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

Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA 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 TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.

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Astressin 2B TFA

Astressin 2B TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of Astressin 2B TFA:

Astressin 2B TFA Related Antibodies

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1 Publications Citing Use of MCE Astressin 2B TFA

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Description

Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA 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 TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA 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 TFA potently binds to CRF2 receptors in rat choroid plexus and blood vessels (IC50=0.57 nM)[1].
Astressin 2B TFA 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 TFA binds to endogenous rat CRF2 (b) receptors in A7r5 cell homogenates with extremely high affinity (Ki=0.17 nM)[2].
Astressin 2B TFA (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 TFA 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) TFA 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) TFA 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) TFA 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) TFA 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.
Molecular Weight

4041.69 (free base)

Formula

C183H307N49O53.xC2HF3O2
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 and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

  • Molarity Calculator

  • Dilution Calculator

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

Concentration (start)

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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; 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 and light)

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

Purity: 99.54%

SDS (252 KB)

COA (248 KB) RP-HPLC (255 KB) MS (193 KB)

Handling Instructions (2659 KB)
References
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Astressin 2B TFA 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 2BCRFRCorticotropin-releasing Factor ReceptorCRHRsmall intestinal protective effectsClostridium difficile toxin Aratsintestinal epithelial damageileal tissueurocortin ICRHR2-deficient mouseCRFR2indomethacin-induced damageblood-brain barrierInhibitorinhibitorinhibit

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