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CGP-42112 acetate

SKU: orb1945052

Description

CGP-42112 acetate is a selective AT2 receptor agonist. It counteracts the LPS-induced activation of protein kinase A, making it a valuable research tool for investigating the renin-angiotensin system in cardiovascular and inflammatory disease models, both in vitro and in vivo.

Research Area

Metabolism Research

Images & Validation

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CGP-42112 acetate

Key Properties

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MW1112.24
Purity99.06% (May vary between batches)
FormulaC54H73N13O13
SMILESOC(C=C1)=CC=C1C[C@H](NC(C2=CN=CC=C2)=O)C(N[C@@H](CCCCNC([C@H](CCCNC(N)=N)NC(OCC3=CC=CC=C3)=O)=O)C(N[C@@H](CC4=CN=CN4)C(N5[C@@H](CCC5)C(N[C@H](C(O)=O)[C@@H](C)CC)=O)=O)=O)=O.CC(O)=O
TargetRAAS
SolubilityDMSO:50 mg/mL (44.95 mM)

Bioactivity

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Target IC50
AT2 receptor:0.07-0.3 nM (Kd)
In Vivo
Intravenous infusions of CGP-42112 acetate (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.
In Vitro
At concentrations of ≥1 nM, CGP-42112 acetate significantly inhibits cGMP production from the basal value and also inhibits TH-enzyme activity from the basal value. The inhibitory effects of CGP-42112 acetate on TH-enzyme activity and cGMP production are nullified by PD123319 (AT(2)-R antagonist), while CV-11974 (AT(1)-R antagonist) is ineffective.[125I]CGP-42112 acetate selectively binds to the AT2 angiotensin II receptor subtype. The binding affinity of [125I]CGP-42112 acetate is higher in the brain than in the adrenal. Beta-mercaptoethanol enhances [125I]CGP-42112 acetate binding in the brain but does not alter its binding in the adrenal.The high-affinity binding of [125I]CGP-42112 acetate (Kd = 0.07-0.3 nM, depending on the area studied) is selective for AT2 receptors. This selectivity is demonstrated by the lack of competition with the AT1 ligand losartan and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 acetate, as well as the non-selective peptides Ang II and angiotensin III (Ang III).

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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AT2 receptor, CGP-42112 acetate(127060-75-7 Free base), CGP42112acetate(127060757Freebase)
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
171360120 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 130.00
5 mg
$ 350.00
10 mg
$ 490.00
1 ml x 10 mM (in DMSO)
$ 740.00
25 mg
$ 740.00
50 mg
$ 980.00
100 mg
$ 1,270.00
200 mg
$ 1,710.00
DispatchUsually dispatched within 3-5 working days
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