| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Kiss2 peptide specifically binds to its cognate G protein-coupled receptor GPR54 (Kiss2R). Upon binding, it activates heterotrimeric G proteins (Galphas and Galphaq), leading to the activation of both the PKA (cAMP response element-dependent) and PKC (serum response element-dependent) signaling pathways. This activation stimulates the secretion of gonadotropin-releasing hormone (GnRH) from the hypothalamus, which in turn regulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary, thereby controlling reproductive function.
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| ln Vitro |
In vitro, Kiss2 peptide (0.01-10 uM) binds to Kiss2R (GPR54) in COS-7 cells transfected with the receptor, activating both PKA and PKC pathways. It enhances cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc) activity. It is a positive regulator of reproductive behavior. The peptide shows species-specific activity; the mouse Kiss2 peptide differs from human Kiss2 at several residues. It is not cytotoxic at concentrations up to 10 uM.
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| ln Vivo |
In vivo, Kiss2 peptide acts as a positive regulator of reproduction by stimulating GnRH secretion and activating the HPG axis. In animal models (e.g., fish, rodents), it is involved in the initiation of puberty, regulation of estrous cycles, and control of reproductive behavior. In fish, Kiss2 peptide has been shown to influence reproductive behavior and gonadal development. In mammals, it is implicated in the regulation of the HPG axis, but the kiss2 gene may have mutated in primates and been lost in birds during evolution. The peptide is not a therapeutic drug but a research tool for studying reproductive endocrinology.
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| Enzyme Assay |
The binding affinity of Kiss2 peptide to Kiss2R (GPR54) can be assessed by radioligand binding assay. Membranes from COS-7 cells expressing human or mouse GPR54 are incubated with a radiolabeled Kiss2 analog (e.g., ¹2⁵I-Kiss2) and varying concentrations (0.01-1000 nM) of unlabeled Kiss2 peptide in binding buffer (50 mM HEPES pH 7.4, 5 mM MgCl2, 0.1% BSA) at 25degC for 60-90 min. Bound radioactivity is separated by filtration, and the IC₅0 is calculated. The Ki is determined using the Cheng-Prusoff equation. For functional assays, cells expressing GPR54 are treated with Kiss2 peptide (0.01-10 uM), and intracellular cAMP levels are measured by ELISA or HTRF. The EC₅0 for cAMP accumulation is calculated.
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| Cell Assay |
For functional assays, COS-7 cells are co-transfected with GPR54 (Kiss2R) and CRE-luciferase or SRE-luciferase reporter plasmids. After 24 h, cells are seeded in 96-well plates (2×10⁴ cells/well) and treated with Kiss2 peptide (0.001-10 uM) for 6-24 h. Luciferase activity is measured using a luciferase assay kit. The EC₅0 for CRE-luc or SRE-luc activation is calculated. For calcium mobilization assays, cells loaded with Fluo-4 AM are treated with Kiss2 peptide, and fluorescence (λex 485 nm, λem 516 nm) is measured. The EC₅0 for calcium flux is calculated.
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| Animal Protocol |
For in vivo studies of reproductive function, the Kiss2 peptide is typically administered by intracerebroventricular (icv) injection or intraperitoneal (IP) injection in rodent models. Female Sprague-Dawley rats (8-10 weeks old, n=10/group) are treated with Kiss2 peptide (0.1-10 nmol/rat, ICV) or vehicle. Blood samples are collected at 15, 30, 60, 120 min post-injection. Serum LH and FSH levels are measured by ELISA. Ovarian histology and estrous cycle stage are assessed. For fish models, Kiss2 peptide is injected intraperitoneally, and reproductive behavior (e.g., spawning) and gonadal development are monitored.
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| ADME/Pharmacokinetics |
Kiss2 peptide (MW 1127.31) is a small neuropeptide. Following intracerebroventricular (icv) administration, it acts centrally within minutes to stimulate GnRH and LH secretion. The peptide has a very short plasma half-life (< 5 min) due to rapid proteolytic degradation by dipeptidyl peptidase IV (DPP-IV) and other peptidases. It does not cross the blood-brain barrier efficiently. For research use, it is stored as a lyophilized powder at -20degC, protected from light and moisture. It is soluble in water and DMSO. Detailed PK data is limited as it is a research reagent.
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| Toxicity/Toxicokinetics |
Kiss2 peptide has low toxicity. Standard safety precautions for handling peptides apply. The peptide may cause skin and eye irritation (H315, H319). It is for research use only and is not intended for human consumption. There are no reported adverse effects in animal studies at the doses used (0.1-10 nM, ICV). For handling, use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact.
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| References | |
| Additional Infomation |
Kiss2 peptide acetate is a research-grade neuropeptide agonist of GPR54 (Kiss2R) used for studying reproductive endocrinology, puberty initiation, and the regulation of the HPG axis. It is not an FDA-approved drug. It is a valuable tool for investigating the kisspeptin signaling pathway and its role in reproductive disorders such as hypogonadotropic hypogonadism and polycystic ovary syndrome (PCOS). For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month. Sequence: pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2.
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| Molecular Formula |
C63H84N16O12.XC2H4O2
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| Molecular Weight |
1257.44 (free base)
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| Related CAS # |
Kiss2 peptide;1111070-93-9
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| Appearance |
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) |
DMSO : ~100 mg/mL (with ultrasonication)
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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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