1. GPCR/G Protein
  2. Angiotensin Receptor
  3. CGP-42112

CGP-42112 (Synonyms: CGP42112A)

Cat. No.: HY-12405 Purity: 99.02%
Handling Instructions

CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.

For research use only. We do not sell to patients.

CGP-42112 Chemical Structure

CGP-42112 Chemical Structure

CAS No. : 127060-75-7

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 1238 In-stock
Estimated Time of Arrival: December 31
1 mg USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 535 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist[1].

In Vitro

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].

In Vivo

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].

Molecular Weight

1052.19

Formula

C₅₂H₆₉N₁₃O₁₁

CAS No.

127060-75-7

SMILES

CC[[email protected]](C)[[email protected]@H](C(O)=O)NC([[email protected]]1N(C([[email protected]](CC2=CNC=N2)NC([[email protected]](CCCCNC([[email protected]](CCCNC(N)=N)NC(OCC3=CC=CC=C3)=O)=O)NC([[email protected]](CC4=CC=C(C=C4)O)NC(C5=CC=CN=C5)=O)=O)=O)=O)CCC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 350 mg/mL (332.64 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9504 mL 4.7520 mL 9.5040 mL
5 mM 0.1901 mL 0.9504 mL 1.9008 mL
10 mM 0.0950 mL 0.4752 mL 0.9504 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

CGP-42112CGP42112ACGP42112CGP 42112Angiotensin ReceptorInhibitorinhibitorinhibit

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CGP-42112
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