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| Targets |
The primary target of Rat CGRP-(8-37) is the calcitonin gene-related peptide (CGRP) receptor, specifically the CGRP1 receptor subtype. CGRP receptors are G protein-coupled receptors (GPCRs) composed of a calcitonin receptor-like receptor (CLR) and a receptor activity-modifying protein 1 (RAMP1). CGRP is a 37-amino acid neuropeptide that is widely distributed in the central and peripheral nervous systems. It acts as a potent vasodilator and plays a key role in the transmission of pain signals, particularly in the trigeminovascular system, which is implicated in the pathophysiology of migraine. By binding to the CGRP receptor, CGRP activates adenylate cyclase, leading to an increase in intracellular cAMP levels and downstream signaling pathways that mediate vasodilation and pain transmission. Rat CGRP-(8-37) is a shortened form of CGRP that lacks the N-terminal amino acids required for receptor activation. It binds to the CGRP receptor with similar affinity to the full-length peptide but acts as a competitive antagonist, blocking the binding and activity of endogenous CGRP.
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| ln Vitro |
CGRP-(8-37) is a shortened form of calcitonin gene-related peptide (CGRP), which binds to CGRP receptors with similar affinity but does not activate receptors [1].
Rat CGRP-(8-37) demonstrates potent in vitro activity as a selective CGRP receptor antagonist. In receptor binding assays, it competes with radiolabeled CGRP for binding to CGRP receptors with high affinity. In functional assays, such as those measuring CGRP-induced cAMP accumulation or vasodilation in isolated blood vessels, Rat CGRP-(8-37) effectively blocks the effects of CGRP in a concentration-dependent manner. Its selectivity for CGRP receptors over other related receptors, such as the adrenomedullin or amylin receptors, makes it a valuable tool for studying CGRP-mediated signaling. The compound is supplied as a white to off-white solid powder with a purity of ≥98%. |
| ln Vivo |
In a dose-dependent manner, CGRP-(8–37) efficiently reduces mechanical and thermal allodynia. The best dose for both forelimb and hindlimb responses was 50 nM. The 20-minute efficacy period begins 10 minutes before the effects start to manifest. The post-Suzhou clear response is not statistically significant when compared to this pre-reaction [1]. Hindpaw withdrawal delay was significantly increased by intrathecal injection of 5 nmol or 10 nmol of CGRP-(8-37), but not 1 nmol. In addition to mediating a considerable increase in response latency relative to basal levels, intrathecal tagging of CGRP-(8–37) reversed the SP-induced decrease in latency of both withdrawal responses [2].
In vivo, Rat CGRP-(8-37) has been shown to effectively block the effects of CGRP in various animal models. In a dose-dependent manner, CGRP-(8-37) efficiently reduces mechanical and thermal allodynia, with the best dose for both forelimb and hindlimb responses being 50 nM. The efficacy period begins 10 minutes after administration and lasts for 20 minutes. Intrathecal injection of 5 nmol or 10 nmol of CGRP-(8-37) significantly increased hindpaw withdrawal latency, while 1 nmol had no effect. Additionally, intrathecal administration of CGRP-(8-37) reversed the substance P (SP)-induced decrease in withdrawal response latency, further confirming its antagonistic activity. These findings demonstrate the compound's ability to modulate pain responses by blocking CGRP receptor signaling. |
| Enzyme Assay |
In vitro receptor binding assays for Rat CGRP-(8-37) are performed using membrane preparations from cells or tissues expressing CGRP receptors. In a typical assay, increasing concentrations of the peptide are incubated with a fixed concentration of a radiolabeled CGRP ligand (e.g., [¹²⁵I]-CGRP) in a binding buffer. After incubation, bound and free radioligand are separated by filtration or centrifugation, and the radioactivity bound to the membranes is quantified. The IC50 value, representing the concentration of the peptide required to displace 50% of the specific binding, is calculated from the competition curve. Functional assays measure the peptide's ability to inhibit CGRP-induced signaling, such as cAMP accumulation in cells expressing CGRP receptors. These assays provide a quantitative measure of the peptide's affinity and antagonist activity.
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| Cell Assay |
In vitro cell-based assays for Rat CGRP-(8-37) are performed using cells expressing the CGRP receptor, such as SK-N-MC cells (which endogenously express CGRP receptors) or recombinant cell lines. Cells are treated with the peptide and then stimulated with CGRP. The inhibition of CGRP-induced cAMP accumulation is measured using a cAMP ELISA or a homogeneous time-resolved fluorescence (HTRF) assay. The peptide's potency as an antagonist can be determined from the shift in the CGRP dose-response curve in the presence of a fixed concentration of the antagonist. These assays provide a functional readout of the compound's antagonist activity in a cellular context.
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| Animal Protocol |
In vivo animal studies for Rat CGRP-(8-37) are conducted to study the role of CGRP in pain, migraine, and other physiological processes. The peptide is typically administered via intrathecal (into the spinal cord) or intracerebroventricular (into the brain ventricles) injection in rodents. In pain models, such as the formalin test or the spinal nerve ligation model of neuropathic pain, the peptide's ability to reduce pain behaviors (e.g., paw withdrawal, licking, or flinching) is assessed. In migraine models, the peptide's effects on CGRP-induced vasodilation or on the activation of the trigeminal system are evaluated. These studies help to elucidate the role of CGRP in these processes and validate CGRP as a therapeutic target.
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| ADME/Pharmacokinetics |
Rat CGRP-(8-37) is a peptide with a molecular weight of approximately 3127.51 and a molecular formula of C₁₃₈H₂₂₄N₄₂O₄₁. It is supplied as a white to off-white solid powder with a purity of ≥98%. The peptide is soluble in water at up to 1 mg/mL. For long-term storage, it is stable as a powder at -80°C for up to two years or at -20°C for up to one year. In solution, it can be stored at -80°C for up to six months or at -20°C for up to one month, protected from light and moisture.
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| Toxicity/Toxicokinetics |
The toxicological profile of Rat CGRP-(8-37) is not extensively documented, as it is a peptide antagonist used in research rather than a therapeutic agent. At the doses used in animal studies, it is generally well-tolerated. For laboratory handling, standard safety precautions for research chemicals should be observed, including the use of personal protective equipment (gloves, lab coat, safety goggles) and working in a well-ventilated area. The compound is intended for research use only and is not for human therapeutic or diagnostic use.
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| References | |
| Additional Infomation |
Rat CGRP-(8-37) is a selective CGRP receptor antagonist that binds to CGRP receptors with similar affinity to the full-length peptide but does not activate the receptor. Its sequence is VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF. The compound has a molecular formula of C₁₃₈H₂₂₄N₄₂O₄₁ and a molecular weight of approximately 3127.51. It is supplied as a white to off-white solid powder with a purity of ≥98%. Rat CGRP-(8-37) is a valuable tool for studying the physiological and pathophysiological roles of CGRP, particularly in pain, migraine, and cardiovascular regulation. Its ability to selectively block CGRP receptors makes it an essential reagent for researchers investigating this important neuropeptide signaling pathway.
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| Molecular Formula |
C138H224N42O41
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|---|---|
| Molecular Weight |
3127.51195999999
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| Exact Mass |
3125.67
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| CAS # |
129121-73-9
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| PubChem CID |
90479762
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| Appearance |
White to off-white solid powder
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| LogP |
0.05
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| Hydrogen Bond Donor Count |
47
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| Hydrogen Bond Acceptor Count |
46
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| Rotatable Bond Count |
103
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| Heavy Atom Count |
221
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| Complexity |
7260
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| Defined Atom Stereocenter Count |
28
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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](CCC(=O)O)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)O)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=CNC=N4)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C(C)C)N)O
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| InChi Key |
HZKKKBMPFPSSKZ-QZMRZBIOSA-N
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| InChi Code |
InChI=1S/C138H224N42O41/c1-64(2)46-84(158-99(189)58-152-112(197)72(17)156-119(204)85(47-65(3)4)165-117(202)80(37-29-43-149-137(144)145)160-122(207)88(51-78-55-148-63-155-78)170-135(220)110(75(20)185)179-130(215)104(142)67(7)8)120(205)166-86(48-66(5)6)121(206)173-94(62-183)128(213)161-81(38-30-44-150-138(146)147)118(203)172-92(60-181)114(199)153-56-98(188)151-57-101(191)174-106(69(11)12)133(218)176-107(70(13)14)132(217)163-79(36-27-28-42-139)116(201)169-91(54-103(194)195)124(209)168-89(52-96(140)186)123(208)167-87(50-77-34-25-22-26-35-77)125(210)177-108(71(15)16)136(221)180-45-31-39-95(180)129(214)178-109(74(19)184)134(219)171-90(53-97(141)187)126(211)175-105(68(9)10)131(216)154-59-100(190)159-93(61-182)127(212)162-82(40-41-102(192)193)115(200)157-73(18)113(198)164-83(111(143)196)49-76-32-23-21-24-33-76/h21-26,32-35,55,63-75,79-95,104-110,181-185H,27-31,36-54,56-62,139,142H2,1-20H3,(H2,140,186)(H2,141,187)(H2,143,196)(H,148,155)(H,151,188)(H,152,197)(H,153,199)(H,154,216)(H,156,204)(H,157,200)(H,158,189)(H,159,190)(H,160,207)(H,161,213)(H,162,212)(H,163,217)(H,164,198)(H,165,202)(H,166,205)(H,167,208)(H,168,209)(H,169,201)(H,170,220)(H,171,219)(H,172,203)(H,173,206)(H,174,191)(H,175,211)(H,176,218)(H,177,210)(H,178,214)(H,179,215)(H,192,193)(H,194,195)(H4,144,145,149)(H4,146,147,150)/t72-,73-,74+,75+,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,104-,105-,106-,107-,108-,109-,110-/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-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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~7.99 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 | 0.3197 mL | 1.5987 mL | 3.1974 mL | |
| 5 mM | 0.0639 mL | 0.3197 mL | 0.6395 mL | |
| 10 mM | 0.0320 mL | 0.1599 mL | 0.3197 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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