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.
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- CAS 番号: 2641013-11-6
- 分子式: C21H21F2N3O
- 分子量:369.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 2641013-11-6
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分子量 369.41
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Progranulin modulator-1 関連分類
HY-153690 関連分類
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