S-777469
Based on 1 Customer Validation
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.
For research use only. We do not sell to patients.
- Purity: 98.19%
- CAS No.: 885496-53-7
- Formula: C23H27FN2O4
- Molecular Weight:414.47
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
24 nM
Compound: 15, S-777469
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Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins
Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins
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[PMID: 22444677] |
| CHO | IC50 |
>2000 nM
Compound: 15, S-777469
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Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins
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[PMID: 22444677] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 885496-53-7
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Appearance Solid
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Molecular Weight 414.47
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Formula C23H27FN2O4
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Color Off-white to light yellow
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SMILES
O=C(C1=CC(C)=C(CC)N(CC2=CC=C(C=C2)F)C1=O)NC3(CCCCC3)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 83.33 mg/mL (201.05 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 (protect from light). 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 (protect from light). 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 (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Odan M, et al. Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2803-6. [Content Brief]
[2]. Haruna T, et al. S-777469, a novel cannabinoid type 2 receptor agonist, suppresses itch-associated scratching behavior in rodents through inhibition of itch signal transmission. Pharmacology. 2015;95(1-2):95-103. [Content Brief]
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 (protect from light). 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 | 2.4127 mL | 12.0636 mL | 24.1272 mL | 60.3180 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8254 mL | 12.0636 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4127 mL | 6.0318 mL | |
| 15 mM | 0.1608 mL | 0.8042 mL | 1.6085 mL | 4.0212 mL | |
| 20 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9651 mL | 2.4127 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0106 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5079 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 1.2064 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4021 mL | 1.0053 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6032 mL |
S-777469 Related Classifications
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