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Synonyms: Astressin acetate (170809-51-5 Free base)
| Description | Astressin acetate is an antagonist of corticotropin releasing factor (CRF) with low affinity for the CRF binding protein and high affinity for the cloned pituitary receptor(Ki = 2 nM). |
| In vitro | Astressin acetate exhibits high affinity for cloned human CRF-RA1 stably expressed in CHO cells and high potency to inhibit ACTH secretion[2]. |
| In vivo | Astressin acetate (i.c.v. 30 min before and 10 min after seizures) decreases damage in some hippocampal cell fields by as much as 84%. Astressin acetate protects even if administered only 10 min following excitotoxin exposure[1]. Astressin acetate is significantly more potent than any previously tested antagonist in reducing hypophyseal corticotropin secretion in stressed or adrenalectomized rats. Astressin acetate (30 and 100 μg/kg; i.v.) produces a significant decrease in ACTH levels at 45 and 90 min, respectively[2]. Astressin acetate significantly reverses the anxiogenic-like response induced by both social stress and i.c.v. rat/humanCRF (r/hCRF) on the elevated plus-maze, but fails to block the effects of r/hCRF-induced locomotor activity in a familiar environment[3]. |
| Synonyms | Astressin acetate (170809-51-5 Free base) |
| Molecular Weight | 3623.21 |
| Formula | C163H273N49O44 |
| Smiles | CC(O)=O.O=C(O)CC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](N)CC1=CC=CC=C1)=O)CC2=CNC=N2)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N)=O)CCC(O)=O)=O)C(C)C)=O)CC(C)C)=O)CCC(O)=O)=O)CCCC)=O)C)=O)CCCNC(N)=N)=O)C)=O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC3)C(N[C@@H](C)C(N[C@@H](CC4=CNC=N4)C(N[C@H](C(N[C@@H](CC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CCCC)C(N[C@@H](CCC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCCCNC3=O)=O)=O)=O)=O)=O)=O)=O)=O |
| Sequence | {D-Phe}-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-His-Lys-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile (Bridge:Glu19-Lys22) |
| Sequence Short | FHLLREVLEXARAEQLAQEAHKNRKLXEII |
| Storage | Store at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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