PROTAC PDE4 degrader-1
PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model.
(Pink: PDE4 ligand (HY-174410); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3087311-36-9
- Formula: C30H27F2N5O7S
- Molecular Weight:639.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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PDE4 41.98 μM (DC50) |
IL-6 |
| Species | Dose | Route | Tmax | T1/2 | F | Cmax | AUC0-t | AUC0-∞ | C0 | Vz | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 0.25 h | 1.05 h | 20.99 % | 989 ng/mL | 1099 ng·h/mL | 1108 ng·h/mL | / | / | / |
| Mice | 5 mg/kg | i.v. | / | 0.59 h | / | / | 2618 ng·h/mL | 2622 ng·h/mL | 12450 ng/mL | 1823 mL/kg | 2026 mL/h/kg |
Chemical Information
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CAS No. 3087311-36-9
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Molecular Weight 639.63
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Formula C30H27F2N5O7S
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SMILES
O=C1CCC(C(N1)=O)N2C(C3=CC=CC(NCCNC(C4=CSC(C5=CC=C(C(OCC6CC6)=C5)OC(F)F)=N4)=O)=C3C2=O)=O
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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)