for investigating the role of Wnt pathway in hair follicle biology.
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| Molecular Formula |
C18H16O4
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|---|---|
| Molecular Weight |
296.32
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| Exact Mass |
296.104
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| CAS # |
1360540-81-3
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| PubChem CID |
56837361
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
500.1±50.0 °C at 760 mmHg
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| Flash Point |
223.1±30.2 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.586
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| LogP |
3.36
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
400
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AOCDRSSVFUCURK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16O4/c19-15(13-4-2-1-3-5-13)7-8-16(20)14-6-9-17-18(12-14)22-11-10-21-17/h1-6,9,12H,7-8,10-11H2
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| Chemical Name |
1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenylbutane-1,4-dione
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| Synonyms |
SM-04554 SM 04554 SM04554 Dalosirvat
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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) |
DMSO : ~83.33 mg/mL (~281.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 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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