Astressin |
| رقم الكتالوجGC16218 |
الأستريسين هو أحد مضادات إطلاق الكورتيكوتروبين القوية (CRF)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 170809-51-5
Sample solution is provided at 25 µL, 10mM.
Astressin is a potent corticotropin releasing factor (CRF) antagonist.
Astressin has low affinity for the CRF binding protein and high affinity (Ki=2 nM) for the cloned pituitary receptor. Astressin shows high affinity for cloned human CRF-RA1 stably expressed in CHO cells and high potency to inhibit ACTH secretion[1].
Astressin is significantly more potent than any previously tested antagonist in reducing hypophyseal corticotropin (ACTH) secretion in stressed or adrenalectomized rats. Low doses of astressin (30 μg and 100 μg per kg) administered i.v. still produce a significant decrease in ACTH levels at 45 and 90 min, respectively[1]. Astressin significantly reverses the anxiogenic-like response induced by both social stress and ICV rat/humanCRF (r/hCRF) on the elevated plus-maze, but fails to block the effects of r/hCRF-induced locomotor activity in a familiar environment[2]. Intracerebroventricular infusion of the peptide both 30 min before and 10 min after seizures decreases damage in some hippocampal cell fields by as much as 84%, a magnitude of protection greater than reported for other CRF antagonists against other models of necrotic neuronal injury. Astressin protects even if administered only 10 min following excitotoxin exposure[3].
References:
[1]. Gulyas J, et al. Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc Natl Acad Sci U S A. 1995 Nov 7;92(23):10575-9.
[2]. Spina MG, et al. Behavioral effects of central administration of the novel CRF antagonist astressin in rats. Neuropsychopharmacology. 2000 Mar;22(3):230-9.
[3]. Maecker H, et al. Astressin, a novel and potent CRF antagonist, is neuroprotective in the hippocampus when administered after a seizure. Brain Res. 1997 Jan 2;744(1):166-70.
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Animal experiment: |
Rats: Rat diet is supplemented with oranges, and their water contained 0.9% NaCl. They are equipped with indwelling jugular cannulae 48 h prior to the i.v. injection of either vehicle or astressin. Astressin is first diluted in sterile, distilled, apyrogenic water, and the pH is adjusted to 7.0. Further dilutions are made in 0.04 M phosphate buffer, pH 7.4, containing 0.1% bovine serum albumin and 0.01% ascorbic acid. Blood samples are obtained immediately before treatment, as well as 15-120 min later. Decanted plasma samples are frozen until assayed for ACTH concentrations[1]. |
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References: [1]. Gulyas J, et al. Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc Natl Acad Sci U S A. 1995 Nov 7;92(23):10575-9. |
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| Cas No. | 170809-51-5 | SDF | |
| Canonical SMILES | CCCC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@@](N)([H])CC1=CC=CC=C1)([H])CC2=CN=CN2)([H])CC(C)C)([H])CC(C)C)([H])CCCNC(N)=N)([H])CCC(O)=O)([H])C(C)C)([H])CC(C)C)([H])CCC(O)=O) | ||
| Formula | C161H269N49O42 | M.Wt | 3563.2 |
| الذوبان | Soluble to 1 mg/ml in 10% Acetic acid / sterile water | Storage | Store at -20°C,away from moisture and light, under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2806 mL | 1.4032 mL | 2.8065 mL |
| 5 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL |
| 10 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL |
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Quality Control & SDS
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- Purity: >98.50%
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