RS 17053 free base
Based on 1 publication(s) in Google Scholar
RS 17053 free base is a selective α1A-adrenoceptor antagonist. RS 17053 free base binds to MrcA/MecA A-class penicillin-binding proteins, inhibits peptidoglycan biosynthesis, and binds to α1A and α1B/α1D-adrenoceptors. RS 17053 free base disrupts bacterial membranes, causing depolarization, ATP depletion, protein leakage, ROS accumulation, and upregulation of stress response genes. RS 17053 free base exerts bactericidal activity against Gram-positive/Gram-negative pathogens. RS 17053 free base can be used for research on bacterial infections and benign prostatic hyperplasia.
For research use only. We do not sell to patients.
- CAS No.: 169506-22-3
- Formula: C24H29ClN2O2
- Molecular Weight:412.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) RS 17053 free base
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
Description
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α1A-adrenergic receptor |
α1B-adrenergic receptor |
α1D-adrenergic receptor |
penicillin-binding proteins |
In Vitro
RS 17053 free base exhibits activity against Brucella spp. in the disk diffusion method[1].
RS 17053 free base has rapid bactericidal activity against Brucella spp.[1].
RS 17053 free base causes cell wall rupture and lysis in Brucella melitensis TZ[1].
RS 17053 free base exhibits bactericidal activity against S. typhimurium SL1344 and MRSA ATCC 43300[1].
RS 17053 free base damages the cell wall membrane of MRSA and causes lysis[1].
RS 17053 free base disrupts the membrane integrity of S. typhimurium SL1344 and MRSA ATCC 43300[1].
RS 17053 free base inhibits nascent peptidoglycan synthesis in S. typhimurium SL1344 and MRSA ATCC 43300[1].
RS 17053 free base reduces S. typhimurium peptidoglycan levels by 98% and MRSA by 96%[1].
RS 17053 free base inhibits Staphylococcus aureus MW2 with an MIC of 8 µg/mL and exhibits activity against multiple drug-resistant Gram-positive isolates[4].
RS 17053 free base increases the NADH/NAD+ ratio in Staphylococcus aureus ATCC 29213[4].
RS 17053 free base depolarizes and permeabilizes the membrane of Staphylococcus aureus MW2 at active concentrations[4].
RS 17053 free base distinguishes two [3H]-Prazosin (HY-B0193) binding components in wild-type mouse brain cortex slices, with pKi values of 8.8 and 7.7, respectively[2].
RS 17053 free base antagonizes norepinephrine-induced contraction in wild-type mouse prostate with a pKB of 6.9[2].
RS 17053 free base binds to human cloned α1a, α1b, and α1d adrenergic receptors with pKi values of 8.90, 7.10, and 7.20, respectively[3].
RS-17053 (0.1-1000 µM) free base antagonizes Phenylephrine (HY-B0769)-induced contraction of isolated rabbit prostate strips, with a pKB of 6.32[3].
RS 17053 free base antagonizes norepinephrine-induced contraction of isolated rabbit prostate strips, with a pKB of 6.7[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 murine macrophages and THP-1 human monocytes
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Concentration:10, 100, and 200 μM
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Incubation Time:24 h
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Result:Did not induce cytotoxicity at 10 μM.
Significantly inhibited cell viability at high concentrations (100 μM and 200 μM).
In Vivo
RS 17053 (10 mg/kg/day; i.m.; once daily; starting 3 hours after infection for 5 consecutive days) free base improves the survival rate of S. typhimurium-infected BALB/c mice and reduces the liver bacterial burden by 4.5 log10 CFU[1].
RS 17053 (10 mg/kg/day; i.m.; once daily; starting 3 hours post-infection for 5 consecutive days) free base improves the survival rate of infected BALB/c mice and reduces the splenic MRSA burden by 3.8 log10 CFU[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, 18 g)[1]
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Dosage:10 mg/kg/day
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Administration:i.m.; once daily; 5 consecutive days starting 3 hours after infection
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Result:Reduced splenic bacterial burden by >2 log10 CFU/mL compared with infected untreated mice.
Significantly restored the body weight of infected mice and alleviated the symptom of splenomegaly.
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Animal Model:BALB/c (female, 6-8 weeks old, 18 g)[1]
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Dosage:10 mg/kg/day
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Administration:i.m.; once daily; 5 consecutive days starting 3 hours after infection
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Result:Produced a mean reduction of 4.5 log10 CFU/liver compared with PBS.
The hazard ratio for death was 0.12 (95% CI 0.03-0.41).
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Animal Model:BALB/c (female, 6-8 weeks old, 18 g)[1]
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Dosage:10 mg/kg/day
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Administration:i.m.; once daily; 5 consecutive days starting 3 hours after infection
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Result:Produced a mean reduction of 3.8 log10 CFU/spleen compared with PBS.
The hazard ratio for death was 0.09 (95% CI 0.02-0.38).
Chemical Information
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CAS No. 169506-22-3
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Molecular Weight 412.96
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Formula C24H29ClN2O2
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SMILES
ClC=1C=CC=2NC=C(C2C1)CC(NCCOC=3C=CC=CC3OCC4CC4)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RS 17053 free base Related Classifications
HY-101336A Related Classifications
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Keywords
- RS 17053
- 169506-22-3
- RS17053
- RS-17053
- Adrenergic Receptor
- Penicillin-binding protein (PBP)
- Reactive Oxygen Species (ROS)
- Bacterial
- Beta Receptor
- Brucella
- Gram-positive bacteria
- MRSA
- Salmonella typhimurium
- benign prostatic hyperplasia
- membrane depolarization
- penicillin-binding proteins
- peptidoglycan biosynthesis
- α1A-adrenoceptor
- α1L-adrenoceptor
- Inhibitor
- inhibitor
- inhibit