| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Smoothened receptor (Smo), a cell surface receptor and key mediator of the Hedgehog (Hh) signaling pathway. GSA-10 is a Smo receptor agonist.
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| ln Vitro |
GSA-10 activates the smoothened receptor (Smo) with an EC50 of 1.2 μM in an alkaline phosphatase-based mouse mesenchymal cell line (C3H10T1/2) differentiation assay. It acts on Smo to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts. GSA-10 does not recognize the classic cyclopamine binding site. The compound mediates Hedgehog (Hh) signaling. The effect on cell differentiation is inhibited by Smo antagonists (MRT-83, SANT-1, LDE225, M25) in the nanomolar range. GSA-10 is strongly potentiated by forskolin and cholera toxin.
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| ln Vivo |
In vivo, GSA-10 mediates Hedgehog signaling, which may have research implications for regenerative medicine. It promotes osteoblast differentiation and bone formation. The compound has been investigated for its potential in regenerative medicine applications, particularly in bone regeneration. Specific animal model data and dosing regimens are available in the primary literature but not extensively detailed in public search results.
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| Enzyme Assay |
GSA-10 Smo receptor activation is assessed using in vitro cell-based assays measuring Hedgehog signaling pathway activity. C3H10T1/2 mouse mesenchymal cells are treated with GSA-10 at various concentrations (typically 0.01-100 μM) for appropriate time periods (e.g., 5-7 days for differentiation assays). Alkaline phosphatase activity is measured as a marker of osteoblast differentiation. GLI-dependent luciferase reporter activity is measured in cells transfected with a GLI-responsive luciferase construct. EC50 values are calculated from dose-response curves using nonlinear regression analysis. The effect of GSA-10 on Smo-mediated signaling is confirmed by inhibition with Smo antagonists such as MRT-83, SANT-1, LDE225, and M25.
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| Cell Assay |
Cellular activity is evaluated in C3H10T1/2 mouse mesenchymal cells or other cells responsive to Hedgehog signaling. Cells are treated with GSA-10 at various concentrations (typically 0.01-100 μM) for appropriate time periods (e.g., 5-7 days for differentiation). Osteoblast differentiation is assessed by alkaline phosphatase activity assay, Alizarin Red S staining for mineralization, and expression of osteoblast marker genes (Runx2, Osterix, Osteocalcin) by qRT-PCR. Hedgehog target gene expression (Gli1, Ptch1) is measured by qRT-PCR. The effect of GSA-10 is confirmed by inhibition with Smo antagonists (MRT-83, SANT-1, LDE225, M25) in the nanomolar range. Potentiation by forskolin and cholera toxin is assessed in parallel assays.
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| Animal Protocol |
In vivo efficacy is studied in animal models of bone regeneration, fracture healing, or other Hedgehog-related conditions. GSA-10 is administered via various routes (oral, intraperitoneal, subcutaneous, local injection) at doses determined from preliminary pharmacokinetic and tolerability studies. Osteoblast differentiation and bone formation are assessed by micro-CT, histology (H&E, Masson's trichrome staining), and immunohistochemistry for osteoblast markers. Hedgehog signaling activity is measured in target tissues by assessing Gli1 and Ptch1 expression. Specific protocols are detailed in the primary literature.
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| ADME/Pharmacokinetics |
GSA-10 has a molecular formula of C26H30N2O5 and a molecular weight of 450.53 g/mol. CAS Number: 300833-95-8. It is a quinoline carboxamide analogue. The compound is a Smo receptor agonist. Solubility in DMSO: 1.67 mg/mL (3.71 mM). Storage: store at -20°C for long-term stability, protected from light and moisture. Detailed pharmacokinetic parameters including half-life, oral bioavailability, volume of distribution, and plasma protein binding are not extensively characterized in publicly available literature.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSA-10 are not extensively published. As a Hedgehog pathway activator, it may have effects on development, tissue homeostasis, and cancer. The compound should be handled with appropriate safety precautions in a biological safety cabinet. Standard laboratory safety practices should be followed, including the use of personal protective equipment (gloves, lab coat, safety goggles) and adequate ventilation. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Avoid inhalation, ingestion, and skin contact. Consult the material safety data sheet (MSDS) for detailed safety information.
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| References |
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| Additional Infomation |
GSA-10 is a research tool compound for studying Smoothened receptor biology and Hedgehog signaling. It is not approved for clinical use. The compound has been investigated for regenerative medicine applications, particularly in bone regeneration. GSA-10 does not recognize the classic cyclopamine binding site, indicating it binds in a distinct pocket. Reference: Gorojankina et al., Discovery, molecular and pharmacological characterization of GSA-10, a novel small-molecule positive modulator of Smoothened. GSA-10 is strongly potentiated by forskolin and cholera toxin. The compound's ability to promote osteoblast differentiation makes it a valuable tool for understanding the role of Hedgehog signaling in bone formation and for identifying potential therapeutic strategies for bone repair and regeneration.
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| Molecular Formula |
C26H30N2O4
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| Molecular Weight |
434.54
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| Exact Mass |
450.215
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| CAS # |
300833-95-8
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| PubChem CID |
54683103
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| Appearance |
White to light yellow solid powder
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| Density |
1.240±0.06 g/cm3
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| Boiling Point |
620.2±55.0 °C at 760 mmHg
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| Flash Point |
328.9±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.610
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| LogP |
5.79
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
33
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| Complexity |
726
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MDLUYYGRCGDKGL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H30N2O5/c1-3-5-6-9-16-28-21-11-8-7-10-20(21)23(29)22(25(28)31)24(30)27-19-14-12-18(13-15-19)26(32)33-17-4-2/h7-8,10-15,29H,3-6,9,16-17H2,1-2H3,(H,27,30)
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| Chemical Name |
propyl 4-[(1-hexyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]benzoate
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| Synonyms |
GSA10; GSA 10; GSA-10
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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 : ~1.67 mg/mL (~3.71 mM)
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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 | 2.3013 mL | 11.5064 mL | 23.0128 mL | |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6026 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3013 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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