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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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]
In Vivo
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
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| 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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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