Astressin 2B

目录号: GC15720纯度: >98%

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

规格	价格	库存	数量	操作
500µg	¥5,870.00	现货	1

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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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产品描述 Description

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.

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]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	A431 epidermoid cells
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. [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.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

681260-70-8

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 g/mol

溶解性

Soluble to 1 mg/ml in Water

保存条件

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°C，然后在超声波浴中震荡一段时间。

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