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RC-3095 (TFA) is a novel and potent bombesin/gastrin releasing peptide receptor antagonist with protective effects by reducing gastric oxidative injury in the arthritic mice.
| 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.
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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. |
| References |
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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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