| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 500mg |
| Targets |
CGRP receptor and adenylyl cyclase. This peptide fragment targets the CGRP receptor and modulates adenylyl cyclase activity, which is involved in cAMP signaling pathways.
|
|---|---|
| ln Vitro |
There are two types of human calcitonin gene-related peptide (CGRP): CGRP α (α-CGRP or CGRP I) and CGRP β (β-CGRP or CGRP II) [2]. Rats using the calcitonin gene-related peptide [Tyr22](22–37) demonstrated that the carboxyl terminus mostly determines receptor binding affinity, whereas the amino terminus primarily determines the ability to stimulate adenylyl cyclase (AC) [3].
The peptide fragment binds to the CGRP receptor, with the carboxyl terminus playing a key role in receptor binding affinity. The amino terminus primarily determines the ability to stimulate adenylyl cyclase. This suggests that the peptide can modulate CGRP receptor signaling in a fragment-specific manner. |
| ln Vivo |
No detailed in vivo activity data has been reported for Tyr-alpha-CGRP (23-37) in available literature. As a CGRP receptor fragment, it may modulate CGRP-mediated physiological effects in vivo, but specific animal study data are limited.
|
| Enzyme Assay |
CGRP receptor binding assays are performed using membrane preparations from tissues or cells expressing the CGRP receptor. Radiolabeled CGRP is used as a tracer, and competition binding experiments are conducted with Tyr-alpha-CGRP (23-37) to determine binding affinity. Adenylyl cyclase activity is measured by detecting cAMP accumulation in response to peptide treatment.
|
| Cell Assay |
Cells expressing the CGRP receptor are treated with Tyr-alpha-CGRP (23-37), and downstream signaling is assessed by measuring cAMP levels using ELISA or radioimmunoassay. The peptide's ability to modulate CGRP receptor activity is evaluated by comparing its effects to full-length CGRP agonists or antagonists.
|
| Animal Protocol |
No in vivo animal model data has been reported for Tyr-alpha-CGRP (23-37). As a CGRP receptor fragment, it could potentially be studied in rodent models of migraine, pain, or cardiovascular disease, but specific protocols have not been published.
|
| ADME/Pharmacokinetics |
Tyr-alpha-CGRP (23-37) has a molecular weight of 1785.95 and a molecular formula of C₈2H120N20O2₅. It is a peptide fragment with a purity of ≥98%. As a peptide, it is typically administered parenterally and has a short half-life in circulation.
|
| Toxicity/Toxicokinetics |
No toxicity data has been published for Tyr-alpha-CGRP (23-37). As a research peptide fragment, it is not intended for human therapeutic use.
|
| References |
|
| Additional Infomation |
[Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a 22-37 fragment of rat calcitonin gene-related peptide (CGRP). Calcitonin is mainly generated by thyroid C cells, while CGRP is secreted and stored in the nervous system. The compound is for research use only and has not entered clinical trials.
|
| Molecular Formula |
C82H120N20O25
|
|---|---|
| Molecular Weight |
1785.95000
|
| Exact Mass |
1784.87
|
| CAS # |
198277-54-2
|
| PubChem CID |
102602009
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.134
|
| Hydrogen Bond Donor Count |
24
|
| Hydrogen Bond Acceptor Count |
27
|
| Rotatable Bond Count |
54
|
| Heavy Atom Count |
127
|
| Complexity |
3800
|
| Defined Atom Stereocenter Count |
16
|
| 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](CC4=CC=C(C=C4)O)N)O
|
| InChi Key |
WWRQPUSVVKOCMA-XRXPIKPPSA-N
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| InChi Code |
InChI=1S/C82H120N20O25/c1-40(2)64(79(124)88-38-61(108)90-57(39-103)77(122)91-51(28-29-62(109)110)71(116)89-43(7)69(114)93-52(68(87)113)33-45-18-11-9-12-19-45)99-76(121)55(36-60(86)107)97-81(126)67(44(8)104)101-78(123)58-23-17-31-102(58)82(127)66(42(5)6)100-75(120)53(34-46-20-13-10-14-21-46)94-73(118)54(35-59(85)106)95-74(119)56(37-63(111)112)96-72(117)50(22-15-16-30-83)92-80(125)65(41(3)4)98-70(115)49(84)32-47-24-26-48(105)27-25-47/h9-14,18-21,24-27,40-44,49-58,64-67,103-105H,15-17,22-23,28-39,83-84H2,1-8H3,(H2,85,106)(H2,86,107)(H2,87,113)(H,88,124)(H,89,116)(H,90,108)(H,91,122)(H,92,125)(H,93,114)(H,94,118)(H,95,119)(H,96,117)(H,97,126)(H,98,115)(H,99,121)(H,100,120)(H,101,123)(H,109,110)(H,111,112)/t43-,44+,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,64-,65-,66-,67-/m0/s1
|
| 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-amino-3-(4-hydroxyphenyl)propanoyl]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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.5599 mL | 2.7996 mL | 5.5993 mL | |
| 5 mM | 0.1120 mL | 0.5599 mL | 1.1199 mL | |
| 10 mM | 0.0560 mL | 0.2800 mL | 0.5599 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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