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Submit ReviewPF 04628935
Description: Potent ghrelin receptor inverse agonist
Chemical Name: 1-[2-[[2-Chloro-4-(2H-1,2,3-triazol-2-yl)phenyl]methyl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone
Purity: ≥98% (HPLC)
Biological Activity for PF 04628935
PF 04628935 is a potent ghrelin receptor inverse agonist (IC50 = 4.6 nM). Orally bioavailable and exhibits reasonable brain penetration.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 04628935
PF 04628935 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PF 04628935
| M. Wt | 496.03 |
| Formula | C24H26ClN7OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1383719-97-8 |
| PubChem ID | 70682037 |
| InChI Key | MTDYDDJVCIHZKH-UHFFFAOYSA-N |
| Smiles | ClC1=C(CN2CC3(CCN(C(CC4=CN(C=C(C)S5)C5=N4)=O)CC3)C2)C=CC(N6N=CC=N6)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 04628935
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.8 | 50 | |
| ethanol | 9.92 | 20 |
Preparing Stock Solutions for PF 04628935
The following data is based on the product molecular weight 496.03. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.03 mL | 20.16 mL | 40.32 mL |
| 2.5 mM | 0.81 mL | 4.03 mL | 8.06 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.03 mL |
| 25 mM | 0.08 mL | 0.4 mL | 0.81 mL |
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Product Datasheets for PF 04628935
References for PF 04628935
References are publications that support the biological activity of the product.
Kung et al (2012) Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg.Med.Chem.Lett. 22 5410 PMID: 22677316
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Keywords: PF 04628935, PF 04628935 supplier, PF04628935, inverse, agonists, agonism, ghrelin, orally, bioavailable, potent, Ghrelin, Receptors, 6347, Tocris Bioscience
Citations for PF 04628935
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.