2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. 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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BMS-814580 Chemical Structure

BMS-814580 Chemical Structure

CAS No. : 1197420-11-3

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BMS-814580 Related Antibodies

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Description

BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities[1].

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.

BMS-814580 Related Antibodies
In Vivo

BMS-814580 (0-3 mg/kg; p.o.; once daily for 28 days) shows antiobesity activities in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Obese male SD rats, chronic diet-induced obese (DIO) rat model[1]
Dosage: 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration: Orally administered as the phosphate prodrug, once daily for 28 days
Result: Dose dependently reduced body weight.
Animal Model: Sprague-Dawley Rats[1]
Dosage: 10 mg/kg
Administration: Oral administration, once
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.
Animal Model: Sprague-Dawley Rats[1]
Dosage: 10 mg/kg (phosphate prodrug) or 1 mg/kg
Administration: Oral (phosphate prodrug) or intravenous administration (Pharmacokinetic Analysis)
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).
Molecular Weight

504.93

Formula

C24H19ClF2N2O4S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BMS-814580 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-8145801197420-11-3BMS814580BMS 814580MCHR1 (GPR24)Melanin concentrating hormone receptor 1antiobesityliver microsome stabilityorally activeInhibitorinhibitorinhibit

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