research use only
Cat.No.S1764
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase |
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| Other Antineoplastic and Immunosuppressive Antibiotics Inhibitors | Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine |
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In vitro |
DMSO
: 100 mg/mL
(121.51 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 822.94 | Formula | C43H58N4O12 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 13292-46-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC-113926 | Smiles | CC1C=CC=C(C(=O)NC2=C(C(=C3C(=C2O)C(=C(C4=C3C(=O)C(O4)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C)O)O)C=NN5CCN(CC5)C)C | ||
| Targets/IC50/Ki |
RNA polymerase
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| In vitro |
Rifampin (Rifampicin) inhibits IκBα degradation and mitogen-activated protein kinase (MAPK) phosphorylation. It is found to bind to human MD-2 in a concentration-dependent manner for both the compound and MD-2. This compound inhibits NF-κB activation induced by LPS (20 ng/ml) in a dose-dependent manner, with an IC50 of 44.1 μM in Blue hTLR4 293 cells (A) and immunocompetent microgial BV-2 cell. At 50 μM, it suppresses NF-κB activation at varying LPS doses, and the maximum NF-κB level induced by LPS in its presence is much lower than that in its absence. It also inhibits NO production induced by LPS (200 ng/ml) in a dose-dependent manner in BV-2 cells, with an IC50 of 21.2 μM. Furthermore, it suppresses LPS induced TNF-α and IL-1β production in both microglia BV-2 and RAW 264.7 macrophage cells. Its inhibition of innate immune signaling is independent of the pregnane X receptor NR1I2. When combined with polyester vascular prostheses (PVP) functionalised with cyclodextrin (PVP-CD), it results in significant bacterial adhesion reduction and growth inhibition against Gram-positive bacteria. At 50 μg/mL, it significantly reduces the CFU counts of stationary-phase cultures and reduces the CFU counts of the log-phase culture to zero. It is particularly suitable since it is bactericidal and starts killing M. tuberculosis within an hour of exposure. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05685719 | Completed | COVID-19 Pneumonia |
Zhejiang ACEA Pharmaceutical Co. Ltd. |
January 4 2023 | Phase 1 |
| NCT05635110 | Completed | Pain |
Vertex Pharmaceuticals Incorporated |
December 15 2022 | Phase 1 |
| NCT05098041 | Completed | Healthy Volunteers |
Takeda |
November 22 2021 | Phase 1 |
| NCT04933682 | Completed | Healthy |
Alexion Pharmaceuticals Inc. |
June 23 2021 | Phase 1 |
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