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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Hemopressin targets the cannabinoid receptor type 1 (CB1). It is a selective inverse agonist at CB1 receptors, meaning it binds to the receptor and reduces its constitutive activity below basal levels. The peptide is orally bioactive, which is unusual for a peptide therapeutic. Hemopressin has been shown to interact with CB1 and modulate its activity, with potential therapeutic applications in various diseases. It reduces food intake through CB1 receptor-mediated mechanisms.
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| ln Vitro |
In vitro, Hemopressin acts as a selective inverse agonist at CB1 cannabinoid receptors. It binds to CB1 receptors and reduces their constitutive activity. The peptide has been shown to modulate CB1 receptor signaling in various cell-based assays. Its activity is distinct from that of classic CB1 antagonists, as inverse agonists reduce baseline receptor signaling rather than merely blocking agonist binding. Standard in vitro assays include receptor binding studies, [35S]GTPγS binding assays for G protein activation, and cAMP accumulation assays.
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| ln Vivo |
Hemopressin produces hypotension in anesthetized rats and is processed in vivo and in vitro by endopeptidase 24.15 (EP24.15), neurolysin (EP24.16), and angiotensin-converting enzyme (ACE)[1]. Oral dose of Hemopressin prevents mechanical hyperalgesia of CCI-rats up to 6h. Hemopressin therapy also lowers Egr-1 immunoreactivity (Egr-1Ir) in the superficial layer of the dorsal horn of the spinal cord of CCI rats[2].
In vivo, Hemopressin exerts antinociceptive effects in inflammatory pain models. The peptide acts through CB1 cannabinoid receptors to reduce food intake in rats and mice. Its oral bioavailability makes it a particularly interesting research tool, as most peptides are not orally active. Hemopressin has shown anti-injury sensory effects in models of inflammatory pain. The compound has potential therapeutic applications in pain management and appetite regulation. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Hemopressin can be evaluated using membrane preparations from cells expressing human CB1 receptors. Radioligand binding displacement experiments are performed using [3H]-CP55940 or [3H]-SR141716A as the radiolabeled ligand. Membrane homogenates are incubated with increasing concentrations of the peptide and a fixed concentration of the radioligand at 30°C for 60 minutes. Bound radioligand is separated from free by filtration through GF/B filters. Nonspecific binding is determined in the presence of 10 µM unlabeled ligand. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human CB1 receptors (e.g., CHO or HEK293 cells) are cultured in appropriate media. For inverse agonist activity assessment, [35S]GTPγS binding assays are performed. Membrane preparations are incubated with GDP, [35S]GTPγS, and various concentrations of Hemopressin. The amount of bound [35S]GTPγS is measured by filtration. A reduction in basal [35S]GTPγS binding compared to control indicates inverse agonist activity. For cAMP accumulation assays, cells are treated with the peptide and cAMP levels are measured using ELISA or HTRF-based detection.
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| Animal Protocol |
For in vivo animal studies, Hemopressin can be administered orally to rodents. In inflammatory pain models (e.g., carrageenan-induced paw inflammation or complete Freund's adjuvant-induced arthritis), mechanical allodynia and thermal hyperalgesia are assessed. In food intake studies, rats or mice are treated with the peptide and food consumption is measured over a period of hours to days. In models of obesity, body weight and metabolic parameters may be measured. Dosing regimens vary depending on the specific model.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Hemopressin are notable for its oral bioavailability. As a peptide, oral bioavailability is unusual and suggests that the peptide may be resistant to proteolytic degradation in the gastrointestinal tract or may be absorbed through specific transport mechanisms. The compound has a molecular weight of 1054.24. Comprehensive pharmacokinetic studies would include assessment of oral bioavailability, half-life, protein binding, and tissue distribution. The compound should be stored appropriately for peptide stability.
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| Toxicity/Toxicokinetics |
The toxicity profile of Hemopressin has not been extensively reported. As a peptide derived from hemoglobin, it may have a favorable safety profile compared to synthetic compounds. The compound is for research use only and not for human consumption. Potential adverse effects may include those associated with CB1 inverse agonism, such as gastrointestinal effects or mood changes. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on food intake and body weight.
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| References | |
| Additional Infomation |
Hemopressin (human, mouse) is a nine-amino acid peptide derived from the α1 chain of hemoglobin, originally isolated from rat brain homogenates. It is an orally bioactive, selective inverse agonist of the CB1 cannabinoid receptor. The peptide exerts antinociceptive effects in inflammatory pain models and reduces food intake through CB1 receptor mechanisms. Hemopressin has potential therapeutic applications in pain management, appetite regulation, and other CB1-mediated conditions. It is available for research purposes only.
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| Molecular Formula |
C50H79N13O12
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|---|---|
| Molecular Weight |
1054.24
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| Exact Mass |
1053.597
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| CAS # |
1314035-51-2
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| Related CAS # |
Hemopressin(human, mouse) TFA;1431329-48-4
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| PubChem CID |
90488877
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1491.3±65.0 °C at 760 mmHg
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| Flash Point |
855.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
0.6
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
75
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CN=CN1)C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]3CCCN3
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| InChi Key |
JEXQOFXDPAGOQL-TZFLQVIRSA-N
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| InChi Code |
InChI=1S/C50H79N13O12/c1-27(2)19-34(44(68)58-35(20-28(3)4)45(69)62-39(25-64)48(72)61-38(50(74)75)22-31-24-53-26-55-31)57-43(67)33(15-10-11-17-51)56-46(70)36(21-30-13-8-7-9-14-30)59-47(71)37(23-40(52)65)60-49(73)41(29(5)6)63-42(66)32-16-12-18-54-32/h7-9,13-14,24,26-29,32-39,41,54,64H,10-12,15-23,25,51H2,1-6H3,(H2,52,65)(H,53,55)(H,56,70)(H,57,67)(H,58,68)(H,59,71)(H,60,73)(H,61,72)(H,62,69)(H,63,66)(H,74,75)/t32-,33-,34-,35-,36-,37-,38-,39-,41-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-3-methyl-2-[[(2S)-pyrrolidine-2-carbonyl]amino]butanoyl]amino]-4-oxobutanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoic 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: ≥ 16.67 mg/mL (15.81 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 | 0.9486 mL | 4.7428 mL | 9.4855 mL | |
| 5 mM | 0.1897 mL | 0.9486 mL | 1.8971 mL | |
| 10 mM | 0.0949 mL | 0.4743 mL | 0.9486 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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