| Bioactivity | (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06[1]. | |||||||||
| Invitro | (αR,8aS)-GSK1614343 (0.1-1μM) demonstrats a surmountable and competitive antagonism of hGHSR1a with a mean p KB value of 8.06[1]. | |||||||||
| In Vivo | (αR,8aS)-GSK1614343 (10 mg/kg; i.v. once) inhibits GH release induced by exogenous ghrelin administration[1].(αR,8aS)-GSK1614343 (i.v. and p.o.) exhibits good oral bioavailability (F=46%), a limited clearance in blood (Clb=28 mL/min/kg) and a suitable half-life (5.0 h). In terms of rat brain penetration, a brain to blood AUC(αR,8aS)-GSK1614343 exhibits a clean profile in terms of inhibition potential for the major human CYP450 isoforms with IC50 value of ≥10 μM[1]. | |||||||||
| Name | (αR,8aS)-GSK1614343 | |||||||||
| CAS | 1092476-84-0 | |||||||||
| Formula | C22H23F6N5O | |||||||||
| Molar Mass | 487.44 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. https://pubmed.ncbi.nlm.nih.gov/20593439/ |
(αR,8aS)-GSK1614343
CAS: 1092476-84-0 F: C22H23F6N5O W: 487.44
(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK161434
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