Astressin 2B
Based on 1 publication(s) in Google Scholar
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
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- 純度: 97.81%
- CAS 番号: 681260-70-8
- 分子式: C183H307N49O53
- 分子量:4041.69
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Astressin 2B
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生物活性
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CRFR2 |
Astressin 2B potently binds to CRF2 receptors in rat choroid plexus and blood vessels (IC50=0.57 nM)[1].
Astressin 2B binds to the cloned human CRF2 (a) receptor expressed in CHO-K1 cell membranes with extremely high affinity (Ki=0.49 nM)[2].
Astressin 2B binds to endogenous rat CRF2 (b) receptors in A7r5 cell homogenates with extremely high affinity (Ki=0.17 nM)[2].
Astressin 2B (1-100 nM; 15 min) concentration-dependently inhibits Urocortin III (HY-P1858)-mediated relaxation of tracheal smooth muscle in in vitro relaxation assays of methacholine (HY-A0083)-precontracted mouse tracheal smooth muscle, with an IC50 of approximately 3 nM[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse tracheal smooth muscle
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:15 min; followed by Methacholine treatment for 30 min
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Result:Concentration-dependent inhibited Urocortin III (HY-P1858)-mediated tracheal smooth muscle relaxation.
Following septal administration of Astressin 2B (24-192 pmol; bilateral septal perfusion) TFA, doses of 24 pmol and 96 pmol block the stress-dependent anxiogenic effect of septal urocortin 2, whereas the 192 pmol dose reduces stress-induced anxiety in both vehicle-treated and urocortin 2-treated mice[3].
Astressin 2B (60 μg/kg; intravenous injection) reverses the CRFR2-mediated protective effects of Ucn I, including attenuation of injury, inhibition of MPO activity, reduction of intestinal bacterial invasion, downregulation of iNOS expression, and alleviation of intestinal hypermotility[4].
Astressin 2B (60 μg/kg; intravenous injection; administered 10 minutes prior to exposure; single dose) exacerbates Indomethacin (HY-14397)-induced small intestinal injury, and completely reverses all the protective effects mediated by Urocortin I (HY-P1858) against Indomethacin-induced intestinal injury, inflammation, bacterial invasion and hyperdynamic state, confirming that these protective effects are mediated via CRFR2[6].
Astressin 2B (3-300 μg/kg; i.p.; administered 30 min prior to exposure; single dose) dose-dependently reduces intestinal fluid secretion, and inhibits neutrophil infiltration, MPO activity and production of proinflammatory chemokines in a mouse model of intestinal inflammation induced by Clostridium difficile toxin A[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CRF2 receptor wild-type (C57BL/6 × 129 mixed background) mice[3]
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Dosage:24 pmol; 96 pmol; 192 pmol
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Administration:i.c., bilateral lateral septal infusion; single dose 10 minutes before urocortin 2
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Result:Blocked the anxiogenic effects of 48 pmol urocortin 2 in high-stress condition at 24 and 96 pmol: significantly decreased latency to enter the light side of the light-dark box, increased time spent in the light side of the light-dark box, and increased percentage time spent in the center of the novel-object test.
Increased percentage time spent in the center of the open field in urocortin 2-treated mice under high-stress condition at 24 pmol.
Reduced anxiety-related behavior in both urocortin 2-treated and vehicle-treated stressed mice at 192 pmol: decreased latency to enter the light side of the light-dark box, increased time spent in the light side of the light-dark box, increased percentage time spent in the center of the open field, and increased percentage time spent in the center of the novel-object test.
Showed no significant effect on anxiety-related behavior in no-stress condition at any dose tested, and no dose altered locomotor activity in either stress condition.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Ac-Asp-Leu-Ser-{d-Phe}-His-{a-methyl-Leu}-Leu-Arg-Lys-{Nle}-Ile-Glu-Ile-Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala-cyclo(Glu-Asn-Asn-Lys)-Leu-Leu-Leu-Asp-{a-methyl-Leu}-Ile-NH2
Ac-DLS-{d-Phe}-H-{a-methyl-Leu}-LRK-{Nle}-IEIEKQEKEKQQA-cyclo(ENNK)-LLLD-{a-methyl-Leu}-I-NH2
化学情報
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CAS 番号 681260-70-8
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性状 Solid
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分子量 4041.69
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分子式 C183H307N49O53
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Color White to off-white
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Neuron
Astrocyte-mediated central amygdala microcircuit gates comorbid anxiety symptoms in chronic pain. [Abstract]2025 Oct 2:S0896-6273(25)00670-1. PMID: 41043420
溶剤 & 溶解度
DMSO : 100 mg/mL (24.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (296 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rivier J, et al. Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J Med Chem. 2002;45(21):4737-4747. [Content Brief]
[2]. Hoare SR, et al. Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF2 receptor selectivity. Peptides. 2005;26(3):457-470. [Content Brief]
[3]. Henry B, et al. The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J Neurosci. 2006;26(36):9142-9152. [Content Brief]
[4]. Kubo Y, et al. Urocortin prevents indomethacin-induced small intestinal lesions in rats through activation of CRF2 receptors. Dig Dis Sci. 2010;55(6):1570-1580. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2474 mL | 1.2371 mL | 2.4742 mL | 6.1855 mL |
| 5 mM | 0.0495 mL | 0.2474 mL | 0.4948 mL | 1.2371 mL | |
| 10 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6186 mL | |
| 15 mM | 0.0165 mL | 0.0825 mL | 0.1649 mL | 0.4124 mL | |
| 20 mM | 0.0124 mL | 0.0619 mL | 0.1237 mL | 0.3093 mL |
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