Astressin TFA

Modify Date: 2024-01-02 12:51:50

Astressin TFA Structure
Astressin TFA structure
Common Name Astressin TFA
CAS Number 170809-51-5 Molecular Weight 3563.16000
Density N/A Boiling Point N/A
Molecular Formula C161H269N49O42 Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of Astressin TFA


Astressin is a potent corticotropin releasing factor (CRF) antagonist.

 Names

Name astressin
Synonym More Synonyms

 Astressin TFA Biological Activity

Description Astressin is a potent corticotropin releasing factor (CRF) antagonist.
Related Catalog
In Vitro Astressin has low affinity for the CRF binding protein and high affinity (Ki=2 nM) for the cloned pituitary receptor. Astressin shows high affinity for cloned human CRF-RA1 stably expressed in CHO cells and high potency to inhibit ACTH secretion[1].
In Vivo Astressin is significantly more potent than any previously tested antagonist in reducing hypophyseal corticotropin (ACTH) secretion in stressed or adrenalectomized rats. Low doses of astressin (30 μg and 100 μg per kg) administered i.v. still produce a significant decrease in ACTH levels at 45 and 90 min, respectively[1]. Astressin significantly reverses the anxiogenic-like response induced by both social stress and ICV 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[2]. Intracerebroventricular infusion of the peptide both 30 min before and 10 min after seizures decreases damage in some hippocampal cell fields by as much as 84%, a magnitude of protection greater than reported for other CRF antagonists against other models of necrotic neuronal injury. Astressin protects even if administered only 10 min following excitotoxin exposure[3].
Animal Admin Rats: Rat diet is supplemented with oranges, and their water contained 0.9% NaCl. They are equipped with indwelling jugular cannulae 48 h prior to the i.v. injection of either vehicle or astressin. Astressin is first diluted in sterile, distilled, apyrogenic water, and the pH is adjusted to 7.0. Further dilutions are made in 0.04 M phosphate buffer, pH 7.4, containing 0.1% bovine serum albumin and 0.01% ascorbic acid. Blood samples are obtained immediately before treatment, as well as 15-120 min later. Decanted plasma samples are frozen until assayed for ACTH concentrations[1].
References

[1]. Gulyas J, et al. Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc Natl Acad Sci U S A. 1995 Nov 7;92(23):10575-9.

[2]. Spina MG, et al. Behavioral effects of central administration of the novel CRF antagonist astressin in rats. Neuropsychopharmacology. 2000 Mar;22(3):230-9.

[3]. Maecker H, et al. Astressin, a novel and potent CRF antagonist, is neuroprotective in the hippocampus when administered after a seizure. Brain Res. 1997 Jan 2;744(1):166-70.

 Chemical & Physical Properties

Molecular Formula C161H269N49O42
Molecular Weight 3563.16000
Exact Mass 3561.04000
PSA 1489.66000
LogP 9.58910
Storage condition 2-8℃

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport

 Articles31

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Acute systemic stress disrupts reproductive function by inhibiting pulsatile gonadotropin secretion. The underlying mechanism involves stress-induced suppression of the GnRH pulse generator, the funct...

Corticotropin-releasing hormone and the sympathoadrenal system are major mediators in the effects of peripherally administered exendin-4 on the hypothalamic-pituitary-adrenal axis of male rats.

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Glucagon-like peptide-1 (GLP-1) and the GLP-1 receptor agonist, exendin-4 (Ex-4), potently stimulate hypothalamic-pituitary-adrenal (HPA) axis activity after either central or peripheral administratio...

Social stress and CRF-dopamine interactions in the VTA: role in long-term escalation of cocaine self-administration.

J. Neurosci. 34(19) , 6659-67, (2014)

The nature of neuroadaptations in the genesis of escalated cocaine taking remains a topic of considerable interest. Intermittent social defeat stress induces both locomotor and dopaminergic cross-sens...

 Synonyms

Astressin
M.W. 3563.24 C161H269N49O42
[D-Phe12,Nle21,38,Glu30
ASTRESSIN TRIFLUOROACETATE SALT
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