BMS-823778 hydrochloride
BMS-823778 hydrochloride is a potent, selective and orally active 11β-HSD1 inhibitor with an IC50 of 2.3 nM against human 11β-HSD1.
For research use only. We do not sell to patients.
- CAS No.: 1140898-87-8
- Formula: C18H19Cl2N3O
- Molecular Weight:364.27
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
Biological Activity
IC50: 2.3 nM (human 11β-HSD1), 600 nM (mouse 11β-HSD1)[1]
Ki: 0.9 nM (human 11β-HSD1), 380 nM (mouse 11β-HSD1)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obese (DIO) mice[1]
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Dosage:10-100 mg/kg
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Administration:Oral, once
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Result:Inhibition of 11β-HSD-1 was observed as a measure of decrease in the plasma concentration of corticosterone. The ED50 was 34 mg/kg.
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Animal Model:Male Balb/C mice[1]
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Dosage:5 or 10 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Single-Dose Pharmacokinetic Parameters of BMS-823778[1]
Species Route Dose (mg/kg) Cmax (µM) Tmax (h) AUC(0-24 h) (µM•h) T1/2 (h) CLTp (mL/min/kg) Vss (L/kg) F (%) Mouse IV* 5 - - 106 5.2 2.3 1.2 - PO** 10 10.6 ± 1.3 3 95 - - - 44
*PO Vehicle: 0.5% Methocel/0.1% Tween 80
** IV vehicle: 10% ethanol/30% propylene glycol/60% normal saline
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1140898-87-8
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Molecular Weight 364.27
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Formula C18H19Cl2N3O
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SMILES
CC(O)(C1=CC=CN2C1=NN=C2C3(C4=CC=C(Cl)C=C4)CC3)C.Cl
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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)
BMS-823778 hydrochloride Related Classifications
HY-120643 Related Classifications
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