Astressin
目录号 : GC16218
Astressin 是一种有效的促肾上腺皮质激素释放因子 (CRF) 拮抗剂。
Cas No.:170809-51-5
Sample solution is provided at 25 µL, 10mM.
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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) | ||
| 分子式 | C161H269N49O42 | 分子量 | 3563.2 |
| 溶解度 | Soluble to 1 mg/ml in 10% Acetic acid / sterile water | 储存条件 | Store at -20°C,away from moisture and light, under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet