1. GPCR/G Protein
  2. MCHR1 (GPR24)
  3. SB-568849

SB-568849 

Cat. No.: HY-100308
Handling Instructions

SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.

For research use only. We do not sell to patients.

SB-568849 Chemical Structure

SB-568849 Chemical Structure

CAS No. : 395679-53-5

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10 mg USD 2404 Get quote

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Description

SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.

IC50 & Target

MCH R1 receptor[1]

In Vitro

SB-568849 is a selective SLC-1 antagonist with a pKi of 7.7 as determined in radioligand binding displacement assays; coincubation of tissue with 1 μM SB-568849 for 45 min completely inhibits the MCH induced increase in corticotropin-releasing factor (CRF) release to basal levels without causing any effect on its own. The only reported MCH receptor in the rat is SLC-1, a G protein coupled receptor found throughout the brain and periphery[2].

In Vivo

SB-568849 (Compound 15h) possesses good receptor affinity and selectivity. SB-568849 proves to be an antagonist with stability in vivo, an acceptable brain–blood ratio and oral bioavailability. SB-568849 retains affinity, demonstrates greater in vivo stability (CLb=16 mL/min/kg) and shows an acceptable brain-blood ratio of 1. SB-568849 also shows >30-fold selectivity over a wide range of monoamine receptors and is an antagonist in the FLIPR assay with a pKb of 7.7[3].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

500.55

Formula

C₂₈H₃₁F₃N₂O₃

CAS No.

395679-53-5

SMILES

O=C(C1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)N(C3=CC=C(OCCN(CC)CC)C(OC)=C3)C

Shipping

Room temperature in continental US; may vary elsewhere

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SB-568849
Cat. No.:
HY-100308
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SB-568849

Cat. No.: HY-100308