PF-04628935
Based on 1 Customer Validation
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 1383719-97-8
- Formula: C24H26ClN7OS
- Molecular Weight:496.03
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Storage:Powder -20°C, 3 years , 4°C, 2 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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GHSR1a 4.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4.6 nM
Compound: 10n
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Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
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[PMID: 22677316] |
Chemical Information
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CAS No. 1383719-97-8
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Appearance Solid
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Molecular Weight 496.03
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Formula C24H26ClN7OS
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Color Light yellow to yellow
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SMILES
CC1=CN2C(S1)=NC(CC(N3CCC4(CN(C4)CC5=CC=C(C=C5Cl)N6N=CC=N6)CC3)=O)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (100.80 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 (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Kung DW, et, al. Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. [Content Brief]
[2]. Cavalcante DP, et, al. Role of dorsal raphe nucleus GHS-R1a receptors in the regulation of inhibitory avoidance and escape behaviors in rats. Behav Brain Res. 2019 Jun 3;365:178-184. [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. 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 | 2.0160 mL | 10.0800 mL | 20.1601 mL | 50.4002 mL |
| 5 mM | 0.4032 mL | 2.0160 mL | 4.0320 mL | 10.0800 mL | |
| 10 mM | 0.2016 mL | 1.0080 mL | 2.0160 mL | 5.0400 mL | |
| 15 mM | 0.1344 mL | 0.6720 mL | 1.3440 mL | 3.3600 mL | |
| 20 mM | 0.1008 mL | 0.5040 mL | 1.0080 mL | 2.5200 mL | |
| 25 mM | 0.0806 mL | 0.4032 mL | 0.8064 mL | 2.0160 mL | |
| 30 mM | 0.0672 mL | 0.3360 mL | 0.6720 mL | 1.6800 mL | |
| 40 mM | 0.0504 mL | 0.2520 mL | 0.5040 mL | 1.2600 mL | |
| 50 mM | 0.0403 mL | 0.2016 mL | 0.4032 mL | 1.0080 mL | |
| 60 mM | 0.0336 mL | 0.1680 mL | 0.3360 mL | 0.8400 mL | |
| 80 mM | 0.0252 mL | 0.1260 mL | 0.2520 mL | 0.6300 mL | |
| 100 mM | 0.0202 mL | 0.1008 mL | 0.2016 mL | 0.5040 mL |
PF-04628935 Related Classifications
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