2. GPCR/G Protein
  3. CRFR
  4. Astressin 2B

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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Astressin 2B

Astressin 2B Chemical Structure

CAS No. : 681260-70-8

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Based on 1 publication(s) in Google Scholar

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Astressin 2B Related Antibodies

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1 Publications Citing Use of MCE Astressin 2B

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Description

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[1][2][3][4][5][6][7].
IC50 & Target

CRFR2

 

In Vitro

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.

Astressin 2B Related Antibodies

Cell Viability Assay[5]

Cell Line: Mouse tracheal smooth muscle
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 15 min; followed by Methacholine treatment for 30 min
Result: Concentration-dependent inhibited Urocortin III (HY-P1858)-mediated tracheal smooth muscle relaxation.
In Vivo

Astressin 2B (3-100 μg/kg; intraperitoneal injection, subcutaneous injection) dose-dependently and completely reverses urocortin-induced delayed gastric emptying in mice, and exerts this effect at a dose of 10 μg/kg (i.p.)[1].
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.

Animal Model: CRF2 receptor wild-type (C57BL/6 × 129 mixed background) mice[3]
Dosage: 24 pmol; 96 pmol; 192 pmol
Administration: i.c., bilateral lateral septal infusion; single dose 10 minutes before urocortin 2
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.
Clinical Trial
Molecular Weight

4041.69

Formula

C183H307N49O53
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

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
Sequence Shortening

Ac-DLS-{d-Phe}-H-{a-methyl-Leu}-LRK-{Nle}-IEIEKQEKEKQQA-cyclo(ENNK)-LLLD-{a-methyl-Leu}-I-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (0.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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Astressin 2B Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Astressin 2B681260-70-8CRFRCorticotropin-releasing Factor ReceptorCRHRCRF2 receptorCRF1 receptorurocortin 2indomethacin-induced small intestinal hemorrhagic lesionsmouseurocortin ICHO-K1 cell membraneshumanratA7r5 cell homogenatesInhibitorinhibitorinhibit

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