| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Calcitonin gene-related peptide (CGRP) receptor. HCGRP-(8-37) is a selective antagonist of the CGRP receptor. It binds to the receptor and blocks the binding of the endogenous ligand, CGRP. This inhibits CGRP-mediated signaling, which includes vasodilation and pain transmission.
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| ln Vitro |
HCGRP-(8-37) is a selective antagonist of the CGRP receptor. It has been shown to inhibit CGRP-induced vasodilation and CGRP-mediated pain transmission in vitro. It is a fragment of the full-length CGRP peptide and lacks the N-terminal amino acids required for agonist activity, making it a competitive antagonist.
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| ln Vivo |
In vivo, HCGRP-(8-37) has been shown to block the effects of CGRP in animal models. It inhibits CGRP-induced vasodilation and has been used to study the role of CGRP in migraine and pain. Its effects are mediated through the blockade of the CGRP receptor.
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| Enzyme Assay |
In vitro assays for HCGRP-(8-37) involve measuring its ability to bind to the CGRP receptor and block CGRP-induced signaling. Receptor binding assays can be performed using membrane preparations from cells expressing the CGRP receptor, with radiolabeled CGRP as a tracer. Functional assays measure the inhibition of CGRP-induced cAMP accumulation in cells expressing the receptor.
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| Cell Assay |
In vitro cell-based assays for HCGRP-(8-37) are performed using cells expressing the CGRP receptor. Cells are treated with the peptide antagonist, and its ability to block CGRP-induced cAMP accumulation is measured. The compound's potency and efficacy can be determined from concentration-response curves.
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| Animal Protocol |
In vivo animal studies for HCGRP-(8-37) are conducted to study the role of CGRP in pain, migraine, and cardiovascular function. The peptide is administered to rodents, and its effects on CGRP-induced vasodilation, pain behavior, or other physiological responses are measured.
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| ADME/Pharmacokinetics |
HCGRP-(8-37) is a peptide antagonist with a molecular weight of 3127.56 and a molecular formula of C139H224N44O40. As a peptide, it is susceptible to proteolytic degradation in vivo, which limits its half-life. It should be stored as a lyophilized powder at -20°C. It is soluble in aqueous solutions.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for HCGRP-(8-37) in the provided sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound.
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| References | |
| Additional Infomation |
HCGRP-(8-37) is a selective antagonist of the CGRP receptor. It is a fragment of human calcitonin gene-related peptide. It is used in research to study the role of CGRP in migraine, pain, and cardiovascular function. It is for research use only.
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| Molecular Formula |
C139H230N44O38
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|---|---|
| Molecular Weight |
3125.58549999999
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| Exact Mass |
3123.74
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| CAS # |
119911-68-1
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| Appearance |
White to off-white solid powder
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| Density |
1.46±0.1 g/cm3
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| LogP |
1.115
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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 : ≥ 20 mg/mL (~6.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 20 mg/mL (6.40 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3199 mL | 1.5997 mL | 3.1994 mL | |
| 5 mM | 0.0640 mL | 0.3199 mL | 0.6399 mL | |
| 10 mM | 0.0320 mL | 0.1600 mL | 0.3199 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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