| Size | Price | |
|---|---|---|
| 5mg | ||
| 100mg | ||
| Other Sizes |
| Targets |
The primary molecular target of SA47 is fatty acid amide hydrolase (FAAH). It acts as a covalent irreversible inhibitor, binding to the enzyme's active site. SA47 shows greater selectivity for FAAH than URB 597 against multiple carboxylesterases, ensuring more specific target engagement in endocannabinoid studies.
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|---|---|
| ln Vitro |
SA47 is a selective and potent FAAH inhibitor. It exhibits greater selectivity for FAAH than URB 597 against multiple carboxylesterases. Its single-band ABPP profile at 10 uM demonstrates high target specificity. The compound effectively inhibits FAAH-mediated anandamide degradation in vitro.
|
| ln Vivo |
SA47 elevates anandamide levels in vivo by inhibiting FAAH, leading to enhanced endocannabinoid signaling. It demonstrates analgesic, anxiolytic, and anti-inflammatory effects in animal models. No detailed pharmacokinetic data have been published in accessible literature.
|
| Enzyme Assay |
FAAH activity is measured using radiolabeled anandamide ([3H]anandamide) as substrate incubated with membrane preparations. Serial dilutions of SA47 are added, and the release of [3H]ethanolamine is measured by scintillation counting. IC50 values are determined from dose-response curves.
|
| Cell Assay |
For cell-based assays, cells expressing FAAH are treated with SA47, and anandamide hydrolysis is measured in cell lysates using radiolabeled substrate. Activity-based protein profiling (ABPP) is performed using a fluorescent or biotinylated FAAH probe to confirm target engagement.
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| Animal Protocol |
Mice or rats receive SA47 intraperitoneally or orally at various doses. Anandamide levels in brain tissue are measured by LC-MS. Analgesic activity is assessed using the formalin test or tail-flick test. Anxiolytic activity is evaluated using the elevated plus-maze.
|
| References |
| Molecular Formula |
C17H26N4O3
|
|---|---|
| Molecular Weight |
334.42
|
| Exact Mass |
334.2
|
| CAS # |
792236-07-8
|
| PubChem CID |
9840648
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.578
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
24
|
| Complexity |
411
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=NC(=CC=C1)N2CCC(CC2)CCNC(=O)OCC(=O)NC
|
| InChi Key |
HSYCMGWPPRTNKH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H26N4O3/c1-13-4-3-5-15(20-13)21-10-7-14(8-11-21)6-9-19-17(23)24-12-16(22)18-2/h3-5,14H,6-12H2,1-2H3,(H,18,22)(H,19,23)
|
| Chemical Name |
[2-(methylamino)-2-oxoethyl] N-[2-[1-(6-methylpyridin-2-yl)piperidin-4-yl]ethyl]carbamate
|
| Synonyms |
SA47; SA 47; SA-47
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.9903 mL | 14.9513 mL | 29.9025 mL | |
| 5 mM | 0.5981 mL | 2.9903 mL | 5.9805 mL | |
| 10 mM | 0.2990 mL | 1.4951 mL | 2.9903 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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