actarit
actarit
CAS: 18699-02-0
Molecular Formula: C10H11NO3
actarit - Names and Identifiers
| Name | actarit |
| Synonyms | ms932 actarit Actarit 242-511-3 RARECHEM AL BO 1520 (p-acetamidophenyl)-aceticaci (p-acetamidophenyl)aceticacid 4-ACETAMIDO-PHENYLACETIC ACID (4-Acetamidophenyl)acetic acid 4-n-acetylaminophenylaceticacid 4-(acetylamino)-benzeneaceticaci 4-(acetylamino)-benzeneacetic acid [4-(ACETYLAMINO)PHENYL]ACETIC ACID [4-(acetylamino)phenyl]acetic acid Benzeneacetic acid, 4-(acetylamino)- |
| CAS | 18699-02-0 |
| EINECS | 242-511-3 |
| InChI | InChI=1/C10H11NO3/c1-7(12)11-9-4-2-8(3-5-9)6-10(13)14/h2-5H,6H2,1H3,(H,11,12)(H,13,14) |
actarit - Physico-chemical Properties
| Molecular Formula | C10H11NO3 |
| Molar Mass | 193.2 |
| Density | 1.288±0.06 g/cm3(Predicted) |
| Melting Point | 173-175°C |
| Boling Point | 449.1±28.0 °C(Predicted) |
| Flash Point | 225.4°C |
| Solubility | DMSO, Ethanol, Methanol |
| Vapor Presure | 7.52E-09mmHg at 25°C |
| Appearance | White or off-white crystals or crystalline solids |
| Color | White to Off-White |
| Merck | 14,133 |
| pKa | 4.34±0.10(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Refractive Index | 1.604 |
| Use | Immunomodulatory drugs |
actarit - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| RTECS | CY1542000 |
| HS Code | 29163990 |
| Toxicity | LD50 in male, female mice, male, female rats (mg/kg): 1.06, 1.30, 1.95, 2.03 i.p.; 5.68, 5.48, 5.48, 6.12 s.c.; 15.3, 14.7, 14.8, 15.4 orally (Toshida) |
actarit - Reference Information
| pharmacological action and mechanism | actari is a new non-steroidal anti-rheumatic drug has obvious anti-inflammatory effect and has good inhibitory effect on acute inflammation and adjuvant arthritis rat model. Through the study of joint lesions and immune function of type II collagen-induced arthritis in mice, it is found that actalit has obvious inhibitory effect on type II collagen-induced foot swelling in mice. In vitro studies have found that actalit can restore the hyperproliferative response of Concanavalin and the production of interleukin (I L)-2 to close to normal in type II collagen arthritis mice, and at the same time, it has a significant inhibitory effect on the excessive IL -1 production in type II collagen arthritis mice. Actarit can significantly reduce the delayed allergy induced by type II collagen, but has no significant effect on the production of antibodies in mice with type II collagen arthritis. Pathological examination showed that actarit could reduce periosteal hyperplasia and cartilage destruction in mice with type Ⅱ collagen-induced arthritis. By observing the effect of actarit on the immune enhancement caused by cyclophosphamide and the delayed type hypersensitivity (DTH) of immunosuppressive model mice, as well as the effect of actarit on the T cell subtypes of mice under the above model, actarit now has a significant inhibitory effect on the enhancement of DTH caused by high-dose cyclophosphamide, and has a recovery effect on the low DTH caused by cyclophosphamide in mice. Actalide can effectively regulate the level of T cell subtypes that are too high or too low. The number of Th Ts decreased in mice with immune enhancement caused by cyclophosphamide, but the proportion of Th decrease was greater than that of Ts, so that the Th/Ts value decreased with the increase of dose. For immunosuppressive mice caused by cyclophosphamide, actalide can make Th and Ts rise somewhat, while Ts rise more obviously, and also make Th/Ts value decrease. Therefore, actalit has a significant two-way immunomodulatory effect, which plays a role by activating the body's own T suppressor cells. The two-way immune regulation effect of actarit can reduce the production of tumor cell necrosis factor (TNF)α, IL-1β and metalloproteinase by synovial cells, reduce serum nitric oxide (NO) levels, etc., and control active rheumatoid arthritis, especially for early rheumatoid arthritis. It has a good effect on reducing synovitis, cartilage erosion and bone destruction. It also has potential effects on neuroimmune diseases such as multiple sclerosis. |
| pharmacological action | is different from the non-steroidal anti-inflammatory drugs currently used in clinical practice. actarit has no obvious anti-inflammatory effect, but it has immunomodulatory effect and has inhibitory effect on delayed hypersensitivity (DTH). Actalide has a significant inhibitory effect on the enhancement of DTH caused by large doses of cyclophosphamide, and has a recovery effect on the low DTH caused by cyclophosphamide in mice. This significant two-way immunomodulatory effect is played by regulating T cell subsets and improving the ratio of Th/Ts. The two-way immunomodulatory effect of actarit can reduce the level of serum nitric oxide (NO), control active rheumatoid arthritis, especially for early rheumatoid arthritis, and has a good effect on reducing synovitis, The effects of cartilage erosion and bone destruction also have potential effects on multiple sclerosis and other neuroimmune diseases. |
| clinical application | clinically, actarit is used to treat chronic rheumatoid arthritis. unlike other drugs for rheumatoid arthritis, actarit is an anti-rheumatoid drug that has an inhibitory effect on delayed allergic reactions. A randomized, single-blind, controlled method was used to select 75 patients with active RA. Treatment group (45 cases) actalit 100mg,3 times/d. The control group (30 cases) was treated with methotrexate (MTX) 10mg, once/w,12w as a course of treatment. The results showed that there was no significant statistical significance in the two groups at 12w (P>0.05). Actarit was better than MTX(P<0.05). Actali has a good therapeutic effect on RA patients with little side effect. |
| Biological activity | Actarit (4-acetylaminophenylacid) is an immunomodulator with oral activity, Used to treat rheumatoid arthritis. |
| use | a generation immunomodulator for rheumatoid arthritis. immunomodulatory drugs |
Last Update：2024-04-10 22:29:15
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