GSK2239633A


CAS No. : 1240516-71-5

1240516-71-5
Price and Availability of CAS No. : 1240516-71-5
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5mg $160 In-stock
10mg $260 In-stock
25mg $550 In-stock
50mg $880 In-stock
100mg $1400 In-stock
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Cat. No. : HY-100183
M.Wt: 549.06
Formula: C24H25ClN4O5S2
Purity: >98 %
Solubility: DMSO : ≥ 250 mg/mL (455.32 mM)
Introduction of 1240516-71-5 :

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11. IC50 & Target: CCR4[1] In Vitro: The GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with a pA2 of 7.11±0.29[1]. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4+ CCR4+ T cells is measured. The pEC50 value is 8.79±0.22[2]. In Vivo: Following intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t1/2: 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach Cmax rapidly (median tmax: 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%[1]. GSK2239633A (Compound 9) demonstrates good pharmacokinetic data in preclinical animal studies (bioavailability in rats and beagle dogs 85% and 97% respectively)[3].

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