| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
alpha-CGRP targets calcitonin gene-related peptide receptors, specifically the CGRP receptor composed of calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 1 (RAMP1). It also binds to the amylin 1 (AMY1) receptor with lower affinity. CGRP receptors are G protein-coupled receptors (GPCRs) that mediate vasodilation, pain signaling, and neurogenic inflammation. CGRP is a key mediator in migraine pathophysiology.
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| ln Vitro |
In vitro, alpha-CGRP is used in receptor binding and functional assays to study CGRP receptor pharmacology. The peptide activates CGRP receptors, leading to cAMP accumulation, vasodilation, and activation of signaling pathways such as PKA and CREB. It is used in calcium mobilization and cAMP assays in cells expressing CGRP receptors. The peptide is also used to study CGRP-induced vasodilation in isolated blood vessel preparations. CGRP receptor antagonists can be screened using this peptide.
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| ln Vivo |
In vivo, alpha-CGRP is a potent vasodilator and is used to study cardiovascular regulation, migraine pathophysiology, and neurogenic inflammation. In animal models, CGRP administration induces vasodilation, lowers blood pressure, and triggers migraine-like symptoms. The peptide is used to study the efficacy of CGRP receptor antagonists and monoclonal antibodies for migraine treatment. CGRP is also involved in pain transmission and is studied in models of inflammatory pain.
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| Enzyme Assay |
In vitro receptor binding assays for alpha-CGRP involve incubating the peptide with membrane preparations expressing CGRP receptors (CLR/RAMP1). Radiolabeled CGRP (e.g., 125I-CGRP) is used as a tracer. Competition binding experiments determine binding affinity (IC50, Ki) for CGRP receptors. Saturation binding experiments determine receptor density (Bmax) and Kd. Assays are performed in buffer systems at physiological pH with protease inhibitors.
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| Cell Assay |
In vitro cell-based assays for alpha-CGRP use cells expressing CGRP receptors, such as SK-N-MC neuroblastoma cells or transfected HEK-293 cells. Cells are treated with the peptide at various concentrations. Functional responses measured include cAMP accumulation (ELISA or HTRF), calcium mobilization (Fluo-4 or Fura-2), or ERK phosphorylation. Dose-response curves determine EC50 values. CGRP receptor antagonists are evaluated by their ability to block CGRP-induced responses.
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| Animal Protocol |
In vivo animal studies for alpha-CGRP use rodent models for migraine and cardiovascular research. The peptide is administered via intravenous or subcutaneous injection. Vasodilation is assessed by measuring blood flow (laser Doppler) or blood pressure. Migraine-like symptoms (e.g., facial allodynia) are evaluated in rodent models. CGRP-induced neurogenic inflammation is assessed by plasma extravasation (Evans blue dye). The peptide is also used to study the efficacy of CGRP-targeting therapeutics.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of alpha-CGRP are typical of neuropeptides. As a 37-amino acid peptide, it has a short half-life in circulation due to rapid degradation by peptidases. CGRP is produced endogenously and acts locally at sites of release. For research applications, the peptide is typically administered by injection. Detailed PK parameters require experimental determination. The peptide is for research use only.
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| Toxicity/Toxicokinetics |
Toxicity data for alpha-CGRP are limited as it is a research peptide. CGRP is an endogenous neuropeptide with well-characterized physiological functions. At high doses, it may cause hypotension, flushing, and other vasodilatory effects. The peptide is for research use only and not for human therapeutic use without appropriate regulatory approvals. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
alpha-CGRP (human) is a 37-amino acid neuropeptide and a potent vasodilator involved in migraine pathophysiology, pain transmission, and neurogenic inflammation. It is a key target for migraine therapeutics, including CGRP receptor antagonists and monoclonal antibodies. alpha-CGRP is used as a research tool to study CGRP receptor pharmacology, migraine mechanisms, and cardiovascular regulation. It is for research use only and not for human therapeutic or diagnostic use.
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| Molecular Formula |
C163H267N51O49S2
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|---|---|
| Exact Mass |
3789.96
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| CAS # |
90954-53-3
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| PubChem CID |
16132372
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| Appearance |
White to off-white solid powder
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| LogP |
-15.7
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| Hydrogen Bond Donor Count |
59
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| Hydrogen Bond Acceptor Count |
57
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| Rotatable Bond Count |
124
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| Heavy Atom Count |
265
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| Complexity |
8970
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| Defined Atom Stereocenter Count |
37
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C(C)C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CS)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)O
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| InChi Key |
DNKYDHSONDSTNJ-XJVRLEFXSA-N
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| InChi Code |
InChI=1S/C163H269N51O49S2/c1-73(2)52-97(186-116(226)65-179-131(233)82(18)183-139(241)98(53-74(3)4)193-137(239)94(44-35-49-176-162(171)172)188-142(244)101(57-91-62-175-72-182-91)199-159(261)128(88(24)221)213-156(258)123(79(13)14)207-151(253)110(71-265)204-160(262)126(86(22)219)210-133(235)84(20)185-157(259)125(85(21)218)211-147(249)105(61-119(229)230)198-150(252)109(70-264)203-130(232)81(17)166)140(242)194-99(54-75(5)6)141(243)202-108(69-217)149(251)190-95(45-36-50-177-163(173)174)138(240)201-106(67-215)134(236)180-63-115(225)178-64-118(228)205-121(77(9)10)155(257)208-122(78(11)12)154(256)191-93(43-32-34-48-165)136(238)196-102(58-112(167)222)144(246)197-103(59-113(168)223)143(245)195-100(56-90-40-29-26-30-41-90)145(247)209-124(80(15)16)161(263)214-51-37-46-111(214)152(254)212-127(87(23)220)158(260)200-104(60-114(169)224)146(248)206-120(76(7)8)153(255)181-66-117(227)187-107(68-216)148(250)189-92(42-31-33-47-164)135(237)184-83(19)132(234)192-96(129(170)231)55-89-38-27-25-28-39-89/h25-30,38-41,62,72-88,92-111,120-128,215-221,264-265H,31-37,42-61,63-71,164-166H2,1-24H3,(H2,167,222)(H2,168,223)(H2,169,224)(H2,170,231)(H,175,182)(H,178,225)(H,179,233)(H,180,236)(H,181,255)(H,183,241)(H,184,237)(H,185,259)(H,186,226)(H,187,227)(H,188,244)(H,189,250)(H,190,251)(H,191,256)(H,192,234)(H,193,239)(H,194,242)(H,195,245)(H,196,238)(H,197,246)(H,198,252)(H,199,261)(H,200,260)(H,201,240)(H,202,243)(H,203,232)(H,204,262)(H,205,228)(H,206,248)(H,207,253)(H,208,257)(H,209,247)(H,210,235)(H,211,249)(H,212,254)(H,213,258)(H,229,230)(H4,171,172,176)(H4,173,174,177)/t81-,82-,83-,84-,85+,86+,87+,88+,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,120-,121-,122-,123-,124-,125-,126-,127-,128-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-[[(2R)-2-[[(2S)-2-aminopropanoyl]amino]-3-sulfanylpropanoyl]amino]-4-oxobutanoic 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 : ~10 mg/mL (~2.64 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.) |
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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