| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CGRP II rat TFA targets the CGRP receptor, which is a complex of the calcitonin receptor-like receptor (CRLR) and receptor activity-modifying protein 1 (RAMP1). Activation of this receptor leads to vasodilation and is involved in neurotransmission. The peptide also binds to other CGRP receptor complexes (CRLR/RAMP2 and CRLR/RAMP3) with different affinities (IC₅0 of 1 nM and 300 nM, respectively). It functions as a potent vasodilator in cardiovascular research.
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| ln Vitro |
With an EC50 value of 0.56 nM, rat TFA containing calcitonin gene related protein (CGRP) II causes vasodilator effects in small-diameter pig left anterior descending (LAD) coronary arteries[1]. Rat TFA, calcitonin Gene Related Peptide (CGRP) II, has an EC50 value of 83 μM and relaxes the spontaneous tone in isolated internal anal sphincter (IAS) strips[2]. Calcitonin Gene Related Peptide (CGRP) II, rat TFA (rβCGRP), in cells co-expressing mRAMP1 (mouse receptor-activity-modifying protein 1) and rCRLR (rat calcitonin receptor-like receptor), reduces [125I]hαCGRP binding (IC50: 7 nM) and promotes cAMP buildup (EC50: 0.56 nM)[3]. With an approximate IC50 value of 2.8 nM, calcitonin gene related protein II, rat TFA (rat-βCGRP, 0.01-100 nM) causes endothelium-independent relaxations in the coronary arteries of both male and female Sprague-Dawley rats[4].
In vitro, CGRP II rat TFA functions as a potent CGRP receptor activator. It induces vasodilation in isolated blood vessel preparations, such as rat aorta or mesenteric arteries, in a concentration-dependent manner. It also stimulates cAMP production in cells expressing the CGRP receptor (CRLR/RAMP1) and has been shown to be a potent inducer of oedema in rat orofacial tissue at concentrations of 8-33 pM. These activities confirm its role as a potent vasodilator. |
| ln Vivo |
In male Sprague-Dawley rats, a bolus injection of 0.3 μg/kg of rat-βCGRP (calcitonin gene-related peptide) at 10-minute intervals causes vasodilatation and hypotension[5].
In vivo, CGRP II rat TFA is a potent and long-lasting vasodilator used in the research of cardiovascular diseases. Administration in animal models results in decreased blood pressure and increased blood flow in various vascular beds due to CGRP receptor activation. It is a potent inducer of oedema in rat orofacial tissue, with a rapidly developing (5-15 min) and long-lasting (6 h) dose-dependent effect. These activities are central to its research applications. |
| Enzyme Assay |
Binding of CGRP II rat TFA to CGRP receptors is assessed using radioligand binding assays on membrane preparations from cells expressing recombinant human or rat CRLR/RAMP1, CRLR/RAMP2, or CRLR/RAMP3. Various concentrations of the peptide are incubated with a labeled CGRP tracer (e.g., [¹2⁵I]-CGRP) in a binding buffer. After incubation, bound and free radioligands are separated by filtration, and radioactivity is measured. IC₅0 values (1 nM for CRLR/RAMP1, 300 nM for CRLR/RAMP2) are calculated.
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| Cell Assay |
Cellular assays are performed using cells expressing the CGRP receptor complex, such as SK-N-MC neuroblastoma cells (which endogenously express CGRP receptors). Cells are treated with various concentrations of CGRP II rat TFA for 10-30 minutes. The primary functional endpoint is the measurement of intracellular cAMP accumulation using a competitive ELISA or a FRET-based biosensor, as CGRP receptors couple to Gs proteins leading to adenylate cyclase activation and cAMP production. The EC₅0 for cAMP stimulation is calculated.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[5]
Doses: 0.01 ng/kg-3 μg/kg (100 μL), succeeded by a 150 μL isotonic saline flush, at 10 min intervals. Route of Administration: A bolus injection Experimental Results: Induced PA (pial artery) dilatation and increased in LCBFFlux (local cortical cerebral blood flow). In vivo animal studies are conducted to evaluate the vasodilator and oedema-inducing effects of CGRP II rat TFA. For vasodilation studies, anesthetized rats are administered the peptide via intravenous injection at doses ranging from 0.1 to 10 microg/kg, and changes in mean arterial pressure (MAP) are recorded. For oedema studies, CGRP II rat TFA (100 microL, 8-33 pM) is injected intradermally into the rat cheek, and oedema formation is measured by assessing tissue swelling at 5-15 min, 30 min, 1 h, 2 h, 4 h, and 6 h post-injection. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for CGRP II rat TFA are not detailed in standard product literature. As a 37-amino acid neuropeptide, its PK profile is characteristic of endogenous peptides, with a relatively short half-life in circulation (minutes) due to rapid proteolytic degradation by peptidases and clearance via CGRP receptors. It is not orally bioavailable and is typically administered via intravenous or intraperitoneal routes in research settings. The TFA salt form enhances solubility for in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CGRP II rat TFA are not provided in standard product literature. As an endogenous neuropeptide, it is generally well-tolerated at physiological concentrations. At research-use doses, no specific toxicities have been reported. For laboratory use, standard chemical safety precautions for handling peptides should be followed. Because it is a potent vasodilator, systemic administration may cause significant hypotension, which should be considered when designing experiments.
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| References |
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| Additional Infomation |
CGRP II rat TFA (alpha-CGRP, rat TFA) has a purity of 97.04%. The peptide sequence contains 37 amino acids and includes a disulfide bridge. It appears as a solid powder. The compound is stored at -20degC or -80degC, sealed, and away from moisture. It is soluble in water and aqueous buffers. CGRP is known as one of the most potent vasodilators identified. The product is for research use only and not for human therapy.
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| Molecular Formula |
C165H268F3N51O52S2
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|---|---|
| Molecular Weight |
3919.33
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| Exact Mass |
3917.932
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| Related CAS # |
Calcitonin Gene Related Peptide (CGRP) II, rat;99889-63-1
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| PubChem CID |
172639685
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
59
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| Hydrogen Bond Acceptor Count |
63
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| Rotatable Bond Count |
113
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| Heavy Atom Count |
273
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| Complexity |
9120
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| Defined Atom Stereocenter Count |
37
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| SMILES |
C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)[C@@H](C)O)CC(=O)N)NC(=O)[C@H](CO)N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](C(C)C)C(=O)N4CCC[C@H]4C(=O)N[C@@H]([C@@H](C)O)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](CC5=CC=CC=C5)C(=O)N)[C@@H](C)O.C(=O)(C(F)(F)F)O
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| InChi Key |
HCQYCJWEBKBRAU-BCJPXGLLSA-N
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| InChi Code |
InChI=1S/C163H267N51O50S2.C2HF3O2/c1-73(2)51-97(186-116(227)64-179-130(233)81(17)183-139(242)98(52-74(3)4)193-137(240)94(43-34-48-176-162(171)172)188-142(245)101(56-90-61-175-72-182-90)199-159(262)128(87(23)222)213-156(259)123(79(13)14)207-151(254)110-71-266-265-70-109(203-133(236)91(166)66-215)150(253)197-103(58-113(168)224)147(250)211-125(84(20)219)157(260)185-83(19)132(235)210-126(85(21)220)160(263)204-110)140(243)194-99(53-75(5)6)141(244)202-108(69-218)149(252)190-95(44-35-49-177-163(173)174)138(241)201-106(67-216)134(237)180-62-115(226)178-63-118(229)205-121(77(9)10)155(258)208-122(78(11)12)154(257)191-93(42-31-33-47-165)136(239)198-105(60-119(230)231)144(247)196-102(57-112(167)223)143(246)195-100(55-89-39-28-25-29-40-89)145(248)209-124(80(15)16)161(264)214-50-36-45-111(214)152(255)212-127(86(22)221)158(261)200-104(59-114(169)225)146(249)206-120(76(7)8)153(256)181-65-117(228)187-107(68-217)148(251)189-92(41-30-32-46-164)135(238)184-82(18)131(234)192-96(129(170)232)54-88-37-26-24-27-38-88;3-2(4,5)1(6)7/h24-29,37-40,61,72-87,91-111,120-128,215-222H,30-36,41-60,62-71,164-166H2,1-23H3,(H2,167,223)(H2,168,224)(H2,169,225)(H2,170,232)(H,175,182)(H,178,226)(H,179,233)(H,180,237)(H,181,256)(H,183,242)(H,184,238)(H,185,260)(H,186,227)(H,187,228)(H,188,245)(H,189,251)(H,190,252)(H,191,257)(H,192,234)(H,193,240)(H,194,243)(H,195,246)(H,196,247)(H,197,253)(H,198,239)(H,199,262)(H,200,261)(H,201,241)(H,202,244)(H,203,236)(H,204,263)(H,205,229)(H,206,249)(H,207,254)(H,208,258)(H,209,248)(H,210,235)(H,211,250)(H,212,255)(H,213,259)(H,230,231)(H4,171,172,176)(H4,173,174,177);(H,6,7)/t81-,82-,83-,84+,85+,86+,87+,91-,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)-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]-3-[[(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]-4-oxobutanoic acid;2,2,2-trifluoroacetic 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 :~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 | 1.2757 mL | 2.5515 mL | |
| 5 mM | 0.0510 mL | 0.2551 mL | 0.5103 mL | |
| 10 mM | 0.0255 mL | 0.1276 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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