For research use only. Not for therapeutic Use.
CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist[1].
CGP-42112 (≥1 nM) significantly inhibits cGMP production from the basal value. CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity from the basal value. These inhibitory effects of CGP-42112 on TH-enzyme activity and-cGMP production are abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) is ineffective[1].
[125I]CGP-42112 binds selectively to the AT2 angiotensin II receptor subtype. [125I]CGP-42112 binds with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP-42112 binding in the brain, but does not alter its binding in the adrenal[2].
[125I]CGP-42112 binds with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP-42112 binding is selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 and the non-selective peptides Ang II and angiotensin III (Ang III)[4].
Intravenous infusions of CGP-42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF[3].
| Catalog Number | I001082 |
| CAS Number | 127060-75-7 |
| Synonyms | (2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-[[(2S)-5-(diaminomethylideneamino)-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-2-[[(2S)-3-(4-hydroxyphenyl)-2-(pyridine-3-carbonylamino)propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid |
| Molecular Formula | C52H69N13O11 |
| Purity | ≥95% |
| InChI | InChI=1S/C52H69N13O11/c1-3-32(2)43(50(73)74)64-48(71)42-17-11-25-65(42)49(72)41(27-36-29-56-31-59-36)62-46(69)39(60-47(70)40(26-33-18-20-37(66)21-19-33)61-44(67)35-14-9-22-55-28-35)15-7-8-23-57-45(68)38(16-10-24-58-51(53)54)63-52(75)76-30-34-12-5-4-6-13-34/h4-6,9,12-14,18-22,28-29,31-32,38-43,66H,3,7-8,10-11,15-17,23-27,30H2,1-2H3,(H,56,59)(H,57,68)(H,60,70)(H,61,67)(H,62,69)(H,63,75)(H,64,71)(H,73,74)(H4,53,54,58)/t32-,38-,39-,40-,41-,42-,43-/m0/s1 |
| InChIKey | UXGNARZDONUMMK-LRMQDCNJSA-N |
| SMILES | CCC(C)C(C(=O)O)NC(=O)C1CCCN1C(=O)C(CC2=CN=CN2)NC(=O)C(CCCCNC(=O)C(CCCN=C(N)N)NC(=O)OCC3=CC=CC=C3)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C5=CN=CC=C5 |
| Reference | [1]. Takekoshi K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells. Biochem Biophys Res Commun. 2000 Jun 7;272(2):544-50. [2]. Speth RC. [125I]CGP 42112 binding reveals differences between rat brain and adrenal AT2 receptor binding sites. Regul Pept. 1993 Mar 19;44(2):189-97. [3]. Naveri L, et al. Angiotensin II AT2 receptor stimulation extends the upper limit of cerebral blood flow autoregulation: agonist effects of CGP 42112 and PD 123319. J Cereb Blood Flow Metab. 1994 Jan;14(1):38-44. [4]. Heemskerk FM, et al. Quantitative autoradiography of angiotensin II AT2 receptors with [125I]CGP 42112. Brain Res. 1995 Apr 17;677(1):29-38. |
