| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
alpha-CGRP (mouse, rat) primarily targets the calcitonin receptor-like receptor (CLR) in complex with receptor activity-modifying protein 1 (RAMP1) to form the functional CGRP receptor. This GPCR couples to Galphas, leading to adenylyl cyclase activation, increased cAMP, and PKA activation. In rodents, CGRP receptors are found on vascular smooth muscle, endothelial cells, sensory neurons, and various other tissues, mediating vasodilation, pain transmission, and neurogenic inflammation.
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| ln Vitro |
In vitro, alpha-CGRP (mouse, rat) TFA is a highly potent vasodilator. It is a full agonist at the rodent CGRP receptor with an EC50 typically in the low nanomolar range for cAMP accumulation. The peptide induces relaxation of pre-contracted isolated blood vessels, including the rat aorta and mesenteric arteries, in a concentration-dependent manner. It also relaxes colonic smooth muscle, demonstrating its broad effects on smooth muscle tone. These properties make it useful for studying vascular function ex vivo.
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| ln Vivo |
In a dosage-dependent way, α-CGRP (mouse, rat) TFA (<0.1 mL; supra-aortic injection, single dose) raises heart rate [1].
In vivo, alpha-CGRP (mouse, rat) TFA is a potent vasodilator in rodents. Peripheral administration leads to a rapid fall in blood pressure and an increase in heart rate in a dose-dependent manner. Administered as a bolus injection above the aorta in volumes less than 0.1 mL, it increases heart rate dose-dependently. CGRP also relaxes colonic smooth muscle in vivo and mediates neurogenic vasodilation in models of inflammation and migraine. It is used as a positive control in pharmacological studies of vascular tone. |
| Enzyme Assay |
For in vitro receptor binding assays, membrane preparations from rat brain (specifically cerebellum or spinal cord) are incubated with [125I]-labeled rat alpha-CGRP (0.05-0.1 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 0.1% BSA) with increasing concentrations of unlabeled alpha-CGRP (0.001-1000 nM). After 90-120 minutes at room temperature, bound radioligand is separated by filtration through GF/B filters pre-treated with 0.3% PEI. The radioactivity is counted to calculate Ki or IC50 values. The assay is used to determine receptor binding affinity.
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| Cell Assay |
For functional cell-based assays, cells expressing rodent CGRP receptors (e.g., SK-N-MC neuroblastoma cells or rodent brain membrane preparations) are incubated with alpha-CGRP (mouse, rat) TFA in a cAMP assay buffer. After 30 minutes at 37degC, the reaction is terminated, and cAMP accumulation is measured using a competitive ELISA or a BRET-based biosensor. The EC50 is determined from a dose-response curve (typically 0.1-100 nM). Data are normalized to a maximum response induced by a saturating concentration of CGRP (e.g., 1 uM).
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[1]
Doses: <0.1 mL Route of Administration: Injected above the dosage aorta, single Experimental Results: Increased heart rate in a dose dependent fashion. For in vivo studies in rats or mice, alpha-CGRP (mouse, rat) TFA is dissolved in sterile saline containing 0.1% BSA and administered via intravenous injection (tail vein) at doses ranging from 0.1 to 10 ug/kg. To measure blood pressure changes, animals are anesthetized (e.g., with isoflurane or pentobarbital), and a catheter is inserted into the carotid artery or femoral artery connected to a pressure transducer. Heart rate is recorded simultaneously. For conscious animal studies, telemetry implants are used. Blood pressure and heart rate are monitored for at least 30 minutes post-injection. Control animals receive vehicle (saline + 0.1% BSA). |
| ADME/Pharmacokinetics |
As a 37-amino acid peptide (molecular weight ~3920 Da), alpha-CGRP (mouse, rat) TFA has a short half-life in circulation due to rapid degradation by neutral endopeptidase (NEP). In rodents, the plasma half-life is typically 2-10 minutes after intravenous administration. The peptide is not orally bioavailable. It is typically stored as a lyophilized powder at -20degC and reconstituted in aqueous buffers containing a carrier protein (e.g., 0.1% BSA) to prevent adsorption to surfaces. For in vivo use, solutions should be freshly prepared.
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| Toxicity/Toxicokinetics |
Toxicological data for alpha-CGRP (mouse, rat) TFA are limited to acute exposure studies. At the low doses used for vasodilation studies (≤10 ug/kg iv), no overt toxicity is observed. At very high doses (e.g., >100 ug/kg), prolonged hypotension may lead to reflex tachycardia and potential cardiovascular stress. No chronic toxicity studies have been published. Standard safety precautions for handling peptides should be followed.
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| References |
[1]. Holman JJ, et al. Human alpha- and beta-CGRP and rat alpha-CGRP are coronary vasodilators in the rat. Peptides. 1986 Mar-Apr;7(2):231-5.
[2]. Arulmani U, et al. Effects of the calcitonin gene-related peptide (CGRP) receptor antagonist BIBN4096BS on alpha-CGRP-induced regional haemodynamic changes in anaesthetised rats. Basic Clin Pharmacol Toxicol. 2004 Jun;94(6):291-7. [3]. Gorzi A, et al. Muscle gene expression of CGRP-α, CGRP receptor, nAchR-β, and GDNF in response to different endurance training protocols of Wistar rats. Mol Biol Rep. 2020 Jul;47(7):5305-5314. |
| Additional Infomation |
alpha-CGRP (mouse, rat) TFA is a research-grade peptide and is not approved for clinical use. Its amino acid sequence is SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF-NH2 with a disulfide bridge between Cys2 and Cys7, and a molecular weight of 3920.27. The free base CAS number is 83651-90-5. This peptide is widely used in cardiovascular, migraine, and metabolic research. Store at -20degC as a lyophilized powder, protected from moisture.
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| Molecular Formula |
C162H262N50O52S2.C2HF3O2
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| Molecular Weight |
3920.27
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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) |
H2O :~25 mg/mL (~6.38 mM)
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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 | 0.2551 mL | 1.2754 mL | 2.5508 mL | |
| 5 mM | 0.0510 mL | 0.2551 mL | 0.5102 mL | |
| 10 mM | 0.0255 mL | 0.1275 mL | 0.2551 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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