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CGP-42112 acetate

Catalog No. T14939L

Synonyms: CGP-42112 acetate(127060-75-7 Free base）

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CGP-42112 acetate, CAS N/A

Pack Size	Availability	Price/USD
1 mg	In stock	$ 127.00
5 mg	In stock	$ 443.00
10 mg	In stock	$ 639.00
25 mg	In stock	$ 992.00
50 mg	In stock	$ 1,330.00
100 mg	In stock	$ 1,780.00
1 mL * 10 mM (in DMSO)	In stock	$ 987.00

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Purity: 99.92%

Purity: 99.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.
Targets&IC50	AT2 receptor:0.07-0.3 nM (Kd)
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[1].[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[2].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)[3].
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[4].

Synonyms	CGP-42112 acetate(127060-75-7 Free base）
Molecular Weight	1112.24
Formula	C54H73N13O13

Storage

store at low temperature,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. Heemskerk FM, et al. Quantitative autoradiography of angiotensin II AT2 receptors with [125I]CGP 42112. Brain Res. 1995 Apr 17;677(1):29-38. 4. 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.

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Keywords

CGP-42112 acetate Endocrinology/Hormones RAAS CGP-42112 acetate(127060-75-7 Free base） CGP42112acetate(127060757Freebase） inhibitor inhibit

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