Antisauvagine-30 is a potent, selective and competitive corticotropin-releasing factor CRF₂ receptor antagonist (K_d values are 1.4 and 153.6 nM for binding to mouse CRF_2β and rat CRF₁ receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF_2β cells (pA₂ = 8.49). Prevents stress-enhanced fear conditioning and MEK 1/2-dependent activation of ERK1/2 in mice in vivo.

Licensing Information

Sold with the permission of the Max Planck Institute

Product Specifications

Molecular Weight

3650.29

Formula

C₁₆₁H₂₇₄N₄₈O₄₆S

Storage

Desiccate at -20°C

CAS Number

220673-95-0

PubChem ID

16138449

InChI Key

INBLUEDNNZCTNZ-JBNJRNGTSA-N

SMILES

[H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCSC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Soluble to 1mg/ml in water

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Background References

References are publications that support the biological activity of the product.

Sananbenesi Mitogen-activated protein kinase signaling in the hippocampus and its modulation by corticotropin-releasing factor receptor 2: a possible link between stress and fear memory. J.Neurosci. 2003 PMID: 14673008
Ruhmann Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): development of CRFR2β-selective antisauvagine-30. Proc.Natl.Acad.Sci.USA
Brauns Pharmacological and chemical properties of astressin, antisauvagine-30 and α-helCRF: significance for behavioral experiments. Neuropharmacology 2001 PMID: 11543771

Antisauvagine-30

Tocris Bioscience, part of Bio-Techne | Catalog # 2071

Key Product Details

Description

Alternative Names

View all CRF2 Receptor Antagonists »

Product Description