Bioactivity | Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying[1][2][3]. | ||||||
Name | Astressin 2B TFA | ||||||
Sequence | Ac-Asp-Leu-Ser-{d-Phe}-His-{a-methyl-Leu}-Leu-Arg-Lys-{Nle}-Ile-Glu-Ile-Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala-{g-Glu}-Asn-Asn-Leu-Leu-Leu-Asp-{a-methyl-Leu}-Ile-NH2 (Lactam bridge: Glu24-Lys27) | ||||||
Shortening | Ac-Asp-LS-{d-Phe}-H-{a-methyl-Leu}-LRK-{Nle}-IEIEKQEKEKQQA-{g-Glu}-NNKLLLD-{a-methyl-Leu}-I-NH2 (Lactam bridge:Glu24-Lys27) | ||||||
Formula | C183H307N49O53.xC2HF3O2 | ||||||
Molar Mass | 4041.69 (free base) | ||||||
Appearance | 固体 | ||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||
Storage | Sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
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Reference | [1]. Rivier J, et al. Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J Med Chem. 2002;45(21):4737-4747. [2]. Hoare SR, et al. Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF2 receptor selectivity. Peptides. 2005;26(3):457-470. [3]. Henry B, et al. The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J Neurosci. 2006;26(36):9142-9152. |