| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The targets of Antagonist G include vasopressin receptors, gastrin-releasing peptide (GRP) receptors, and bradykinin receptors. Antagonist G is a potent vasopressin antagonist. It is also a weak antagonist of GRP and bradykinin. As a substance P analog, Antagonist G acts as a broad-spectrum neuropeptide antagonist. The compound blocks Swiss 3T3 cell growth induced by vasopressin, gastrin-releasing peptide, and bradykinin. By antagonizing these neuropeptide receptors, Antagonist G inhibits neuropeptide-dependent proliferation of cancer cells. The compound also activates JNK and stimulates apoptosis.
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| ln Vitro |
In SCLC cells, agonist G (0-100 μM) causes apoptosis that is caspase-dependent and redox-sensitive [2]. In SCLC cells, agonist G activates JNK1 [2]. While agonist G only slightly enhances the production of free radicals in SCLC cells (6.2-fold), it also causes a 61% rise in the activity of the redox-sensitive transcription factor AP-1 [2]. Antagonist G is not primarily a free radical oxygen donor.
In vitro, Antagonist G demonstrates broad-spectrum neuropeptide antagonist and antiproliferative activity. The compound blocks Swiss 3T3 cell growth induced by vasopressin, gastrin-releasing peptide, and bradykinin. Antagonist G inhibits neuropeptide-dependent and -independent proliferation of small cell lung cancer in vitro. The compound activates JNK and stimulates apoptosis. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy. The compound is an anticancer agent and is resistant to degradation by peptidases. These in vitro activities demonstrate the compound's potential as an anticancer therapeutic. |
| ln Vivo |
In vivo, Antagonist G inhibits the growth of small cell lung cancer xenografts in mice. The compound's broad-spectrum neuropeptide antagonist activity and antiproliferative effects have been demonstrated in animal models. Antagonist G can induce the transcription of AG-1 and sensitize cancer cells to chemotherapy. The compound's resistance to degradation by peptidases suggests it may have favorable in vivo stability. Further in vivo studies are needed to fully characterize its efficacy and safety in various cancer models. The compound has been investigated for its anticancer potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Antagonist G focus on its interactions with neuropeptide receptors. Binding affinity to vasopressin, GRP, and bradykinin receptors can be assessed using radioligand competition assays. The compound's ability to block receptor-mediated signaling can be evaluated using calcium flux assays or second messenger measurements. AP-1 transcription activity can be measured using luciferase reporter assays. JNK activation can be assessed by Western blot using phospho-specific antibodies. These methods are for research purposes only.
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| Cell Assay |
Cell viability assay [2]
Cell Types: SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells. Tested Concentrations: 0-100 μM. Incubation Duration: 24 hrs (hours). Experimental Results: Inhibition of cell growth. In vitro cell-based assays for Antagonist G evaluate its antiproliferative and pro-apoptotic effects. Small cell lung cancer cell lines or Swiss 3T3 cells are treated with Antagonist G at various concentrations (typically 0.1-100 µM) for 24-72 hours. Cell proliferation is assessed using MTT, BrdU incorporation, or cell counting assays. Apoptosis is measured using Annexin V/PI staining, caspase activity assays, and JNK activation by Western blot. AP-1 transcription activity is measured using reporter assays. Chemosensitization is evaluated by combining Antagonist G with chemotherapeutic agents and assessing cell viability. Standard cell culture conditions are used. |
| Animal Protocol |
In vivo animal studies for Antagonist G utilize xenograft mouse models of small cell lung cancer. Tumor-bearing mice are treated with Antagonist G via intraperitoneal or intravenous administration at various doses. Tumor volumes are measured regularly using calipers, and body weight is monitored for toxicity assessment. Combination studies with chemotherapeutic agents are conducted to evaluate sensitization effects. Pharmacodynamic studies evaluate AP-1 transcription, JNK activation, and apoptosis in tumor tissues. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Antagonist G are not fully characterized in publicly available literature. The compound is a peptide with a molecular weight of 951.19 Da and is resistant to degradation by peptidases. This resistance may contribute to favorable in vivo stability. The compound is for research use only and is not approved for clinical use. Detailed pharmacokinetic parameters (half-life, Cmax, AUC, clearance) would need to be determined in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of Antagonist G is not fully characterized in publicly available literature. The compound is classified for research use only and not for human consumption. Standard safety precautions for handling peptides apply, including the use of personal protective equipment and working in a chemical fume hood. Preclinical toxicology studies would be required for clinical development. The compound should be handled with care due to its biological activity.
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| References | |
| Additional Infomation |
Additional information: Antagonist G has the CAS number 115150-59-9 and the molecular weight 951.19 Da. The compound is a substance P analog with the sequence RWFWLM (modifications: Trp-2 = D-Trp, Phe-3 = N-Methyl-Phe, Trp-5 = D-Trp, Met-7 = C-terminal amide). Antagonist G is a potent vasopressin antagonist and a weak antagonist of GRP and bradykinin. The compound activates JNK and stimulates apoptosis. Antagonist G induces AP-1 transcription and sensitizes cancer cells to chemotherapy. The compound inhibits neuropeptide-dependent and -independent proliferation of small cell lung cancer in vitro and inhibits growth of SCLC xenografts in mice. Antagonist G is resistant to degradation by peptidases. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C49H66N12O6S
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|---|---|
| Molecular Weight |
951.19000
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| Exact Mass |
950.495
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| CAS # |
115150-59-9
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| Related CAS # |
Antagonist G TFA
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| PubChem CID |
163960
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.35g/cm3
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| Index of Refraction |
1.666
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| LogP |
6.473
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
68
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| Complexity |
1700
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)N(C)C(=O)[C@@H](CC4=CNC5=CC=CC=C54)NC(=O)[C@H](CCCN=C(N)N)N
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| InChi Key |
CUCSSYAUKKIDJV-FAXBSAIASA-N
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| InChi Code |
InChI=1S/C49H66N12O6S/c1-29(2)23-39(45(64)57-38(43(51)62)20-22-68-4)58-46(65)40(25-31-27-55-36-18-10-8-15-33(31)36)59-47(66)42(24-30-13-6-5-7-14-30)61(3)48(67)41(26-32-28-56-37-19-11-9-16-34(32)37)60-44(63)35(50)17-12-21-54-49(52)53/h5-11,13-16,18-19,27-29,35,38-42,55-56H,12,17,20-26,50H2,1-4H3,(H2,51,62)(H,57,64)(H,58,65)(H,59,66)(H,60,63)(H4,52,53,54)/t35-,38-,39-,40+,41+,42-/m0/s1
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| Chemical Name |
(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]-methylamino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]-4-methylpentanamide
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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 : ~50 mg/mL (~52.57 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 | 1.0513 mL | 5.2566 mL | 10.5131 mL | |
| 5 mM | 0.2103 mL | 1.0513 mL | 2.1026 mL | |
| 10 mM | 0.1051 mL | 0.5257 mL | 1.0513 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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