Progranulin modulator-1
Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 2641013-11-6
- Formula: C21H21F2N3O
- Molecular Weight:369.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EC50: 83 nM (PGRN); IC50: 3100 nM (hERG)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BV-2 | EC50 |
83 nM
Compound: 60
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Induction of progranulin secretion in mouse BV-2 cells
Induction of progranulin secretion in mouse BV-2 cells
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[PMID: 36368496] |
Progranulin modulator-1 (Compound 60) has an efflux ratio (ER) value <2, indicating that it is not a substrate for MDR and shows high brain tissue binding and high metabolic stability[1].
Progranulin modulator-1 In vitro ADME properties for selected molecules[1]
| MDCK-MDR1 PappA→B [ER] | Protein Binding, Fu | Brain Tissue Binding, Fu | Hepatocytes t1/2 , CLint |
| 0.53 [1.11] | 3.1 (m); 5.5 (h) | 0.9 (m) | >120, <68.2 (m); >120, <14.7 (h) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Parameters for Progranulin Modulator-1 in Mouse[1]
| PO t1/2 (h) | IV t1/2 (h) | Cmax,u (nM) | Kpuu @ 8 h | F (%) | CL | Vdss |
| 4.8 | 7.4 | 62 | 2.91 | 99 | 2.08 | 15.2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2641013-11-6
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Molecular Weight 369.41
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Formula C21H21F2N3O
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SMILES
FC1=CC=C(C=C1)[C@@H]2N(C3=N[C@H](C4(CNC4)F)CO3)CCC5=CC=CC=C52
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Progranulin modulator-1 Related Classifications
HY-153690 Related Classifications
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