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BMS-823778
CAS No. 1140898-87-8
BMS-823778( BMS823778 )
Catalog No. M10497 CAS No. 1140898-87-8
BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 873 | Get Quote |
|
| 50MG | 1782 | Get Quote |
|
| 100MG | 2250 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameBMS-823778
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NoteResearch use only, not for human use.
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Brief DescriptionBMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM.
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DescriptionBMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2; exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).Diabetes Phase 2 Clinical.
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In Vitro——
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In VivoAnimal Model:Diet-induced obese (DIO) miceDosage:10-100 mg/kg Administration:Oral, once 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.Animal Model:Male Balb/C mice Dosage:5 or 10 mg/kg Administration:IV or PO (Pharmacokinetic Analysis)Result:Single-Dose Pharmacokinetic Parameters of BMS-823778.
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SynonymsBMS823778
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PathwayMetabolic Enzyme/Protease
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Target11β-HSD
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Recptor11β-HSD
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Research AreaMetabolic Disease
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IndicationDiabetes
Chemical Information
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CAS Number1140898-87-8
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Formula Weight364.27
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Molecular FormulaC18H18ClN3O · HCl
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Purity>98% (HPLC)
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Solubility——
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SMILESCC(C)(C1=CC=CN2C1=NN=C2C3(CC3)C4=CC=C(C=C4)Cl)O.Cl
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Chemical Name3-[1-(4-Chlorophenyl)cyclopropyl]-α,α-dimethyl-1,2,4-triazolo[4,3-a]pyridine-8-methanol hydrochloride
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Cheng Y, et al. Br J Clin Pharmacol. 2018 Jan;84(1):130-141.
2.?Jun Li, et al. Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1). ACS Med. Chem. Lett. 2018 Nov. DOI: 10.1021/acsmedchemlett.8b00307.
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