| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Ki: 3.52 nM (CRF receptor)[1].
CRF, bovine TFA is a potent and selective agonist of the CRF receptor (CRFR). It displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM. It shows pEC50 values of 11.16, 8.53, and 8.70 for human CRF1, human CRF2, and rat CRF2alpha, respectively. It binds with highest affinity to human CRF1. |
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| ln Vitro |
CRF, bovine is a strong agonist of the CRF receptor and has a Ki of 3.52 nM, which allows it to displace [125I-Tyr]ovine CRF[1]. The pEC50 values for rat CRF2α, human CRF1, and human CRF2 are 8.53, 8.70, and 11.16 in CRF[2]. Stress-induced release of CRF from the hypothalamic-pituitary-adrenal (HPA) axis results in the synthesis of glucocorticoids, which suppress immunological responses. CRF also contributes to inflammation. Brain microvessel endothelial cells (BMEC) are impacted by CRF in terms of their structure or function. CRF at 100 nM dramatically raises cAMP in BMEC[3].
In vitro, CRF, bovine TFA is a strong agonist of the CRF receptor. It is used to study CRF receptor subtype specificity, binding affinity, and signal transduction pathways. It activates adenylate cyclase and increases cAMP accumulation in cells expressing CRF1 or CRF2 receptors in a concentration-dependent manner. |
| ln Vivo |
CRF is released from the hypothalamic-pituitary-adrenal (HPA) axis in response to stress and leads to the production of glucocorticoids, which down-regulate immune responses. In animal models, CRF administration induces anxiety-like behaviors and activates the HPA axis, increasing plasma ACTH and corticosterone levels.
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| Enzyme Assay |
For in vitro binding assays, CRF receptor affinity is determined using radioligand displacement. Membranes from CHO cells stably expressing human CRF1 or CRF2 are incubated with 0.05 nM [125I-Tyr]ovine CRF and varying concentrations of unlabeled CRF, bovine TFA (0-1000 nM) in assay buffer (50 mM Tris-HCl, 2 mM EGTA, 5 mM MgCl2, 0.1% BSA). After 90 minutes at 25degC, bound radioactivity is measured by filtration.
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| Cell Assay |
For cell-based assays, cells expressing CRF receptors (e.g., Y-79 retinoblastoma cells or transfected HEK293 cells) are seeded in 96-well plates. Cells are treated with CRF, bovine TFA (0-1000 nM) for 15-30 minutes at 37degC. cAMP accumulation is measured using a homogeneous time-resolved fluorescence (HTRF) or a chemiluminescence-based immunoassay. EC50 values are calculated from dose-response curves.
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| Animal Protocol |
For animal studies of stress response and anxiety, male C57BL/6J mice (6-8 weeks) are anesthetized and implanted with an intracerebroventricular (i.c.v.) cannula. CRF, bovine TFA is dissolved in artificial cerebrospinal fluid (aCSF). On test day, mice receive an i.c.v. injection of CRF (0.1-1 microg). Behavior is assessed 30 minutes post-injection using the elevated plus maze (EPM) and open-field test. Plasma is collected for ACTH and corticosterone measurement.
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| ADME/Pharmacokinetics |
CRF, bovine TFA (bovine CRF) has a molecular weight of approximately 4697.34 Da. The TFA salt form enhances water solubility (1 mg/mL in water or saline). As a peptide, it is susceptible to proteolytic degradation; it should be stored lyophilized at -20degC and reconstituted immediately before use. CRF has a short half-life in vivo (minutes).
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| Toxicity/Toxicokinetics |
CRF, bovine TFA is a research-grade peptide (purity typically >98% by HPLC) intended for research use only. It is non-toxic at typical research doses. Standard precautions for handling peptides (avoid inhalation, skin contact) should be followed. High doses may cause prolonged HPA axis activation. It is not for human therapeutic use.
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| References |
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| Additional Infomation |
CRF, bovine TFA (CAS: 92307-52-3; Sequence: SQEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII-NH2) is used as a reference ligand for characterizing CRF receptor subtype specificity, binding affinity, and signal transduction. It is structurally identical to human/rat CRF except for seven amino acid substitutions. It is used in HPA axis, stress, and anxiety research.
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| Molecular Formula |
C208H341F3N60O65S
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|---|---|
| Molecular Weight |
4811.36
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| Related CAS # |
CRF, bovine;92307-52-3
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2078 mL | 1.0392 mL | 2.0784 mL | |
| 5 mM | 0.0416 mL | 0.2078 mL | 0.4157 mL | |
| 10 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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