BMS-814580
BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities.
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- CAS No.: 1197420-11-3
- Formule: C24H19ClF2N2O4S
- Masse moléculaire:504.93
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
Ki: 16.9 nM (MCHR1)[1]
In Vitro
BMS-814580 (3.0 μM; 10 min) shows stability with 90%, 95% and 100% remaining in human, rat and mouse liver microsomes, respectively[1].
BMS-814580 displays modest in vitro ion channel inhibition of 43%, 21%, and 15%, respectively, for hERG, Na (4 Hz), and L-type Ca channels at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Obese male SD rats, chronic diet-induced obese (DIO) rat model[1]
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Dosage:0.03, 0.1, 0.3, 1 and 3 mg/kg
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Administration:Orally administered as the phosphate prodrug, once daily for 28 days
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Result:Dose dependently reduced body weight.
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Animal Model:Sprague-Dawley Rats[1]
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Dosage:10 mg/kg
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Administration:Oral administration, once
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Result:Pharmacokinetics (PK) and Pharmacodynamics (PD) Data: Plasma and Brain Concentrations of Cyclic Tertiary Alcohols and the Effect on Body Weights in Sprague-Dawley Rats
8 h rat PK studyb 4-day PD studyc day 4 parent compd concn at 20 h compd dosed asa AUC (μM•h) brain (nM) plasma (nM) % weight loss brain (nM) plasma (nM) BMS-814580 glycinate 38.1 11330 4500 6.4d 7955 12801
aRats were dosed orally with parent compound or a prodrug; prodrugs doses were adjusted to parent compounds. Vehicle = 0.5% Methocel, 0.1% Tween 80, 99.4% distilled water. bDose = 10 mg/kg; plasma and brain concentrations are reported 8 h after dose, n = 2. cCompounds were dosed at 3, 10, and 30 mg/kg orally once a day for 4 days; weight loss data is reported only for the 10 mg/kg dose, n = 8; reduction in body weight is reported as % change from baseline body weight compared to vehicle treated animals. NT = not tested. dNo biliary lesions were seen in this model.
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Animal Model:Sprague-Dawley Rats[1]
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Dosage:10 mg/kg (phosphate prodrug) or 1 mg/kg
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Administration:Oral (phosphate prodrug) or intravenous administration (Pharmacokinetic Analysis)
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Result:Pharmacokinetics Data for BMS-814580 in Rata
species compd (mg/kg) route of admin Cmax (μM) Tmax (h) AUC0−∞ (μM•h) T1/2 (h) CL (mL/min/kg) Vss(L/kg) F (%) rat BMS-814580 (1) iv 11.5 >24 0.9 4.1 BMS-814580 phosphate (10) po 4.0 6.7 107 54
aVehicles: iv, PEG400/DMAC/water (70:5:25); po, Methocel/Tween80/water (0.5:0.1:99.4).
Chemical Information
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CAS No. 1197420-11-3
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Masse moléculaire 504.93
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Formule C24H19ClF2N2O4S
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SMILES
O=C1C2=C(N=CN1C3=CC=C(OCC4(O)CC(C4)(F)F)C(OC)=C3)C=C(S2)C5=CC=C(C=C5)Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-814580 Related Classifications
HY-120608 Related Classifications
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