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| 1mg |
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| 5mg | |||
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| Other Sizes |
| Targets |
RC-3095 TFA selectively targets the bombesin/gastrin releasing peptide receptor (GRPR), a G protein-coupled receptor that belongs to the bombesin receptor family. GRPR is activated by bombesin and gastrin-releasing peptide (GRP), which regulate various physiological processes including gastrointestinal motility, secretion, and growth, as well as neurotransmission and inflammation. GRPR overexpression has been implicated in various cancers, including prostate, breast, and small-cell lung cancer. By antagonizing GRPR, RC-3095 blocks GRP-mediated signaling, inhibiting tumor growth, inflammation, and oxidative injury. The compound exerts protective effects by reducing gastric oxidative injury in arthritic mice.
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| ln Vitro |
In vitro, RC-3095 TFA acts as a selective antagonist at the bombesin/GRP receptor. The compound competitively inhibits the binding of bombesin and GRP to GRPR, blocking receptor-mediated signaling pathways including phospholipase C activation, calcium mobilization, and MAPK/ERK signaling. In cellular assays, RC-3095 inhibits GRP-stimulated cell proliferation and migration in cancer cell lines expressing GRPR. The compound also reduces inflammatory cytokine production and oxidative stress markers in various cell types. RC-3095's in vitro profile supports its use as a tool for studying GRPR biology and as a potential therapeutic for GRPR-associated diseases.
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| ln Vivo |
Rather than harming the recognition memory, RC-3095 damages the Wistar's loaded auspicious memory[1]. Induction-induced arthritis (CIA) and induction-induced arthritis (AIA), two experimental models of arthritis, RC-3095 (0.3 mg/kg or 1 mg/kg; SC) shows anti-inflammatory effects [ 2]. GRPR expression was upregulated in arthritic arthritis patients treated with RC-3095, although IL-17, IL-1, and TNF concentrations were markedly decreased.
In vivo, RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in arthritic mice. The compound has been studied in animal models of inflammation and cancer. In arthritic mice, RC-3095 reduces gastric mucosal injury by decreasing oxidative stress and inflammatory responses. In tumor models, GRPR antagonists like RC-3095 have shown efficacy in inhibiting tumor growth and metastasis. The compound's ability to block GRPR-mediated signaling provides a mechanism for its anti-inflammatory and antitumor effects. However, detailed pharmacokinetic and efficacy data for RC-3095 TFA are limited in publicly available sources. |
| Enzyme Assay |
In vitro receptor binding assays for RC-3095 TFA are performed using membrane preparations from cells expressing recombinant human GRPR. Radiolabeled ligands such as [¹2⁵I]-GRP or [¹2⁵I]-bombesin are used. Membranes are incubated with varying concentrations of RC-3095 in assay buffer at room temperature for 60-90 minutes. Bound and free radioligands are separated by rapid filtration through glass fiber filters. Filter-bound radioactivity is quantified by gamma counting. Ki values are calculated using the Cheng-Prusoff equation. Functional assays measure calcium mobilization or inositol phosphate accumulation in cells expressing GRPR to confirm antagonist activity. IC₅0 values for inhibition of GRP-stimulated signaling are determined.
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| Cell Assay |
In vitro cellular assays for RC-3095 TFA are performed using cell lines expressing GRPR, such as Swiss 3T3 fibroblasts or cancer cell lines. Cells are cultured in appropriate medium and seeded in 96-well plates. Cells are treated with serial dilutions of RC-3095 (0.001-10 microM) for 30-60 minutes prior to stimulation with GRP or bombesin. Calcium mobilization is measured using fluorescent calcium indicators (e.g., Fluo-4, Fura-2). Cell proliferation is assessed by [3H]-thymidine incorporation or BrdU labeling. Inflammatory cytokine production (IL-6, TNF-alpha) is measured by ELISA. IC₅0 values for inhibition of GRP-stimulated responses are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male Balb/c wild-type mice (body weight 18-25 gm), AIA model ; Reduce[2]. CIA Model Male DBA/1J inbred mice (body weight 18-25 g) [2]
Doses: 1 mg/kg for AIA studies; 0.3 mg/kg or 1 mg/kg for CIA studies Dosing: daily for AIA studies subcutaneous injections were given twice for a total of 2 or 10 days; subcutaneous injections were given twice (two times) daily for 10 days after onset of illness for CIA studies. Experimental Results: Mice with AIA had diminished neutrophil migration, mechanical nociception, and proteoglycan loss; resulting in Dramatically diminished arthritis clinical scores and disease severity in the CIA model. In vivo animal studies for RC-3095 TFA are conducted in rodent models of inflammation and cancer. In arthritic mouse models, RC-3095 is administered intraperitoneally at doses of 10-100 microg/kg. Gastric mucosal injury is assessed by measuring oxidative stress markers (malondialdehyde, glutathione) and histological examination. In tumor models, mice bearing GRPR-expressing tumor xenografts are treated with RC-3095, and tumor growth is monitored. Pharmacokinetic parameters are determined from plasma samples. Efficacy is compared to vehicle control and standard-of-care agents. The compound's protective effects are evaluated by assessing tissue injury, inflammation, and oxidative stress. |
| ADME/Pharmacokinetics |
RC-3095 (TFA) (CAS#: 1217463-61-0) has molecular formula C₅₈H₈0F3N1₅O11 and molecular weight 1220.34. The compound is a peptide-based bombesin/gastrin releasing peptide receptor (GRPR) antagonist. It exerts protective effects by reducing gastric oxidative injury in arthritic mice. The TFA salt form enhances solubility and formulation characteristics. The compound is supplied as a research chemical for laboratory use only. Purity is typically ≥98%. Storage should be at -20degC, protected from light and moisture.
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| References |
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| Additional Infomation |
RC-3095 (TFA) (CAS#: 1217463-61-0) is a novel and potent bombesin/gastrin releasing peptide receptor (GRPR) antagonist. GRPR is a G protein-coupled receptor that mediates the biological effects of bombesin and gastrin-releasing peptide, which are involved in gastrointestinal function, neurotransmission, inflammation, and tumor growth. RC-3095 exerts protective effects by reducing gastric oxidative injury in arthritic mice. The compound is used in research to study GRPR-mediated signaling pathways and their roles in inflammation, cancer, and gastrointestinal disorders. As of the current date, RC-3095 TFA remains a preclinical research compound and is not approved for clinical use.
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| Molecular Formula |
C60H81F6N15O13
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| Molecular Weight |
1334.3682744503
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| Exact Mass |
1219.611
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| CAS # |
1217463-61-0
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| Related CAS # |
RC-3095;138147-78-1
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| PubChem CID |
16219940
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
87
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| Complexity |
2220
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| Defined Atom Stereocenter Count |
8
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| SMILES |
FC(C(=O)O)(F)F.FC(C(=O)O)(F)F.O=C([C@H]1CC2C3C=CC=CC=3NC=2CN1)N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@H](C(NCC(N[C@@H](CC1=CN=CN1)C(N[C@H](CN[C@H](C(N)=O)CC(C)C)CC(C)C)=O)=O)=O)C(C)C)=O)=O)CC1=CNC2C=CC=CC1=2)=O)CCC(N)=O
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| InChi Key |
ZHNRKEKBKBWCMF-RWWZSYIDSA-N
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| InChi Code |
InChI=1S/C56H79N15O9.C2HF3O2/c1-29(2)18-35(25-61-42(50(58)74)19-30(3)4)66-55(79)45(21-34-24-59-28-64-34)68-48(73)27-63-56(80)49(31(5)6)71-51(75)32(7)65-54(78)44(20-33-23-60-39-14-10-8-12-36(33)39)70-52(76)41(16-17-47(57)72)69-53(77)43-22-38-37-13-9-11-15-40(37)67-46(38)26-62-43;3-2(4,5)1(6)7/h8-15,23-24,28-32,35,41-45,49,60-62,67H,16-22,25-27H2,1-7H3,(H2,57,72)(H2,58,74)(H,59,64)(H,63,80)(H,65,78)(H,66,79)(H,68,73)(H,69,77)(H,70,76)(H,71,75);(H,6,7)/t32-,35-,41-,42-,43+,44-,45-,49-;/m0./s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methylpentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(3R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl]amino]pentanediamide;2,2,2-trifluoroacetic acid
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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) |
H2O : ~40 mg/mL (~32.78 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 | 0.7494 mL | 3.7471 mL | 7.4942 mL | |
| 5 mM | 0.1499 mL | 0.7494 mL | 1.4988 mL | |
| 10 mM | 0.0749 mL | 0.3747 mL | 0.7494 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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