Astressin 2B

Name: Astressin 2B
Brand: GlpBio
SKU: GC15720
Availability: InStock
Rating: 5 (20 reviews)

カタログ番号GC15720

アストレッシン2Bは、コルチコトロピン放出因子受容体2（CRF2）の選択的かつ強力な拮抗剤であり（IC50値は、CRF2が1.3nMである一方、CRF1が> 500 nMです）、胃排出を妨げるCRF2介在性の阻害を拮抗します。

Products are for research use only. Not for human use. We do not sell to patients.

Astressin 2B 化学構造

Cas No.: 681260-70-8

サイズ

価格

在庫数

個数

500µg

$576.00

在庫あり

Tel：(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.

評判の良い論文で引用されたGlpBio製品

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

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.

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.

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)(
Formula	C₁₈₃H₃₀₇N₄₉O₅₃	M.Wt	4041.69
溶解度	Soluble to 1 mg/ml in Water	Storage	Store at -20°C
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.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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Astressin 2B

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

評判の良い論文で引用されたGlpBio製品

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

レビュー

Astressin 2B

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

評判の良い論文で引用されたGlpBio製品

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

Related Products

レビュー