| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
GPR55 and CB2 receptors; PSB-SB-487 is a potent GPR55 antagonist and a CB2 receptor agonist. GPR55 is an orphan G protein-coupled receptor that has been implicated in various physiological and pathological processes, including pain, inflammation, and cancer. CB2 is a cannabinoid receptor primarily expressed in immune cells and is involved in modulating inflammation and immune responses. By antagonizing GPR55 and agonizing CB2, the compound may exert therapeutic effects in a range of diseases.
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| ln Vitro |
In vitro, PSB-SB-487 shows potent antagonism of GPR55 with an IC₅₀ of 0.113 µM and agonism of CB2 with a Ki of 0.292 µM. The compound is used to study the roles of GPR55 and CB2 in various cellular processes. It modulates signaling pathways associated with these receptors, potentially affecting cell proliferation, inflammation, and pain signaling. The compound is typically dissolved in DMSO for in vitro assays.
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| ln Vivo |
In vivo, PSB-SB-487 is being studied for its potential therapeutic applications in diabetes, Parkinson's disease, neuropathic pain, and cancer. By targeting GPR55 and CB2, the compound may modulate metabolic, neurodegenerative, and inflammatory pathways. However, detailed in vivo efficacy and pharmacokinetic data are not extensively documented in the available literature. The compound is primarily used as a research tool for preclinical pharmacology studies.
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| Enzyme Assay |
In vitro, cell lines expressing GPR55 or CB2 are treated with PSB-SB-487 at various concentrations. Receptor activity is assessed using standard functional assays, such as calcium mobilization assays for GPR55 or cAMP accumulation assays for CB2. The compound is typically dissolved in DMSO and diluted in assay buffer. The IC₅₀ for GPR55 antagonism and the Ki for CB2 agonism are determined. The compound's effects on downstream signaling pathways can also be assessed.
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| Animal Protocol |
In vivo, PSB-SB-487 is administered to animal models of diabetes, Parkinson's disease, neuropathic pain, or cancer. The compound is typically administered via intraperitoneal or oral routes. The animals are monitored for changes in disease-related parameters, such as blood glucose levels, motor function, pain sensitivity, or tumor growth. The compound's efficacy and safety are evaluated. All procedures are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
PSB-SB-487 has a molecular weight of 408.53 and the chemical formula C₂₆H₃₂O₄. It is a small molecule with a chromenone core. The compound is soluble in DMSO. It should be stored as a powder at -20°C for up to 3 years and at 4°C for up to 2 years. The compound is for research use only and not for human therapeutic use.
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| Toxicity/Toxicokinetics |
Specific toxicity data for PSB-SB-487 are not extensively documented. As a GPR55 antagonist and CB2 agonist, it may modulate immune and inflammatory responses. The compound is for research use only and not for human therapeutic use. It should be handled with appropriate safety precautions, including the use of personal protective equipment. The compound should be stored in a sealed container in a cool, dry place away from incompatible materials.
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| References | |
| Additional Infomation |
PSB-SB-487 is a potent GPR55 antagonist and CB2 agonist with an IC₅₀ of 0.113 µM for GPR55 and a Ki of 0.292 µM for human CB2. It is being studied for potential applications in diabetes, Parkinson's disease, neuropathic pain, and cancer. It is a small molecule with a molecular weight of 408.53. It is supplied as a powder and should be stored at -20°C. It is for research use only.
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| Molecular Formula |
C26H32O4
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|---|---|
| Molecular Weight |
408.529888153076
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| Exact Mass |
408.23
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| CAS # |
1399049-81-0
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| PubChem CID |
70678101
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| Appearance |
White to off-white solid powder
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| LogP |
8.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
596
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C(CC2C=CC=CC=2O)=CC2=C(C=C(C=C12)C(C)(C)CCCCCCC)O)=O
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| InChi Key |
YNWOMOUVWNKICO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H32O4/c1-4-5-6-7-10-13-26(2,3)20-16-23(28)21-15-19(25(29)30-24(21)17-20)14-18-11-8-9-12-22(18)27/h8-9,11-12,15-17,27-28H,4-7,10,13-14H2,1-3H3
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| Chemical Name |
5-hydroxy-3-[(2-hydroxyphenyl)methyl]-7-(2-methylnonan-2-yl)chromen-2-one
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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 : ~100 mg/mL (~244.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.12 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 25.0 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: ≥ 2.5 mg/mL (6.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4478 mL | 12.2390 mL | 24.4780 mL | |
| 5 mM | 0.4896 mL | 2.4478 mL | 4.8956 mL | |
| 10 mM | 0.2448 mL | 1.2239 mL | 2.4478 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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