![[K15,R16,L27]VIP(1-7)/GRF(8-27) acetate](/upload/1124/V77340.png)
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
VIP1[1]
Vasoactive intestinal peptide receptor 1 (VIP1, also known as VPAC1). VIP1 is a class B G-protein coupled receptor (GPCR) widely expressed in the immune system, gastrointestinal tract, and central nervous system. [K15,R16,L27]VIP(1-7)/GRF(8-27) acetate is a selective agonist that potently activates VIP1, regulating inflammation, smooth muscle relaxation, and immunomodulation. It shows high selectivity for VIP1 over the closely related VIP2 receptor (rat VIP2 IC50 = 30,000 nM). |
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| ln Vitro |
In vitro, this peptide exhibits potent binding affinity with IC50 values of 2 nM for the human VIP1 receptor and 1 nM for the rat VIP1 receptor. Its selectivity for VIP1 over VIP2 is extremely high (>1000-fold), as demonstrated by an IC50 of 30,000 nM for the rat VIP2 receptor. This high selectivity makes it a valuable tool for dissecting the distinct physiological roles of VIP1 and VIP2 receptor subtypes.
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| ln Vivo |
As a highly selective VIP1 agonist, this peptide is used in animal models to investigate VIP1-mediated signaling pathways. It is ideal for studying neuroendocrine regulation, inflammation (anti-inflammatory effects), smooth muscle relaxation (e.g., bronchodilation, vasodilation), and immunomodulation. The hybrid structure combines the N-terminal receptor-binding domain of VIP with the C-terminal domain of GRF for enhanced potency and receptor selectivity.
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| Enzyme Assay |
A non-cell competitive radioligand binding assay is used to determine receptor affinity. Membrane preparations from CHO cells expressing human VIP1 receptor are incubated with the radioligand [125I]-VIP (50-100 pM) and varying concentrations of the unlabeled test peptide (0.01-1000 nM) in assay buffer containing 50 mM HEPES (pH 7.4), 5 mM MgCl2, and 0.1% BSA. After incubation at 25degC for 60 minutes, the mixture is rapidly filtered through GF/C filters, and bound radioactivity is counted. IC50 values are calculated, and Ki values are derived using the Cheng-Prusoff equation.
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| Cell Assay |
A functional cAMP accumulation assay is used to measure VIP1 receptor activation. HEK-293 cells stably expressing human VIP1 receptors are seeded in 96-well plates. After pre-incubation with 0.5 mM IBMX, cells are treated with varying concentrations of the peptide (0.01-1000 nM) for 30-60 minutes. The resulting intracellular cAMP levels are then measured using a competitive ELISA or HTRF-based cAMP assay kit (e.g., Cisbio). The EC50 for cAMP accumulation is calculated from the dose-response curve; this peptide is typically a full agonist with EC50 in the low nanomolar range.
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| Animal Protocol |
For in vivo efficacy studies, the peptide is used in rodent models of inflammatory bowel disease or acute lung injury. A typical protocol involves administering the peptide intravenously (IV, 10-30 ug/kg) or intraperitoneally (IP, 50-200 ug/kg) 30 minutes before induction of inflammation (e.g., by LPS or colitis-inducing agents). Endpoints include measurement of pro-inflammatory cytokines (TNF-alpha, IL-6) in plasma or tissue homogenates by ELISA, as well as histological scoring of tissue inflammation and neutrophil infiltration. The VIP1 agonist reduces inflammation in a dose-dependent manner.
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| ADME/Pharmacokinetics |
As a 35-amino acid hybrid peptide, the acetate salt is highly water-soluble and stable. The peptide has a short plasma half-life (approximately 2-5 minutes) due to rapid degradation by ubiquitous proteases, which limits its direct therapeutic use but makes it suitable for bolus injection studies. For in vivo administration, it is typically formulated in sterile PBS (pH 7.4) or saline with 0.1% BSA to prevent adsorption to plastic surfaces. Long-term storage: lyophilized powder at -80degC; avoid repeated freeze-thaw.
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| Toxicity/Toxicokinetics |
The toxicity of [K15,R16,L27]VIP(1-7)/GRF(8-27) acetate is not extensively documented beyond its pharmacological effects. At the doses used for research (e.g., 10-200 ug/kg), no overt toxicity such as weight loss, organ damage, or abnormal behavior has been reported. Due to its VIP1-mediated vasodilatory effects, hypotension may occur if administered systemically at high doses. The acetate counterion is non-toxic at these concentrations.
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| References |
[1]. P Gourlet, et al. Development of high affinity selective VIP1 receptor agonists. Peptides. 1997;18(10):1539-45.
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| Additional Infomation |
[K15,R16,L27]VIP(1-7)/GRF(8-27) acetate is a research-grade chemical tool for studying VIP1 receptor pharmacology. It is not a drug and has no FDA approval. It is used to explore VIP1 receptor pathways in inflammation, smooth muscle relaxation, and immunomodulation. This product is a highly selective alternative to native VIP, which non-selectively activates both VIP1 and VIP2. This product is for research use only (RUO).
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| Molecular Formula |
C142H240N44O38.XC2H4O2
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| Molecular Weight |
3171.70 (free base)
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| Related CAS # |
[K15,R16,L27]VIP(1-7)/GRF(8-27);201995-58-6
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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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