Astressin 2B
目录号 : GC15720
Astressin 2B 是促肾上腺皮质激素释放因子受体 2 (CRF2) 的选择性强效拮抗剂（IC50 值为 1.3 和 >；CRF2 和 CRF1 分别为 500 nM），可拮抗 CRF2 介导的胃排空抑制。
Cas No.:681260-70-8
Sample solution is provided at 25 µL, 10mM.
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Astressin 2B is selective and potent antagonist of corticotropin-releasing factor receptor 2 (CRF2) (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively) that antagonizes CRF2-mediated inhibition of gastric emptying.
Ach-mediated effects on cell adhesion are blocked by astressin 2b, a CRF2 antagonist, suggesting that Ach action depends partly on CRF2 signaling[4].
Astressin-2B also exacerbated the intestinal ulcerogenic response induced by indomethacin. Urocortin I prevented indomethacin-induced intestinal lesions, together with the suppression of bacterial invasion and an increase in mucosal MPO activity and iNOS expression. Urocortin I suppressed the hypermotility response to indomethacin, and this effect was also abrogated by astressin-2B[2]. In mcie, Central administration of Ucn1 increased significantly the number of entries into the chamber of the unknown male, without changing the time of interaction and this effect was blocked by astressin2B[1]. NmU, a potent endogenous anorectic, serves as a catabolic signaling molecule in the brain. For an investigation of the possible role of receptors in mediating hyperthermia, the animals were treated with astressin 2B, a CRH2 receptor antagonist. NmU increased the colon temperature, maximal action being observed at 2-3h[3].
References:
[1]. Bagosi Z, Karasz G, et,al. The effects of CRF and urocortins on the sociability of mice. Brain Res. 2017 May 15;1663:114-122. doi: 10.1016/j.brainres.2017.03.003. Epub 2017 Mar 14. PMID: 28315311.
[2]. Kubo Y, Kumano A, et,al. Urocortin prevents indomethacin-induced small intestinal lesions in rats through activation of CRF2 receptors. Dig Dis Sci. 2010 Jun;55(6):1570-80. doi: 10.1007/s10620-009-0930-1. Epub 2009 Aug 26. PMID: 19707872.
[3]. Telegdy G, Adamik A. Mediators involved in the hyperthermic action of neuromedin U in rats. Regul Pept. 2014 Jun-Aug;192-193:24-9. doi: 10.1016/j.regpep.2014.07.004. Epub 2014 Aug 7. PMID: 25108055.
[4]. Pelissier-Rota M, Chartier NT, et,al. A crosstalk between muscarinic and CRF2 receptors regulates cellular adhesion properties of human colon cancer cells. Biochim Biophys Acta Mol Cell Res. 2017 Jul;1864(7):1246-1259. doi: 10.1016/j.bbamcr.2017.04.008. Epub 2017 Apr 18. PMID: 28432022.
Astressin 2B 是促肾上腺皮质激素释放因子受体 2 (CRF2) 的选择性强效拮抗剂（IC50 值为 1.3 和 >；CRF2 和 CRF1 分别为 500 nM），可拮抗 CRF2 介导的胃排空抑制。
Ach 介导的细胞粘附作用被 CRF2 拮抗剂 astressin 2b 阻断，表明 Ach 作用部分取决于 CRF2 信号[4]。
Astressin-2B 还加剧了吲哚美辛诱导的肠道溃疡反应。 Urocortin I 可预防吲哚美辛引起的肠道损伤，同时抑制细菌入侵并增加粘膜 MPO 活性和 iNOS 表达。 Urocortin I 抑制对吲哚美辛的过度运动反应，并且这种作用也被 astressin-2B[2] 消除。在 mcie 中，Ucn1 的中央管理显着增加了未知男性进入腔室的次数，而没有改变相互作用的时间，并且这种作用被 astressin2B[1] 阻断。 NmU 是一种有效的内源性厌食剂，在大脑中充当分解代谢信号分子。为了研究受体在介导体温过高中的可能作用，动物接受了 astressin 2B（一种 CRH2 受体拮抗剂）治疗。 NmU 增加结肠温度，在 2-3 小时观察到最大作用[3]。
| Cell experiment [1]: | |
|
Cell lines |
A431 epidermoid cells |
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Preparation Method |
cells were pretreated overnight with Astressin 2b (1 µM). Non-adherent cells were removed by washing three times with PBS, and cell adhesion was estimated by a colorimetric cell proliferation assay. |
|
Reaction Conditions |
Astressin 2b (1 µM) overnight |
|
Applications |
Ach-mediated effects on cell adhesion are blocked by astressin 2b, a CRF2 antagonist, suggesting that Ach action depends partly on CRF2 signaling. |
| Animal experiment [2]: | |
|
Animal models |
Male Sprague-Dawley rats (240-280 g) |
|
Preparation Method |
The animals were administered indomethacin and killed 24 h later under deep ether anesthesia. Ucn I (a CRFR1 and CRFR2 agonist: 2 20 µg/kg) or astressin (a nonselective CRFR antagonist: 50 µg/kg) was given i.v. 10 min before the administration of indomethacin. NBI-27914 or astressin 2B (60 µg/kg) was given i.v. 10 min before the administration of Ucn I or indomethacin. |
|
Dosage form |
60 µg/kg astressin 2B |
|
Applications |
Astressin 2B also exacerbated the intestinal ulcerogenic response induced by indomethacin. Urocortin I prevented indomethacin-induced intestinal lesions, together with the suppression of bacterial invasion and an increase in mucosal MPO activity and iNOS expression. Urocortin I suppressed the hypermotility response to indomethacin, and this effect was also abrogated by astressin-2B. |
|
References: [1]. Pelissier-Rota M, Chartier NT,et,al. A crosstalk between muscarinic and CRF2 receptors regulates cellular adhesion properties of human colon cancer cells. Biochim Biophys Acta Mol Cell Res. 2017 Jul;1864(7):1246-1259. doi: 10.1016/j.bbamcr.2017.04.008. Epub 2017 Apr 18. PMID: 28432022. | |
| Cas No. | 681260-70-8 | SDF | |
| Canonical SMILES | CCCC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](CC(C)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)([H])CC(O)=O)([H])CC(C)C)([H])CO)([H])CC1=CC=CC=C1)([H])CC2=CN=CN2)C)([H])CC(C)C)([H])CCCNC(N)=N)([H])CCCCN)( | ||
| 分子式 | C183H307N49O53 | 分子量 | 4041.69 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Store at -20°C |
| 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 | 0.2474 mL | 1.2371 mL | 2.4742 mL |
| 5 mM | 0.0495 mL | 0.2474 mL | 0.4948 mL |
| 10 mM | 0.0247 mL | 0.1237 mL | 0.2474 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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