| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Targets the kisspeptin receptor KISS1 (GPR54) as a competitive antagonist. The kisspeptin receptor is a GPCR that binds the endogenous peptide kisspeptin, which stimulates gonadotropin-releasing hormone (GnRH) release and plays a central role in puberty onset and reproductive function.
|
|---|---|
| ln Vitro |
As a KISS1R antagonist, Kisspeptin 234 TFA blocks the activation of the kisspeptin receptor by endogenous kisspeptin peptides, thereby inhibiting downstream signaling pathways that include calcium mobilization, MAPK activation, and GnRH secretion in hypothalamic neurons and pituitary gonadotrope cells.
|
| ln Vivo |
In the bleomycin (BLM)-induced C57BL/6 mice pulmonary fibrosis model, kisspeptin 234 (1 mg/kg, ip, daily, 28 days) TFA can suppress the anti-fibrotic action of kisspeptin-13, particularly with regard to weight loss, decreased survival rate, increased lung coefficient, and massive infiltration [1].
In a bleomycin (BLM)-induced pulmonary fibrosis model in C57BL/6 mice, intraperitoneal administration of Kisspeptin 234 TFA (1 mg/kg, once daily for 28 days) significantly inhibits the antifibrotic effect of Kisspeptin-13, evidenced by reduced body weight, decreased survival rates, increased lung coefficients, and extensive inflammatory infiltration, confirming its in vivo antagonist activity. |
| Enzyme Assay |
Non-cell binding assays are performed using human KISS1R-expressing cell membranes and radiolabeled kisspeptin-10 tracer (e.g., [¹2⁵I]Kp-10). Membranes are incubated with cold competitor peptide (0.1 nM-10 microM) for 90 min at room temperature, then filtered through GF/C filters. Bound radioactivity is measured with a gamma counter to determine IC50 and Ki values.
|
| Cell Assay |
HEK293 cells stably expressing human KISS1R are loaded with Fluo-4 AM fluorescent calcium indicator (2 microM) for 30 min at 37degC. After wash, cells are pre-incubated with antagonist (0.1 nM-10 microM) for 10 min, then stimulated with 1 nM kisspeptin-10. Fluorescence changes (Ex/Em=488/525 nm) are recorded for 60 sec using a fluorometric imaging plate reader.
|
| Animal Protocol |
In mouse pulmonary fibrosis models, BLM (2.5 U/kg) is intratracheally instilled on day 0. Mice receive Kisspeptin 234 TFA (1 mg/kg, i.p.) or vehicle daily for 28 days. Body weight and survival are recorded daily. At day 28, lungs are harvested for histology (H&E and Masson's trichrome staining), hydroxyproline content, and inflammatory cytokine analysis.
|
| ADME/Pharmacokinetics |
Detailed pharmacokinetic parameters for this peptide antagonist are not publicly available. As a peptide, it is expected to have limited oral bioavailability and a short half-life due to proteolytic degradation in vivo. Peptides are typically administered via parenteral routes (i.p., i.v., or s.c.) for in vivo studies.
|
| Toxicity/Toxicokinetics |
Specific toxicity data is not publicly available for Kisspeptin 234 TFA. As a peptide antagonist, it is expected to have minimal off-target toxicity based on its specificity for KISS1R. However, long-term inhibition of the kisspeptin system may disrupt normal reproductive physiology and puberty onset.
|
| References | |
| Additional Infomation |
Kisspeptin 234 TFA is a research peptide not approved for clinical use. The KISS1R (GPR54) is a major gatekeeper of the HPG axis and a potential therapeutic target for hormone-dependent cancers, reproductive disorders, and precocious puberty. This antagonist is a useful pharmacological tool for blocking kisspeptin signaling in experimental models.
|
| Molecular Formula |
C65H79F3N18O15
|
|---|---|
| Molecular Weight |
1409.42958378792
|
| Exact Mass |
1408.592
|
| CAS # |
1848962-29-7
|
| Related CAS # |
Kisspeptin 234;1145998-81-7
|
| PubChem CID |
168007005
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
19
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
37
|
| Heavy Atom Count |
101
|
| Complexity |
2760
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
FC(C(=O)O)(F)F.O=C([C@@H](CC1=CNC2C=CC=CC1=2)NC(CNC([C@H](CC1C=CC=CC=1)NC(CNC([C@H](CC(N)=O)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@H](CC(N)=O)NC([C@@H](C)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(N[C@H](C(N)=O)CC1C=CC=CC=1)=O)CCCNC(=N)N
|
| InChi Key |
XYUGIYOAGFFAEE-VIJDQBLHSA-N
|
| InChi Code |
InChI=1S/C63H78N18O13.C2HF3O2/c1-34(74-35(2)82)56(88)79-50(29-52(65)84)62(94)80-48(27-39-31-71-43-21-12-10-19-41(39)43)61(93)81-49(28-51(64)83)58(90)73-32-53(85)75-46(25-37-16-7-4-8-17-37)57(89)72-33-54(86)76-47(26-38-30-70-42-20-11-9-18-40(38)42)60(92)77-44(22-13-23-69-63(67)68)59(91)78-45(55(66)87)24-36-14-5-3-6-15-36;3-2(4,5)1(6)7/h3-12,14-21,30-31,34,44-50,70-71H,13,22-29,32-33H2,1-2H3,(H2,64,83)(H2,65,84)(H2,66,87)(H,72,89)(H,73,90)(H,74,82)(H,75,85)(H,76,86)(H,77,92)(H,78,91)(H,79,88)(H,80,94)(H,81,93)(H4,67,68,69);(H,6,7)/t34-,44+,45+,46+,47-,48+,49+,50+;/m1./s1
|
| Chemical Name |
(2S)-2-[[(2R)-2-acetamidopropanoyl]amino]-N-[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1-[[2-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]butanediamide;2,2,2-trifluoroacetic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 25 mg/mL (17.74 mM)
H2O: 1.67 mg/mL (1.18 mM) |
|---|---|
| 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 | 0.7095 mL | 3.5475 mL | 7.0951 mL | |
| 5 mM | 0.1419 mL | 0.7095 mL | 1.4190 mL | |
| 10 mM | 0.0710 mL | 0.3548 mL | 0.7095 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
