| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
L-759,633 targets the cannabinoid receptor 2 (CB2), a G protein-coupled receptor that is primarily expressed on immune cells and is involved in the regulation of inflammation and immune responses. It acts as a high-affinity agonist, with a Ki of 6.4 nM for CB2 and 1043 nM for CB1, demonstrating 163-fold selectivity for CB2 over CB1. Activation of CB2 by L-759,633 inhibits adenylyl cyclase, reducing cAMP production.
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| ln Vitro |
In CB2-transfected cells, L759633 (0.1-1000 nM) suppresses the generation of cyclic AMP induced by forskolin with an EC50 of 8.1 nM [1]. At 10 μM, L759633 reduces the generation of cyclic AMP induced by forskolin by 48% [1].
In vitro, L-759,633 potently inhibits forskolin-stimulated cAMP production via CB2 receptors expressed in CHO cells, with an EC50 of 8.1 nM. The compound shows great potency against cAMP production in CB2-transfected cells compared to CB1-transfected cells. L-759,633's high affinity and selectivity for CB2 make it a valuable tool for studying CB2 receptor function in immune cells and inflammation. |
| ln Vivo |
In vivo, L-759,633 has been studied for its potential in inflammatory and pain models. By activating CB2 receptors on immune cells, the compound may modulate inflammatory responses and reduce pain. However, specific in vivo efficacy data are limited in the available literature. L-759,633 is primarily used as a research tool for studying CB2 receptor pharmacology.
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| Enzyme Assay |
The non-cellular assay for L-759,633 involves measuring its binding affinity for CB2 and CB1 receptors using radioligand binding assays. Membrane preparations from cells expressing CB2 or CB1 receptors are incubated with a radiolabeled cannabinoid receptor ligand (such as [³H]-CP-55,940) and varying concentrations of L-759,633. The inhibition of radioligand binding is measured, and the Ki is determined from competition curves.
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| Cell Assay |
The cellular assay for L-759,633 involves treating cells expressing CB2 receptors (e.g., CHO cells) with the compound and measuring its effects on cAMP production. Cells are pre-incubated with forskolin to stimulate adenylyl cyclase, and L-759,633 is added at various concentrations. The inhibition of cAMP accumulation is measured using a competitive immunoassay. The EC50 is determined from concentration-response curves.
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| Animal Protocol |
In the in vivo efficacy study, L-759,633 is administered to rodent models of inflammation or pain. The compound is typically administered by intraperitoneal injection or oral gavage. Inflammatory markers, pain thresholds, and other relevant endpoints are measured to assess the compound's effects. However, specific published protocols for L-759,633 are limited.
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| ADME/Pharmacokinetics |
L-759,633 has a molecular weight of 384.59 and a molecular formula of C₂₆H₄₀O₂. The compound has a purity of ≥98% (HPLC). It should be stored at +4°C. L-759,633 should be handled with appropriate laboratory safety precautions. The compound is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
The toxicological profile of L-759,633 has not been extensively characterized in the published literature. As a CB2 agonist, it may have effects on immune function and inflammation. Comprehensive toxicology data are limited, and L-759,633 is not approved for clinical use. The compound should be handled with appropriate laboratory safety precautions.
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| References |
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| Additional Infomation |
6h-dibenzo[b,d]pyran, 3-(1,1-dimethylheptyl)-6a,7,10,10a-tetrahydro-1-methoxy-6,6,9-trimethyl-,(6ar,10ar)- is a 1-benzopyran.
L-759,633 is a high-affinity, selective CB2 receptor agonist that has been used as a research tool to study CB2 receptor function. Its 163-fold selectivity for CB2 over CB1 makes it a valuable tool for dissecting CB2-specific effects in immune cells and inflammation. L-759,633 is a synthetic classical cannabinoid belonging to the 1-methoxy-Δ8-THC derivative class. The compound is not approved for clinical use and is strictly a research tool. |
| Molecular Formula |
C26H40O2
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|---|---|
| Molecular Weight |
384.6
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| Exact Mass |
384.302
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| CAS # |
174627-50-0
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| PubChem CID |
5311215
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
447.9±45.0 °C at 760 mmHg
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| Flash Point |
134.2±28.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.500
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| LogP |
9.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
547
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCCCCCC(C)(C)C1=CC(=C2[C@@H]3CC(=CC[C@H]3C(C)(C)OC2=C1)C)OC
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| InChi Key |
SUFMHSFGODDLKI-NHCUHLMSSA-N
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| InChi Code |
InChI=1S/C26H40O2/c1-8-9-10-11-14-25(3,4)19-16-22(27-7)24-20-15-18(2)12-13-21(20)26(5,6)28-23(24)17-19/h12,16-17,20-21H,8-11,13-15H2,1-7H3/t20-,21-/m1/s1
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| Chemical Name |
(6aR,10aR)-1-methoxy-6,6,9-trimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydrobenzo[c]chromene
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| Synonyms |
L759633; L 759,633; L-759,633
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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 | 2.6001 mL | 13.0005 mL | 26.0010 mL | |
| 5 mM | 0.5200 mL | 2.6001 mL | 5.2002 mL | |
| 10 mM | 0.2600 mL | 1.3001 mL | 2.6001 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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