Description
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
Product information
CAS Number: 215804-67-4
Molecular Weight: 475.02
Formula: C28H31ClN4O
Chemical Name: N-((1r, 4r)-4-(2-(6-cyano-3, 4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)quinoline-4-carboxamide hydrochloride
Smiles: Cl.N#CC1C=CC2CN(CCC=2C=1)CC[C@@H]1CC[C@H](CC1)NC(=O)C1=CC=NC2=CC=CC=C21
InChiKey: DKPTUMKZXQOJCX-DYXJTDGYSA-N
InChi: InChI=1S/C28H30N4O.ClH/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27;/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33);1H/t20-,24-;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (105.26 mM; Need ultrasonic). H2O : 16.67 mg/mL (35.09 mM; Need ultrasonic).
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 Vivo:
SB-277011 hydrochloride has an excellent pharmacokinetic profile, exhibits oral bioavailability 43%, half-life:2.0 h, plasma clearance 19 mL/min/kg) and to be highly brain-penetrant (brain:blood ratio of 3.6:1), with a clean P450 profile in the rat. SB-277011 hydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats. SB-277011 (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011 can significantly inhibit basal and cocaine-enhanced locomotion in rats.
Products are for research use only. Not for human use.
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