For research use only. Not for therapeutic Use.
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.
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].
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].
Catalog Number | I019770 |
CAS Number | 1876450-21-3 |
Synonyms | (2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[2-[[(2S)-6-amino-2-[[(2S)-2-[[(3S,6R,11R,14S,17S,20S)-6-amino-3,17-bis[3-(diaminomethylideneamino)propyl]-14-(2-methylpropyl)-2,5,13,16,19-pentaoxo-8,9-dithia-1,4,12,15,18-pentazabicyclo[18.3.0]tricosane-11-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]hexanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid |
Molecular Formula | C67H106N22O14S3 |
Purity | ≥95% |
InChI | InChI=1S/C67H106N22O14S3/c1-38(2)30-46-57(94)86-49(36-106-105-35-41(69)54(91)81-44(18-10-25-76-67(72)73)63(100)88-27-12-20-51(88)61(98)80-43(56(93)83-46)17-9-24-75-66(70)71)59(96)84-47(32-40-33-74-37-78-40)58(95)79-42(16-7-8-23-68)55(92)77-34-53(90)87-26-11-19-50(87)60(97)82-45(22-29-104-3)64(101)89-28-13-21-52(89)62(99)85-48(65(102)103)31-39-14-5-4-6-15-39/h4-6,14-15,33,37-38,41-52H,7-13,16-32,34-36,68-69H2,1-3H3,(H,74,78)(H,77,92)(H,79,95)(H,80,98)(H,81,91)(H,82,97)(H,83,93)(H,84,96)(H,85,99)(H,86,94)(H,102,103)(H4,70,71,75)(H4,72,73,76)/t41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-/m0/s1 |
InChIKey | RKFGCZWTURNFPN-SVENNQHVSA-N |
SMILES | CC(C)CC1C(=O)NC(CSSCC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)CCCN=C(N)N)CCCN=C(N)N)N)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCCCN)C(=O)NCC(=O)N4CCCC4C(=O)NC(CCSC)C(=O)N5CCCC5C(=O)NC(CC6=CC=CC=C6)C(=O)O |
Reference | [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. |