| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CB1
Cannabinoid receptor type 1 (CB1R) and type 2 (CB2R). RVD-Hpalpha acts as a selective agonist at CB1 receptors, directly activating the receptor. Additionally, it functions as a high-affinity positive allosteric modulator (PAM) at CB2 receptors (Ki=50 nM), meaning it binds to a site distinct from the orthosteric site to enhance the effect of endogenous or orthosteric agonists. |
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| ln Vitro |
In vitro, RVD-Hpalpha increases intracellular Ca2+ levels in cells expressing CB1 receptors, confirming its functional activity as a CB1 agonist. It also acts as a high-affinity CB2 positive allosteric modulator (PAM) with a Ki of 50 nM. This dual mechanism (agonist at CB1, allosteric enhancer at CB2) is a unique and defining feature of this peptide.
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| ln Vivo |
Specific in vivo activity data for RVD-Hpalpha TFA is not detailed in the provided references. As a peptide, its in vivo use may be limited by rapid proteolytic degradation unless administered directly into the CNS or protected by modifications. Its dual CB1 agonist/CB2 PAM profile suggests potential for unique in vivo effects distinct from traditional orthosteric ligands.
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| Enzyme Assay |
The binding affinity of RVD-Hpalpha for CB2 as a PAM is determined via a radioligand binding assay in the presence of an orthosteric agonist. Membranes from CHO cells expressing human CB2R are incubated with [3H]CP-55,940, a fixed concentration of a CB2 orthosteric agonist (e.g., JWH-133), and varying concentrations of RVD-Hpalpha. An increase in [3H]CP-55,940 binding indicates positive allosteric modulation.
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| Cell Assay |
Functional CB1 agonist activity is assessed by measuring intracellular calcium flux. HEK-293 cells expressing human CB1R and a chimeric G-protein (Gqi5) are loaded with a calcium-sensitive dye (e.g., Fluo-4). Cells are then treated with varying concentrations of RVD-Hpalpha, and the resulting increase in fluorescence is measured to determine the EC50 for receptor activation.
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| Animal Protocol |
In vivo protocols for hemopressin-derived peptides often involve intracerebroventricular (ICV) injection in mice to bypass the blood-brain barrier. RVD-Hpalpha would be dissolved in sterile saline or artificial CSF and injected directly into the lateral ventricle (e.g., 5-20 nmol/mouse). Behavioral endpoints such as nociception (tail-flick test), locomotor activity, or anxiety-like behavior (elevated plus maze) are then measured.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data for RVD-Hpalpha TFA is provided. As a 12-amino acid peptide with a molecular weight of approximately 1538.68 g/mol, it is expected to have very poor oral bioavailability and a short half-life in vivo due to rapid degradation by proteases in blood and tissues. Its use is primarily confined to in vitro studies or direct CNS injection.
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| Toxicity/Toxicokinetics |
No specific toxicological data is provided. As a peptide that acts on cannabinoid receptors, potential toxicities would be extensions of its pharmacology, such as CB1-mediated CNS effects (sedation, hypothermia, catalepsy). Its trifluoroacetate (TFA) salt form is common for peptide handling but TFA can be toxic in vivo if not properly exchanged.
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| Additional Infomation |
RVD-Hpalpha TFA is a significant tool because it reveals the complexity of the “hemopressin family” of peptides. Hemopressin itself (PVNFKLLSH) is an inverse agonist at CB1, while its N-terminally extended form (RVD-Hpalpha) is an agonist. This simple N-terminal extension completely flips the pharmacological activity, demonstrating the exquisite sensitivity of the CB1 receptor to peptide conformation and charge distribution.
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| CAS # |
1431329-51-9
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| Appearance |
White to off-white solid powder
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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) |
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.) |
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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