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| Cas No.: | 133737-32-3 |
| Synonyms: | (+)-RP-59037; IP-456; RP-62955; CI-1043 |
| SMILES: | O=C1N(C2=CC=C(C=C3)C(N=C3Cl)=N2)C(CC(CCC(C)C)=O)C4=CC=CC=C4 |
| Formula: | C23H22ClN3O2 |
| M.Wt: | 407.89 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Pagoclone has high and approximately equivalent affinity (Ki values=0.7-9.1 nM) for recombinant human GABAA receptors containing either an α1, α2, α3 or α5 subunit. Pagoclone has significant agonist activity at all four diazepam-sensitive GABAA receptor subtypes, with EC50 of 3.1-6.6 nM.Pagoclone (3 mg/kg, p.o.) has significant anxiolytic-like activity, but at all three doses tested (0.3, 1 and 3 mg/kg p.o.) it produces a significant reduction in the total distance travelled. Pagoclone (3 mg/kg, p.o.) produces a dose-dependent increase in time spent on the open arms compared to control. Pagoclone (1, 3 or 10 mg/kg) lowers the cumulative chain-pulling response in the response sensitivity test. Plasma pagoclone concentrations are dose-dependent but not linear, with plasma concentrations of pagoclone being 0.4±0.1, 1.1±0.2 and 2.2±0.2 ng/mL, respectively. Pagoclone (0.3, 1 or 3 mg/kg) reduces locomotor activity in rats in a dose dependent manner. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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