| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
IC50: 1 nM (CRLR/RAMP1, cell assay), 300 nM (CRLR/RAMP2, cell assay)[1]
β-CGRP, human TFA acts via the complex of calcitonin receptor-like receptor (CRLR) and receptor activity-modifying proteins (RAMPs). It has IC50 values of 1 nM for CRLR/RAMP1 and 300 nM for CRLR/RAMP2 in cells. As a potent vasodilatory neuropeptide, β-CGRP plays critical roles in cardiovascular regulation, nociception, and migraine pathophysiology. |
|---|---|
| ln Vitro |
Human β-CGRP is a calcitonin peptide that functions via a complex of calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein (RAMP) with an IC50 of 1 nM. NG108-15 and HEK293T cells that express CRLR and RAMP2 express 130 nM and 300 nM, respectively [1]. SK-N-MC and Swiss 3T3 cells both express CRLR and RAMP1, and SK-N-MC and Swiss 3T3 cells express both CRLR and RAMP1 [1]. In addition to being a strong vasodilator, CGRP has anti- and pro-inflammatory properties [2].
In vitro studies have characterized β-CGRP, human TFA as a calcitonin peptide that acts through the CRLR/RAMP receptor complex. In cell-based assays, the peptide shows IC50 values of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2, respectively. These in vitro activities demonstrate the peptide's potent receptor activation capabilities and its utility in studying CGRP receptor pharmacology. |
| ln Vivo |
In vivo activity of β-CGRP has been extensively studied in animal models. As a potent vasodilator, β-CGRP induces vasodilation and modulates cardiovascular function in vivo. The peptide is involved in pain transmission and has been implicated in migraine pathophysiology. In animal studies, β-CGRP is typically administered via intravenous or other routes to study its effects on blood pressure, vascular tone, and nociceptive responses. Dosing regimens vary depending on the specific study objectives.
|
| Enzyme Assay |
For non-cellular assays, β-CGRP, human TFA is characterized by standard analytical techniques including HPLC and mass spectrometry to confirm identity and purity. The peptide can be evaluated in receptor binding assays using membrane preparations expressing CRLR/RAMP complexes. Typical protocols involve incubating the peptide with receptor preparations and measuring binding affinity or receptor activation. The peptide is supplied as a solid and should be stored under appropriate conditions.
|
| Cell Assay |
For in vitro cell-based studies, β-CGRP, human TFA is dissolved in appropriate buffers and diluted in cell culture medium to working concentrations. Cells expressing CRLR/RAMP receptors are treated with the peptide to assess receptor activation, signaling pathway activation, or downstream functional responses. The peptide shows IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells. Appropriate controls should be included in the experimental design.
|
| Animal Protocol |
For in vivo animal studies, β-CGRP, human TFA is typically administered via intravenous injection or other routes depending on the study design. The peptide is used to study vasodilation, cardiovascular function, pain transmission, and migraine mechanisms in animal models. Dosing solutions should be freshly prepared using appropriate vehicles. Dosing regimens and administration protocols follow approved animal welfare guidelines and institutional protocols.
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| ADME/Pharmacokinetics |
β-CGRP, human TFA has a molecular weight of 3907.38 and molecular formula C164H268F3N51O50S3. It is supplied as a solid and should be stored under appropriate conditions. The peptide is the human beta isoform of calcitonin gene-related peptide supplied as the trifluoroacetate salt. The compound is stable under recommended storage conditions. Solubility: soluble in aqueous buffers and appropriate solvents.
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| Toxicity/Toxicokinetics |
β-CGRP, human TFA is for research use only and not for therapeutic or diagnostic use. Standard laboratory safety practices should be followed when handling this peptide. Appropriate personal protective equipment including gloves and safety glasses should be worn. Specific toxicological profiles have not been extensively reported for research-grade peptide preparations.
|
| References | |
| Additional Infomation |
β-CGRP, human TFA (CAS not assigned) is also known as Human β-CGRP TFA and CGRP-II (Human) (TFA). It is a calcitonin peptide that functions via a complex of calcitonin receptor-like receptor (CRLR) and receptor activity-modifying proteins (RAMPs). The peptide is used in research studying vasodilation, cardiovascular function, pain pathways, and migraine. No clinical or therapeutic approvals exist for this research-grade peptide.
|
| Molecular Formula |
C164H268F3N51O50S3
|
|---|---|
| Molecular Weight |
3907.38
|
| Appearance |
Typically exists as solid at room temperature
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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)
|
| Solubility (In Vitro) |
H2O :~100 mg/mL (~25.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (12.80 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2559 mL | 1.2796 mL | 2.5593 mL | |
| 5 mM | 0.0512 mL | 0.2559 mL | 0.5119 mL | |
| 10 mM | 0.0256 mL | 0.1280 mL | 0.2559 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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