| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| 500mg |
| Targets |
Calcitonin gene-related peptide (CGRP) receptor. Alpha-CGRP acts as a potent agonist at the CGRP receptor, which is a G protein-coupled receptor widely distributed in the nervous and cardiovascular systems.
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|---|---|
| ln Vitro |
Alpha-CGRP (mouse, rat) functions as a potent vasodilator in vitro. It induces concentration-dependent relaxation of isolated blood vessels and colonic smooth muscle. The peptide also stimulates adenylyl cyclase activity in target cells, leading to increased cyclic AMP production. It exhibits anti-inflammatory and nociceptive-modulating properties in various cell-based assays.
|
| ln Vivo |
In a dose-dependent manner, α-CGRP (mouse, rat) (<0.1 mL; supra-aortic injection, single dose) raises heart rate [1].
In vivo, alpha-CGRP (mouse, rat) causes a fall in blood pressure and an increase in heart rate upon peripheral administration. It functions as an appetite suppressant and contributes to gastric acid secretion. The peptide has been studied in animal models of migraine, cardiovascular disease, and inflammatory conditions. |
| Enzyme Assay |
CGRP receptor binding assays are performed using membrane preparations from tissues expressing the CGRP receptor (e.g., SK-N-MC cells or rat brain membranes). Radiolabeled [¹2⁵I]-alpha-CGRP is used as a tracer, and competition binding experiments are conducted with increasing concentrations of unlabeled alpha-CGRP to determine binding affinity (IC₅0 or Kᵢ values). Non-specific binding is determined in the presence of excess unlabeled peptide.
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| Cell Assay |
Alpha-CGRP activity is assessed in cell lines expressing the CGRP receptor, such as SK-N-MC or NIH-3T3 cells transfected with the receptor. Cells are treated with alpha-CGRP, and downstream signaling is measured by cAMP accumulation using ELISA or radioimmunoassay. Receptor internalization and calcium mobilization can also be monitored. Dose-response curves are generated to calculate EC₅0 values for receptor activation.
|
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [1]
Doses: <0.1 mL Route of Administration: Supraaortic injection, single dose Experimental Results: Heart rate increased in a dose-dependent manner. Animal studies utilize rodent models (rats or mice) to evaluate the cardiovascular and neurological effects of alpha-CGRP. The peptide is administered via intravenous, intraperitoneal, or subcutaneous injection. Blood pressure, heart rate, and regional blood flow are monitored. In migraine models, alpha-CGRP is used to induce migraine-like symptoms. Behavioral and physiological responses are recorded. |
| ADME/Pharmacokinetics |
Alpha-CGRP (mouse, rat) has a molecular weight of 3806.25 and a molecular formula of C1₆2H2₆2N₅0O₅2S2. It is a peptide with a disulfide bridge between Cys2 and Cys7. As a peptide, it is typically administered parenterally and has a short half-life in circulation due to rapid degradation by peptidases.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for alpha-CGRP in standard toxicology studies. As a naturally occurring peptide and research compound, it is not intended for human therapeutic use. At pharmacological doses, it can cause significant hemodynamic changes including hypotension and tachycardia.
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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) has the sequence SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF-NH2. It is a CGRP receptor agonist and a potent vasodilator. It is used in research on migraine, cardiovascular disease, inflammation, and metabolism. The compound is for research use only and has not been approved for clinical use.
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| Molecular Formula |
C162H262N50O52S2
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|---|---|
| Molecular Weight |
3806.24751329422
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| Exact Mass |
3804.886
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| CAS # |
83651-90-5
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| Related CAS # |
β-CGRP (mouse); α-CGRP (mouse, rat) TFA
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| PubChem CID |
90479760
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| Sequence |
Ser-Cys-Asn-Thr-Ala-Thr-Cys-Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asp-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Glu-Ala-Phe-NH2 (Disulfide bridge:Cys2-Cys7)SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF-NH2 (Disulfide bridge:Cys2-Cys7)
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| SequenceShortening |
SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF-NH2 (Disulfide bridge:Cys2-Cys7)
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| Appearance |
White to off-white solid powder
|
| LogP |
-17.7
|
| Hydrogen Bond Donor Count |
58
|
| Hydrogen Bond Acceptor Count |
59
|
| Rotatable Bond Count |
112
|
| Heavy Atom Count |
266
|
| Complexity |
9110
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| Defined Atom Stereocenter Count |
37
|
| SMILES |
S1C[C@@H](C(N[C@H](C(N[C@@H]([C@@H](C)O)C(N[C@@H](CC2=CNC=N2)C(N[C@H](C(N[C@H](C(N[C@@H](C)C(NCC(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@H](C(N[C@@H](CO)C(NCC(NCC(N[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC(=O)O)C(N[C@@H](CC(N)=O)C(N[C@@H](CC2C=CC=CC=2)C(N[C@@H](C(C)C)C(N2CCC[C@H]2C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC2C=CC=CC=2)=O)C)=O)CCC(=O)O)=O)CO)=O)=O)C(C)C)=O)CC(N)=O)=O)[C@@H](C)O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCCNC(=N)N)=O)=O)CC(C)C)=O)CC(C)C)=O)=O)=O)CC(C)C)=O)CCCNC(=N)N)=O)=O)=O)C(C)C)=O)NC([C@H]([C@@H](C)O)NC([C@H](C)NC([C@H]([C@@H](C)O)NC([C@H](CC(N)=O)NC([C@H](CS1)NC([C@H](CO)N)=O)=O)=O)=O)=O)=O
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| InChi Key |
SVAGNGUJZNLSEY-TYNJZYKVSA-N
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| InChi Code |
InChI=1S/C162H262N50O52S2/c1-71(2)49-95(184-114(225)62-177-129(233)79(17)181-138(242)96(50-72(3)4)191-136(240)91(40-32-46-174-161(169)170)186-141(245)99(54-88-59-173-70-180-88)197-158(262)127(85(23)220)211-155(259)122(77(13)14)205-150(254)108-69-266-265-68-107(201-132(236)89(164)64-213)149(253)195-101(56-111(166)222)146(250)209-124(82(20)217)156(260)183-81(19)131(235)208-125(83(21)218)159(263)202-108)139(243)192-97(51-73(5)6)140(244)200-106(67-216)148(252)187-92(41-33-47-175-162(171)172)137(241)199-104(65-214)133(237)178-60-113(224)176-61-116(227)203-120(75(9)10)154(258)206-121(76(11)12)153(257)189-90(39-30-31-45-163)135(239)196-103(58-118(230)231)143(247)194-100(55-110(165)221)142(246)193-98(53-87-37-28-25-29-38-87)144(248)207-123(78(15)16)160(264)212-48-34-42-109(212)151(255)210-126(84(22)219)157(261)198-102(57-112(167)223)145(249)204-119(74(7)8)152(256)179-63-115(226)185-105(66-215)147(251)188-93(43-44-117(228)229)134(238)182-80(18)130(234)190-94(128(168)232)52-86-35-26-24-27-36-86/h24-29,35-38,59,70-85,89-109,119-127,213-220H,30-34,39-58,60-69,163-164H2,1-23H3,(H2,165,221)(H2,166,222)(H2,167,223)(H2,168,232)(H,173,180)(H,176,224)(H,177,233)(H,178,237)(H,179,256)(H,181,242)(H,182,238)(H,183,260)(H,184,225)(H,185,226)(H,186,245)(H,187,252)(H,188,251)(H,189,257)(H,190,234)(H,191,240)(H,192,243)(H,193,246)(H,194,247)(H,195,253)(H,196,239)(H,197,262)(H,198,261)(H,199,241)(H,200,244)(H,201,236)(H,202,263)(H,203,227)(H,204,249)(H,205,254)(H,206,258)(H,207,248)(H,208,235)(H,209,250)(H,210,255)(H,211,259)(H,228,229)(H,230,231)(H4,169,170,174)(H4,171,172,175)/t79-,80-,81-,82+,83+,84+,85+,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,119-,120-,121-,122-,123-,124-,125-,126-,127-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(4R,7S,10S,13S,16S,19R)-19-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-16-(2-amino-2-oxoethyl)-7,13-bis[(1R)-1-hydroxyethyl]-10-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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: ≥ 100 mg/mL (~26.3 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 | 0.2627 mL | 1.3136 mL | 2.6273 mL | |
| 5 mM | 0.0525 mL | 0.2627 mL | 0.5255 mL | |
| 10 mM | 0.0263 mL | 0.1314 mL | 0.2627 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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