PSNCBAM-1
Based on 1 Customer Validation
PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity.
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 877202-74-9
- Formula: C22H21ClN4O
- Molecular Weight:392.88
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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hCB1-R 0.1 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>10 μM
Compound: 2; PSNCBAM-1
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Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c
Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c
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[PMID: 31596583] |
| CHO-K1 | EC50 |
3.84 nM
Compound: 2; PSNCBAM-1
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Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay
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[PMID: 26529344] |
| CHO-K1 | EC50 |
70.8 nM
Compound: 2; PSNCBAM-1
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Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte
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[PMID: 26529344] |
| HEK293 | EC50 |
167 nM
Compound: 4, PSNCBAM-1
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Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting
Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting
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[PMID: 25162172] |
| HEK293 | IC50 |
1.47 nM
Compound: 2; PSNCBAM-1
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Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
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[PMID: 31596583] |
| HEK293 | IC50 |
2620 nM
Compound: 2; PSNCBAM-1
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Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure
Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure
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[PMID: 31596583] |
| HEK293 | IC50 |
455 nM
Compound: 2; PSNCBAM-1
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Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
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[PMID: 31596583] |
| U-937 | IC50 |
>10 μM
Compound: PSNCBAM-1
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Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method
Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method
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[PMID: 29079014] |
Chemical Information
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CAS No. 877202-74-9
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Appearance Solid
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Molecular Weight 392.88
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Formula C22H21ClN4O
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1NC(NC2=CC=CC(C3=CC=CC(N4CCCC4)=N3)=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (318.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5453 mL | 12.7265 mL | 25.4531 mL | 63.6327 mL |
| 5 mM | 0.5091 mL | 2.5453 mL | 5.0906 mL | 12.7265 mL | |
| 10 mM | 0.2545 mL | 1.2727 mL | 2.5453 mL | 6.3633 mL | |
| 15 mM | 0.1697 mL | 0.8484 mL | 1.6969 mL | 4.2422 mL | |
| 20 mM | 0.1273 mL | 0.6363 mL | 1.2727 mL | 3.1816 mL | |
| 25 mM | 0.1018 mL | 0.5091 mL | 1.0181 mL | 2.5453 mL | |
| 30 mM | 0.0848 mL | 0.4242 mL | 0.8484 mL | 2.1211 mL | |
| 40 mM | 0.0636 mL | 0.3182 mL | 0.6363 mL | 1.5908 mL | |
| 50 mM | 0.0509 mL | 0.2545 mL | 0.5091 mL | 1.2727 mL | |
| 60 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 1.0605 mL | |
| 80 mM | 0.0318 mL | 0.1591 mL | 0.3182 mL | 0.7954 mL | |
| 100 mM | 0.0255 mL | 0.1273 mL | 0.2545 mL | 0.6363 mL |
PSNCBAM-1 Related Classifications
HY-110179 Related Classifications
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