DPTIP-prodrug 18
DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research.
For research use only. We do not sell to patients.
- CAS No.: 2881068-33-1
- Formula: C36H44N4O4S
- Molecular Weight:628.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
nSMase2[1]
DPTIP-prodrug 18 is metabolically stable with >75% intact prodrug remaining after 1 h of incubation at 37 °C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DPTIP-prodrug 18 shows significant inhibition of nSMase2 activity and IL-1β-induced EV release in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CES1–/– mice[1]
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Dosage:10 mg/kg DPTIP equivalent
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Administration:Orally, once (Pharmacokinetic Analysis)
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Result:Exhibited >fourfold higher plasma (AUC0-t=1047 pmol·h/mL) and brain exposures (AUC0-t=247 pmol·h/g) versus DPTIP and a significant enhancement of DPTIP half-life (2 h vs ~0.5 h).
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Animal Model:Interleukin-1β-injected mice (a mouse model of brain injury)[1]
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Dosage:0, 3 and 10 mg/kg (DPTIP equivalent)
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Administration:Orally, once
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Result:Significantly inhibited the release of brain-derived GFP+ EVs into the blood at both 3 and 10 mg/kg (DPTIP equivalent dose).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2881068-33-1
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Molecular Weight 628.82
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Formula C36H44N4O4S
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SMILES
COC1=CC(C2=NC(C3=CC=CC=C3)=C(C4=CC=CS4)N2)=CC(OC)=C1OC(N5C(CC)CC(CC5CC)N6CCCCC6)=O
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Synonyms
P18
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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)
DPTIP-prodrug 18 Related Classifications
HY-149025 Related Classifications
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