Cas No.: | 1876450-21-3 |
Chemical Name: | MM 07 |
Synonyms: | MM 07;cyclo[1-6]CRPRLCHKGPMPF;GTPL8523;MM07;BDBM50518047;H-Cys(1)-Arg-Pro-Arg-Leu-Cys(1)-His-Lys-Gly-Pro-Met-Pro-Phe-OH;L-cysteinyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-cysteinyl-L-histidyl-L-lysyl-glycyl-L-prolyl-L-methionyl-L-prolyl-L-phenylalanine (1->6)-disulfide |
SMILES: | S(C)CC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(=O)O)CC1C=CC=CC=1)=O)=O)NC([C@@H]1CCCN1C(CNC([C@H](CCCCN)NC([C@H](CC1=CN=CN1)NC([C@@H]1CSSC[C@@H](C(N[C@@H](CCC/N=C(\N)/N)C(N2CCC[C@H]2C(N[C@H](C(N[C@H](C(N1)=O)CC(C)C)=O)CCC/N=C(\N)/N)=O)=O)=O)N)=O)=O)=O)=O)=O |
Formula: | C67H106N22O14S3 |
M.Wt: | 1539.89254903793 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart. |
Target: | KD: 300 nM (apelin receptor in CHO-K1 cells), 172 nM (apelin receptor in human heart)[1]. |
In Vivo: | MM 07 causes a dose-dependent increase in cardiac output, and although there is a decrease in vascular resistance, this is without corresponding effects on BP. Administration of SNAP produces a profound fall in BP in both [Pyr1]apelin-13 and MM 07-treated groups; however, although cardiac output is significantly increased in response to SNAP in the MM 07 group, it is significantly reduced in the [Pyr1]apelin-13 group. Neither peptide causes a significant change in heart rate, respiratory rate, or temperature. Both [Pyr1]apelin 13 and MM 07 increases peak velocity above basal levels[1]. |
In Vitro: | MM 07 competes with nanomolar affinities for binding of [Glp65,Nle75,Tyr77] [125I]apelin-13 to human apelin receptors in CHO-K1 cells (KD, 300 nM) and human heart (KD, 172 nM, n=3)[1]. |
Animal Administration: | Rats[1]Rats (230-260 g), anaesthetized with 2% isoflurane, are given a single intravenous bolus (600 nM) of apelin or MM 07 (both n=3)[1]. |
References: | [1]. Brame AL, et al. Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist. Hypertension. 2015 Apr;65(4):834-40. |