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CAS NO.5104-49-4
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C15H13FO2 |
| Molar Mass | 244.26 |
| Density | 1.199±0.06 g/cm3(Predicted) |
| Melting Point | 110-113°C(lit.) |
| Boling Point | 376.2±30.0 °C(Predicted) |
| Flash Point | 57.7°C |
| Solubility | Soluble in DMSO (50 mg/ml), methanol (50 mg/ml), ethanol (~100 mg/ml), DMF (~100 mg/ml) |
| Vapor Presure | 2.84mmHg at 25°C |
| Appearance | White crystal |
| Color | White to off-white |
| pKa | 4.14±0.10(Predicted) |
| Storage Condition | Room Temprature |
| Refractive Index | 1.34 |
| MDL | MFCD00079303 |
| In vitro study | Tarenflurbil ((R)-Flurbiprofen) can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [ 3 H]9-cis-RA and RXRα is competitively inhibited by both unlabeled (R)-Flurbiprofen and 9-cis-RA. (R)-Flurbiprofen can interfere with the interaction between RXRα and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases Tarenflurbil ((R)-Flurbiprofen)’s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((R)-Flurbiprofen) affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing. |
| In vivo study | Effects of the early and late onset of treatment with Tarenflurbil ((R)-Flurbiprofen) are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapsing-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day). |
can inhibit prostaglandin synthesis of cyclooxygenase and analgesic, anti-inflammatory and antipyretic effects. Its anti-inflammatory and analgesic effects were 250 times and 50 times that of aspirin (also known as acetylsalicylic acid). Oral absorption is rapid, 1.5 hours after the peak blood concentration, half-life of 3.5 hours, tissue distribution, PPB is 99.4%, it can compete with drugs with high plasma protein binding rate for the effect of plasma protein. Metabolized in the liver to hydroxyflurbiprofen and its uronic acid conjugates. T1/2 is 3.5 h. Excreted by urine and feces, about 60% and 40%, respectively. Age had no significant effect on drug metabolism. Mainly used for rheumatoid arthritis, rheumatoid arthritis, ankylosing spondylitis, degenerative arthritis. It can also prevent the occurrence of aphakic cystoid mottling edema after surgical removal of the lens, and inhibit the treatment of eye inflammation after surgery of pupillary contraction, cataract and trabeculectomy argon laser. It is also suitable for pain caused by other causes such as trauma, sprain, surgery, etc.
| Anti-inflammatory analgesic | |
| toxicity | Non-steroidal anti-inflammatory drugs (NSAIDs) have anti-inflammatory, analgesic and antipyretic effects, the list of toxicity from small to large is naphtone, salenoxyl, sulindac, diclofenac, ibuprofen, ketoprofen, aspirin, naproxen, tolmetin, flurbiprofen, yantongxikang, phenoxyibuprofen, indomethacin, chloromethanoic acid. Aspirin may be the first choice for traditional NSAID drugs. If children cannot tolerate their adverse reactions during treatment, other non-steroidal anti-inflammatory drugs can be used. Selective COX-2 inhibitors have been developed that will all replace traditional NSAIDs. The listed selective COX-2 inhibitors include Nimesulide (Nimesulide), rofecoxib (vioxab), celecoxib (celecoxib), etodolac (Rodine), meloxicam, etc. A recent large-scale, international, multicenter, randomized, double-blind, prospective study showed that selective COX-2 inhibitors had few gastrointestinal and renal side effects and had no significant effect on platelet function, it can be used as the first choice for early combination therapy in children with JRA instead of aspirin. |
| adverse reactions | The most common adverse reactions were dyspepsia, stomach discomfort, etc., occasionally Head Pain, rash, etc. Peptic ulcer, bronchial asthma patients and pregnant women, lactating women should not take. other adverse reactions were Nausea, Diarrhea, Abdominal Pain, blurred vision, urinary tract infection, dermatitis and so on. A small number of liver transaminase increased, continue medication, may develop, can remain unchanged or disappear. When instilled into the eye, there was mild tingling and burning sensation and/or visual disturbance. There is a report that the bleeding time is prolonged due to the influence of platelet aggregation, and the tendency of increasing intraocular hemorrhage after the application of this drug in ophthalmic surgery is reported. In animal experiments, flurbiprofen 50~100 mg/kg, 3 months, can cause renal papillary necrosis. It can also have this effect in humans. |
| biological activity | Tarenflurbil ((R)-Flurbiprofen) is the R-type enantiomer of Flurbiprofen, tarenflurbil ((R)-Flurbiprofen) inhibited [3H]9-cis-RA binding to rxrα LBD with an IC50 of 75 μm. |
| Target | IC50: 75 μm (rxrα) |
| in vitro study | Tarenflurbil ((R)-flurbipfen) can significant reduce A beta secret, but at the same time, the level of tracellular Aβ. The binding between [ 3 H]9-cis-RA and RXR α is competitive inhibited by both unlabelled (R)-flurbiparofen and 9-cis-RA. (R)-flurbipfen can interference with the interaction between RXR α and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases Tarenflurbil ((R)-Flurbiprofen)'s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((R)-Flurbiprofen) affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing. |
| in vivo studies | Effects of the early and late on are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapse-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day). |
| Use | antipyretic, analgesic and anti-inflammatory drugs |
CAS:
5104-49-4
MF:
C15H13FO2
MW:
244.27
EINECS:
225-827-6
MDL No.:
MFCD00079303
Melting point:
110-112 °C(lit.)
Boiling point:
376.2±30.0 °C(Predicted)
Density
1.1795 (estimate)
storage temp.
Sealed in dry,Room Temperature
solubility
methanol: soluble50mg/mL
pka
pKa 3.80(H2O) (Uncertain)
form
White solid
color
white to off-white
Water Solubility
8mg/L(room temperature)
Merck
14,4199
InChIKey
SYTBZMRGLBWNTM-UHFFFAOYSA-N
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.