Antisauvagine-30Potent, selective and competitive CRF2 antagonist CAS# 220673-95-0 |
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| Cas No. | 220673-95-0 | SDF | Download SDF |
| PubChem ID | 90471086 | Appearance | Powder |
| Formula | C161H274N48O46S | M.Wt | 3650.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | [D-Phe<sup>11</sup>,His<sup>12</sup>]-Sauvagine (11-40) | ||
| Solubility | Soluble to 1 mg/ml in water | ||
| Sequence | FHLLRKMIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, Ile-30 = C-terminal amide) | ||
| SMILES | CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(C)C(=O)NC(C)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)NC(C(C)O)C(=O)NC(C(C)CC)C(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(C(C)CC)NC(=O)C(CCSC)NC(=O)C(CCCCN)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC=N1)NC(=O)C(CC2=CC=CC=C2)N | ||
| Standard InChIKey | JDWSXVUWDQFRCE-JBNJRNGTSA-N | ||
| Standard InChI | InChI=1S/C161H273N47O47S/c1-21-84(14)126(205-145(240)105(51-58-124(221)222)195-157(252)127(85(15)22-2)206-146(241)106(59-66-256-20)193-137(232)96(42-30-34-63-165)182-138(233)97(43-35-64-177-160(172)173)186-147(242)107(67-79(4)5)199-150(245)110(70-82(10)11)202-152(247)112(73-91-77-176-78-179-91)197-132(227)92(166)72-90-37-25-24-26-38-90)156(251)194-104(50-57-123(219)220)144(239)185-94(40-28-32-61-163)135(230)190-101(47-54-118(169)212)141(236)192-103(49-56-122(217)218)143(238)184-95(41-29-33-62-164)136(231)191-102(48-55-121(215)216)142(237)183-93(39-27-31-60-162)134(229)189-100(46-53-117(168)211)140(235)188-99(45-52-116(167)210)133(228)181-87(17)130(225)180-88(18)131(226)196-113(74-119(170)213)154(249)203-114(75-120(171)214)153(248)187-98(44-36-65-178-161(174)175)139(234)198-108(68-80(6)7)148(243)200-109(69-81(8)9)149(244)201-111(71-83(12)13)151(246)204-115(76-125(223)224)155(250)208-129(89(19)209)158(253)207-128(159(254)255)86(16)23-3/h24-26,37-38,77-89,92-115,126-129,209H,21-23,27-36,39-76,162-166H2,1-20H3,(H2,167,210)(H2,168,211)(H2,169,212)(H2,170,213)(H2,171,214)(H,176,179)(H,180,225)(H,181,228)(H,182,233)(H,183,237)(H,184,238)(H,185,239)(H,186,242)(H,187,248)(H,188,235)(H,189,229)(H,190,230)(H,191,231)(H,192,236)(H,193,232)(H,194,251)(H,195,252)(H,196,226)(H,197,227)(H,198,234)(H,199,245)(H,200,243)(H,201,244)(H,202,247)(H,203,249)(H,204,246)(H,205,240)(H,206,241)(H,207,253)(H,208,250)(H,215,216)(H,217,218)(H,219,220)(H,221,222)(H,223,224)(H,254,255)(H4,172,173,177)(H4,174,175,178)/t84-,85-,86-,87-,88-,89+,92+,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,126-,127-,128-,129-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells (pA2 = 8.49). Prevents stress-enhanced fear conditioning and MEK 1/2-dependent activation of ERK1/2 in mice in vivo. |
Antisauvagine-30 Dilution Calculator
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Anxiolytic-like effects of antisauvagine-30 in mice are not mediated by CRF2 receptors.[Pubmed:24015170]
PLoS One. 2013 Aug 28;8(8):e63942.
The role of brain corticotropin-releasing factor type 2 (CRF2) receptors in behavioral stress responses remains controversial. Conflicting findings suggest pro-stress, anti-stress or no effects of impeding CRF2 signaling. Previous studies have used Antisauvagine-30 as a selective CRF2 antagonist. The present study tested the hypotheses that 1) potential anxiolytic-like actions of intracerebroventricular (i.c.v.) administration of Antisauvagine-30 also are present in mice lacking CRF2 receptors and 2) potential anxiolytic-like effects of Antisauvagine-30 are not shared by the more selective CRF2 antagonist astressin2-B. Cannulated, male CRF2 receptor knockout (n = 22) and wildtype littermate mice (n = 21) backcrossed onto a C57BL/6J genetic background were tested in the marble burying, elevated plus-maze, and shock-induced freezing tests following pretreatment (i.c.v.) with vehicle, Antisauvagine-30 or astressin2-B. Antisauvagine-30 reduced shock-induced freezing equally in wildtype and CRF2 knockout mice. In contrast, neither astressin2-B nor CRF2 genotype influenced shock-induced freezing. Neither CRF antagonist nor CRF2 genotype influenced anxiety-like behavior in the plus-maze or marble burying tests. A literature review showed that the typical Antisauvagine-30 concentration infused in previous intracranial studies ( approximately 1 mM) was 3 orders greater than its IC50 to block CRF1-mediated cAMP responses and 4 orders greater than its binding constants (Kd , Ki ) for CRF1 receptors. Thus, increasing, previously used doses of Antisauvagine-30 also exert non-CRF2-mediated effects, perhaps via CRF1. The results do not support the hypothesis that brain CRF2 receptors tonically promote anxiogenic-like behavior. Utilization of CRF2 antagonists, such as astressin2-B, at doses that are more subtype-selective, can better clarify the significance of brain CRF2 systems in stress-related behavior.
Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): development of CRFR2beta-selective antisauvagine-30.[Pubmed:9860957]
Proc Natl Acad Sci U S A. 1998 Dec 22;95(26):15264-9.
Different truncated and conformationally constrained analogs of corticotropin-releasing factor (CRF) were synthesized on the basis of the amino acid sequences of human/rat CRF (h/rCRF), ovine CRF (oCRF), rat urocortin (rUcn), or sauvagine (Svg) and tested for their ability to displace [125I-Tyr0]oCRF or [125I-Tyr0]Svg from membrane homogenates of human embryonic kidney (HEK) 293 cells stably transfected with cDNA coding for rat CRF receptor, type 1 (rCRFR1), or mouse CRF receptor, type 2beta (mCRFR2beta). Furthermore, the potency of CRF antagonists to inhibit oCRF- or Svg-stimulated cAMP production of transfected HEK 293 cells expressing either rCRFR1 (HEK-rCRFR1 cells) or mCRFR2beta (HEK-mCRFR2beta cells) was determined. In comparison with astressin, which exhibited a similar affinity to rCRFR1 (Kd = 5.7 +/- 1.6 nM) and mCRFR2beta (Kd = 4.0 +/- 2.3 nM), [DPhe11,His12]Svg(11-40), [DLeu11]Svg(11-40), [DPhe11]Svg(11-40), and Svg(11-40) bound, respectively, with a 110-, 80-, 68-, and 54-fold higher affinity to mCRFR2beta than to rCRFR1. The truncated analogs of rUcn displayed modest preference (2- to 7-fold) for binding to mCRFR2beta. In agreement with the results of these binding experiments, [DPhe11, His12]Svg(11-40), named Antisauvagine-30, was the most potent and selective ligand to suppress agonist-induced adenylate cyclase activity in HEK cells expressing mCRFR2beta.
125I-Antisauvagine-30: a novel and specific high-affinity radioligand for the characterization of corticotropin-releasing factor type 2 receptors.[Pubmed:11077077]
Neuropharmacology. 2001;40(1):114-22.
Corticotropin-releasing factor (CRF) receptors type 1 (CRF(1)) and type 2 (CRF(2)) differ from each other in their pharmacological properties. The human and ovine CRF versions bind to CRF(1) receptors with significantly higher affinity than to CRF(2) receptors. Recently Antisauvagine-30, an N-terminally truncated version of the CRF analog sauvagine, was characterized as a specific antagonist to mouse CRF(2B). We have synthesized the radiolabeled version (125)I-Antisauvagine-30 and tested it for its affinity at human CRF(1) (hCRF(1)), hCRF(2A), Xenopus CRF(1) (xCRF(1)) and xCRF(2) receptors. In control binding studies (125)I-labeled hCRF, sauvagine and astressin were also bound to these receptors. (125)I-Antisauvagine-30 exclusively bound to hCRF(2A) and xCRF(2) but not to hCRF(1) and xCRF(1) receptors. (125)I-Antisauvagine-30 binding to hCRF(2A) and xCRF(2) receptors was saturable and of high affinity (hCRF(2A): K(d)=125 pM; xCRF(2): K(d)=1.1 nM). In displacement binding experiments using (125)I-Antisauvagine-30 as radioligand several CRF analogs bound to hCRF(2A) and xCRF(2) receptors with similar rank orders as reported with other CRF radioligands. Finally, preliminary studies using (125)I-Antisauvagine-30 binding to membrane homogenates prepared from different rat brain structures showed that the peptide bound specifically to brain areas expressing CRF(2) receptors. These data demonstrate that (125)I-Antisauvagine-30 is the first high-affinity ligand to specifically label CRF(2) receptors.
Pharmacological and chemical properties of astressin, antisauvagine-30 and alpha-helCRF: significance for behavioral experiments.[Pubmed:11543771]
Neuropharmacology. 2001 Sep;41(4):507-16.
Corticotropin releasing factor (CRF) represents an early chemical signal in the stress response and modulates various brain functions through G protein-coupled receptors. Two CRF receptor subtypes, CRF(1) and CRF(2), have been identified. Since the physicochemical properties of CRF receptor antagonists might influence their biological potency, the peptidic antagonists astressin, alpha-helical CRF(9-41) (alpha-helCRF) and Antisauvagine-30 (aSvg-30) have been analyzed. The rank order of solubility of these compounds in artificial cerebrospinal fluid (aCSF, pH 7.4) was aSvg-30>alpha-helCRF>>astressin, whereas the rank order of relative lipophilicity as determined with RP-HPLC was alpha-helCRF>astressin>aSvg-30. The calculated isoelectric points were 4.1 (alpha-helCRF), 7.4 (astressin) and 10.0 (aSvg-30). According to Schild analysis of the CRF receptor-dependent cAMP production of transfected HEK cells, aSvg-30 exhibited a competitive antagonism and displayed a 340 fold selectivity for mCRF(2 beta) receptor. For astressin, however, the pharmacodynamic profile could not be explained by a simple competitive mechanism as indicated by Schild slopes >1 for rCRF(1) or mCRF(2 beta) receptor. Behavioral experiments demonstrated that after i.c.v. injection, alpha-helCRF reduced oCRF-induced anxiety-like behavior in the elevated plus-maze, whereas astressin, despite its higher in vitro potency, did not. These findings could be explained by different physicochemical properties of the antagonists employed.
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.[Pubmed:14673008]
J Neurosci. 2003 Dec 10;23(36):11436-43.
A coordinated activation of multiple interlinked signaling pathways involving cAMP-dependent protein kinase (PKA) and mitogen-activated extracellular signal-regulated kinases (Mek-1/2) regulates gene expression and neuronal changes underlying memory consolidation. In the present study we investigated whether these molecular cascades might mediate the effects of stress on memory formation. We also investigated the role of hippocampal corticotropin-releasing factor receptor 2 (CRF2) in stress-enhanced learning and molecular signaling mediated by PKA, Mek-1/2, and their downstream targets extracellularly regulated kinases 1 and 2 (Erk-1/2) and p90-ribosomal-s-kinase-1 (p90Rsk-1). Acute 1 hr immobilization was used as a stressful stimulus, and one-trial context-dependent fear conditioning was used as a model for associative learning. Training of BALB/c mice 3 hr after the end of immobilization resulted in an enhancement of conditioned fear, as indicated by significantly increased freezing behavior of stressed when compared with nonstressed mice. Interestingly, Erk-1/2 phosphorylation after conditioning of nonstressed and stressed mice depended on PKA and Mek-1/2, respectively. Intrahippocampal injection of the selective Mek-1/2 inhibitor U0126 or CRF2 antagonist Antisauvagine-30 (aSvg-30) prevented stress-enhanced fear conditioning and Mek-1/2-dependent activation of Erk-1/2 and p90Rsk-1. aSvg-30 did not affect the phosphorylation of the PKA regulatory subunit II of stressed mice. The molecular and behavioral effects of CRF2 coincided with stress-induced upregulation of CRF2 mRNA. These results suggest that modulation of Mek-1/2-dependent signaling by hippocampal CRF2 can be selectively involved in the delayed effects of stress on memory consolidation.
