Amunine,Also known as CRF (Ovine) Trifluoroacetate,it is a trifluoroacetate form of corticotropin releasing factor (CRF) extracted from sheep and synthesized. It usually appears white,which is a typical color in its pure state. In some cases,due to differences in preparation processes or storage conditions,the color may vary slightly,but generally remains within the range of white to off white. This substance is mostly in powder form,making it easy to store and use. In addition,it may also exist in the form of freeze-dried powder,which helps maintain its stability and activity.
Its main physiological function is to stimulate the release of adrenocorticotropic hormone (ACTH) from the anterior pituitary gland. ACTH further acts on the adrenal cortex,promoting the synthesis and release of glucocorticoids such as cortisol. This process is an important component of the hypothalamic pituitary adrenal axis (HPA axis),which is crucial for maintaining the body's stress response,energy metabolism,and immune function.
Our Products Form
Amunine COA
 |
||
| Certificate of Analysis | ||
| Compound name | CRF(Ovine)Trifluoroacetate | |
| Grade | Pharmaceutical grade | |
| CAS No. | 79804-71-0 | |
| Quantity | 15g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co.,Ltd | |
| Lot No. | 202501090026 | |
| MFG | Jan 9th 2025 | |
| EXP | Jan 8th 2028 | |
| Structure |
|
|
| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.39% |
| Loss on drying | ≤1.0% | 0.26% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.99% |
| Single impurity | <0.8% | 0.53% |
| Total microbial count | ≤750cfu/g | 99 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed,dark,and dry place below -20°C | |
|
|
||
| Chemical Formula | C205H339N59O63S |
| Exact Mass | 4667.49 |
| Molecular Weight | 4670.38 |
| M/Z | 4669.49 (100.0%),4668.49 (90.6%),4670.50 (73.1%),4667.49 (40.9%),4671.50 (39.5%),4670.49 (21.8%),4669.49 (19.8%),4672.50 (16.2%),4671.50 (12.9%),4670.49 (11.7%),4671.49 (11.3%),4668.48 (8.9%),4672.50 (5.7%),4669.49 (5.3%),4671.49 (4.6%),4671.49 (4.5%),4673.50 (4.3%),4670.48 (4.1%),4673.51 (3.9%),4672.50 (3.6%),4672.50 (3.1%),4672.50 (2.9%),4672.49 (2.3%),4669.48 (1.8%),4673.49 (1.8%),4671.49 (1.6%),4670.48 (1.3%) |
| Elemental Analysis | C,53.69; H,6.87; N,19.50; O,17.59; S,2.35 |
Amunine (CRF(Ovine)Trifluoroacetate) is a core regulatory molecule of the hypothalamic pituitary adrenal axis (HPA axis) in mammals, playing a crucial role in stress response, emotion regulation, and metabolic balance. CRF (Ovine) Trifluoroacetate, as a CRF analogue derived from sheep, has become an important tool for studying the physiological functions of the CRF system and drug development due to its high specificity and stability.
Molecular basis and chemical modification of CRF (Ovine)
Origin and structural characteristics of natural CRF
CRF was initially isolated and purified from the hypothalamus of sheep by Vale and other scientists in 1981. Its amino acid sequence is:
H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Leu-Asp-Ile-Ala-NH2
This sequence contains 41 amino acids with a molecular weight of approximately 4.7 kDa, with serine (Ser) at the N-terminus and alanine (Ala) amidation modification at the C-terminus. The amino acid homology between sheep CRF and human CRF is 95%, with only differences at positions 7, 10, 13, 16, 21, 23, 26, 28, 31, 34, and 38, but the functions are highly conserved.
Chemical significance of Trifluoroacetate modification
CRF (Ovine) Trifluoroacetate (CAS number: 79804-71-0) is a salt compound formed by combining the carboxyl end of CRF with trifluoroacetic acid (TFA). The advantages of TFA modification include:
Enhanced solubility: The strong acidic group (- COCF ∝) of TFA can increase the solubility of peptides in organic solvents, facilitating experimental operations.
Stable peptide structure: TFA reduces peptide aggregation and degradation by forming salt bridges, prolonging half-life.
Maintain biological activity: Modified CRF can still efficiently bind to CRF receptor (CRFR), retaining the functional characteristics of natural molecules.
Synthesis Method and Quality Control
CRF (Ovine) Trifluoroacetate is usually prepared by solid-phase peptide synthesis (SPPS), where the amino acid side chains are protected by Fmoc or Boc protecting groups, gradually coupled to form a linear polypeptide chain, and finally cut by TFA resin and purified. The quality control standards include:
Purity: High performance liquid chromatography (HPLC) detects a purity of ≥ 98%.
Molecular weight verification: Mass spectrometry (MS) confirms that the molecular weight is consistent with the theoretical value.
Biological activity assay: Verify its ability to stimulate the secretion of adrenocorticotropic hormone (ACTH) through in vitro cell experiments (such as AtT-20 pituitary tumor cells).
Classification and signal transduction mechanism of CRF receptors
Structure and distribution of CRF receptors
The CRF receptor belongs to the B-class G protein coupled receptor (GPCR) family, which includes two subtypes: CRF ₁ R and CRF ₂ R
CRF ₁ R: Widely distributed in the central nervous system (such as cerebral cortex, hippocampus, amygdala) and peripheral tissues (such as pituitary gland, adrenal gland, placenta).
CRF ₂ R: mainly expressed in the paraventricular nucleus of the hypothalamus, locus coeruleus, spinal cord, and peripheral tissues such as the heart, blood vessels, and gastrointestinal tract.
The homology of amino acid sequences between the two receptors reaches 70%, but there are differences in ligand binding specificity: CRF ₁ R has a higher affinity for CRF than CRF ₂ R, which tends to bind to Urocortin (UCN) family ligands.
G protein coupled signaling pathway
After binding to the receptor, CRF promotes adenylate cyclase (AC) activity by activating G α s protein, leading to an increase in intracellular adenosine monophosphate (cAMP) levels, which in turn activates protein kinase A (PKA) and downstream signaling molecules such as CREB. In addition, CRF can activate phospholipase C (PLC) through G α q protein, triggering calcium ion (Ca ² ⁺) mobilization and protein kinase C (PKC) activation.
The key signal nodes are
CAMP PKA pathway: regulates ACTH secretion, glucose metabolism, and gene expression.
Ca ² ⁺ - PKC pathway: involved in neuronal excitability regulation and synaptic plasticity.
MAPK pathway: mediates long-term adaptive responses (such as neuronal survival) through ERK1/2 phosphorylation.
Mechanisms of receptor desensitization and endocytosis
Long term exposure to CRF can lead to receptor desensitization, manifested as decreased G protein coupling efficiency and receptor phosphorylation. The desensitization of CRF ₁ R mainly relies on β - arrestin mediated endocytosis, while the endocytosis efficiency of CRF ₂ R is relatively low, which may be related to differences in receptor subcellular localization. After endocytosis, receptors can be recycled to the cell membrane or enter lysosomes for degradation, which is crucial for maintaining receptor functional homeostasis.
Pharmaceutical Industry
As a diagnostic reagent to evaluate pituitary function
Amunine is the gold standard diagnostic reagent for evaluating pituitary adrenal axis function. Its mechanism of action is as follows:
Stimulating ACTH secretion: After intravenous injection of CRF (Ovine), CRF ₁ R in the anterior pituitary gland can be rapidly activated, promoting the synthesis and release of ACTH.
Indirectly promoting cortisol secretion: ACTH enters the bloodstream and acts on the adrenal cortex, inducing cortisol secretion. By detecting changes in plasma ACTH and cortisol levels, the functional status of the pituitary and adrenal glands can be evaluated Can be used for differential diagnosis of Cushing's syndrome. Patients with Cushing's syndrome have ACTH dependent cortisol secretion, but the cause may be pituitary adenoma (Cushing's disease) or ectopic ACTH syndrome. The CRF (Ovine) stimulation test can distinguish between ACTH and cortisol by observing their response patterns.
Pituitary Cushing's disease is characterized by an enhanced response of the pituitary gland to CRF (Ovine), with significantly elevated levels of ACTH and cortisol. Ectopic ACTH syndrome refers to the secretion of ACTH by non functional pituitary adenomas or ectopic tumors, which do not respond to CRF (Ovine).Patients with primary adrenal insufficiency (such as Addison's disease) have weakened response to ACTH due to adrenal cortex destruction, and insufficient increase in cortisol levels after CRF (Ovine) stimulation; Patients with secondary adrenal insufficiency (such as pituitary lesions) have reduced ACTH secretion, leading to decreased cortisol response.
Tool compounds in drug development
The CRF system plays a crucial role in emotional disorders such as anxiety and depression, and CRF ₁ R antagonists have become a hot topic in the development of anti anxiety/depression drugs. CRF (Ovine) Trifluoroacetate is used as a tool compound for receptor binding experiments to screen high affinity CRF ₁ R antagonists and evaluate their competitive binding ability. Functional experiments were conducted to validate the inhibitory effect of antagonists on ACTH secretion induced by CRF (Ovine) in a cell model. Animal model studies use anxiety like behavior models induced by CRF (Ovine), such as elevated maze tests, to evaluate the anti anxiety effects of antagonists.
Representative drugs:
Verucerfont: Phase II clinical trials have been completed and shown to be effective in treating generalized anxiety disorder (GAD).
Pexacerfont: Used to treat depression by inhibiting CRF ₁ R to alleviate stress response.
Development of CRF2 R agonists
CRF2R plays an important role in cardiovascular protection and stress adaptation, while Amunine is used for:
Receptor selectivity research: Distinguishing the functional differences between CRF 1 R and CRF2 R to guide the design of selective agonists.
Cardiovascular disease model: In myocardial infarction models, CRF ₂ R agonists (such as UCN2) can reduce myocardial cell apoptosis and improve heart function.
Frequently Asked Questions
Why is CRF specifically sourced from "sheep" instead of human or rat sources?
+
-
Due to its unique pharmacological properties. Compared with human or rat CRF, sheep CRF (oCRF) has a stronger binding affinity to CRF receptor type 1 and a longer half-life in vivo, producing a stronger and more persistent ACTH release response, making it a standardized and more sensitive tool peptide for basic research and diagnostic testing.
What does the suffix 'trifluoroacetate' mean? Is this a common salt form in pharmaceuticals?
+
-
This is a common byproduct in the purification and preparation process of peptide compounds. Trifluoroacetic acid is an acidic mobile phase component used in the purification of peptides by high-performance liquid chromatography, which can remain in the final product and form salts. It is not an active ingredient and trace amounts are usually allowed in biological preparations.
How does it help reveal the direct connection between "stress" and "anxiety" behaviors in scientific research?
+
-
Injecting oCRF directly into specific areas of the animal brain (such as the amygdala) can bypass the endocrine system and directly activate central CRF neurons, thereby inducing typical anxiety like behaviors (such as increased alertness and reduced exploratory behavior). This provides direct causal evidence for the neural circuits that lead to anxiety caused by stress.
Besides stimulating the pituitary gland, what are its lesser known roles in the immune system?
+
-
Immune cells, such as T cells and macrophages, also express CRF receptors. OCRF can directly regulate the function of immune cells, such as inhibiting the release of inflammatory factors by macrophages and affecting lymphocyte proliferation. It is a key connecting molecule in the neuroendocrine immune network.
Why is it an ideal tool for studying the negative feedback regulation of the hypothalamic pituitary adrenal axis?
+
-
By administering exogenous and standard doses of oCRF, the HPA axis can be precisely challenged, and the release kinetics and peak values of ACTH and cortisol can be monitored. This can sensitively reflect the responsiveness of the pituitary gland to CRH and the negative feedback intensity of cortisol, used to evaluate the integrity of HPA axis function.
Hot Tags: amunine, China amunine manufacturers, suppliers, salcatonin injection, intranasal desmopressin acetate, best glp 1 peptide, biotinoyl tripeptide 1, glp1 shot, etelcalcetide structure
