Description
SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
Product information
CAS Number: 395679-53-5
Molecular Weight: 500.55
Formula: C28H31F3N2O3
Chemical Name: N-{4-[2-(diethylamino)ethoxy]-3-methoxyphenyl}-N-methyl-4'-(trifluoromethyl)-[1,1'-biphenyl]-4-carboxamide
Smiles: CN(C(=O)C1C=CC(=CC=1)C1C=CC(=CC=1)C(F)(F)F)C1C=C(OC)C(=CC=1)OCCN(CC)CC
InChiKey: JAIIZWCZERLWEK-UHFFFAOYSA-N
InChi: InChI=1S/C28H31F3N2O3/c1-5-33(6-2)17-18-36-25-16-15-24(19-26(25)35-4)32(3)27(34)22-9-7-20(8-10-22)21-11-13-23(14-12-21)28(29,30)31/h7-16,19H,5-6,17-18H2,1-4H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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