Bioactivity | GPR10 agonist 1 (compound 18-S4) is a potent GPR10 agonist with EC50 values of 80, 7.8 nM in the presence (10%) or absence (0%) of FBS, respectively. GPR10 agonist 1 has the potential for the research of chronic obesity[1]. |
In Vivo | GPR10 agonist 1 (compound 18-S4) (0.5, 5 mg/kg; s.c.; daily for 12 day) 可降低饮食引起的肥胖 (DIO) 小鼠的体重[1]。药代动力学参数 (1 mg/kg; s.c.; 7-9 weeks, male C57 mice)[1]。 t1/2(h) |
Sequence | Ser-Arg-Ala-His-Gln-Cys-Ser-{Nle}-Glu-Thr-Arg-Thr-Cys-Asp-Ile-Asn-Pro-Ala-Trp-Tyr-Thr-Gly-{hArg}-Gly-Ile-Arg-Pro-Val-Gly-Arg-Phe-NH2 (Disulfide bridge: Cys6-Cys13; multiple ethylene glycol-fatty acid; hArg=Homoarginine) |
Shortening | SRAHQCS-{Nle}-ETRTCDINPAWYTG-{hArg}-GIRPVGRF-NH2 (Disulfide bridge: Cys6-Cys13; multiple ethylene glycol-fatty acid; hArg=Homoarginine) |
Formula | C200H324N58O57S2 |
Molar Mass | 4517.20 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Pflimlin E, et al. Design of a Long-Acting and Selective MEG-Fatty Acid Stapled Prolactin-Releasing Peptide Analog. ACS Med Chem Lett. 2019 Jul 5;10(8):1166-1172. |