Actarit | CAS# 18699-02-2 | Arthritis-treating drug

MedKoo Cat#: 571534 | Name: Actarit

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Actarit is a drug that has been shown to suppress disease activity of rheumatoid arthritis (RA). Actarit reduces spontaneous tumor necrosis factor-alpha and interleukin 1beta secretion by primary synovial cells of patients with RA. Actarit likely acts on RA synovial cells to reduce cell-cell interactions with autologous synovium infiltrating lymphocytes and to inhibit proinflammatory cytokine and MMP production, leading to amelioration of symptoms of RA.

Chemical Structure

Actarit

CAS#18699-02-0

Theoretical Analysis

MedKoo Cat#: 571534

Name: Actarit

CAS#: 18699-02-0

Chemical Formula: C10H11NO3

Exact Mass: 193.0739

Molecular Weight: 193.20

Elemental Analysis: C, 62.17; H, 5.74; N, 7.25; O, 24.84

Price and Availability

Size	Price	Availability
5g	USD 350.00	2 Weeks
10g	USD 550.00	2 Weeks
25g	USD 850.00	2 Weeks

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Related CAS #

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Synonym

Actarit; NSC 170317; NSC-170317; NSC170317

IUPAC/Chemical Name

2-(4-acetamidophenyl)acetic acid

InChi Key

MROJXXOCABQVEF-UHFFFAOYSA-N

InChi Code

InChI=1S/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)

SMILES Code

O=C(O)CC1=CC=C(NC(C)=O)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

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Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 193.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Takeba Y, Suzuki N, Wakisaka S, Nagafuchi H, Mihara S, Kaneko A, Asai T, Sakane T. Effects of actarit on synovial cell functions in patients with rheumatoid arthritis. J Rheumatol. 1999 Jan;26(1):25-33. PubMed PMID: 9918236. 2: Fujisawa H, Nishimura T, Motonaga A, Inoue Y, Inoue K, Suzuka H, Yoshifusa H, Kimura K, Muramatsu M. Effect of actarit on type II collagen-induced arthritis in mice. Arzneimittelforschung. 1994 Jan;44(1):64-8. PubMed PMID: 8135880. 3: Loya P, Saraf MN. Determination of actarit from human plasma for bioequivalence studies. Indian J Pharm Sci. 2010 Nov;72(6):726-31. doi: 10.4103/0250-474X.84581. PubMed PMID: 21969744; PubMed Central PMCID: PMC3178973. 4: Canudas N, Figueroa L, Zamora D, Villamizar JE, Guedez A, Fuentes JM, Castelli C, Taddei A. Photosensitizing properties of Actarit, an antirheumatic drug. Arzneimittelforschung. 2008;58(4):182-7. doi: 10.1055/s-0031-1296490. PubMed PMID: 18540480. 5: Sakurai T, Iso T, Inoue H, Sano K, Takeuchi K, Takagishi K. [Effect of actarit combination therapy in patients with active rheumatoid arthritis resistant to gold agents]. Ryumachi. 2001 Jun;41(3):635-45. Japanese. PubMed PMID: 11505513. 6: Kawai K, Kobayashi Y, Hirayama M, Shiratori M, Sobue G. Suppressive effects of 4-acetylaminophenylacetic acid (actarit) on experimental autoimmune encephalomyelitis in rats. Immunopharmacology. 1998 May;39(2):127-38. PubMed PMID: 9716259. 7: Kawada A, Hiruma M, Miura Y, Noguchi H, Akiyama M, Ishibashi A. Photosensitivity due to actarit. Contact Dermatitis. 1997 Mar;36(3):175-6. PubMed PMID: 9145282. 8: Ye J, Wang Q, Zhou X, Zhang N. Injectable actarit-loaded solid lipid nanoparticles as passive targeting therapeutic agents for rheumatoid arthritis. Int J Pharm. 2008 Mar 20;352(1-2):273-9. Epub 2007 Oct 22. PubMed PMID: 18054182. 9: Ramakrishna R, Bhateria M, Puttrevu SK, Durga Prasad Y, Singh R, Bhatta RS. A liquid chromatography-tandem mass spectrometry method for the quantitation of actarit in rabbit plasma: application to pharmacokinetics and metabolic stability. J Mass Spectrom. 2016 Jan;51(1):69-78. doi: 10.1002/jms.3730. PubMed PMID: 26757074. 10: Abiramasundari A, Joshi RP, Jalani HB, Sharma JA, Pandya DH, Pandya AN, Sudarsanam V, Vasu KK. Stability-indicating assay method for determination of actarit, its process related impurities and degradation products: Insight into stability profile and degradation pathways(☆). J Pharm Anal. 2014 Dec;4(6):374-383. doi: 10.1016/j.jpha.2014.01.002. Epub 2014 Jan 25. PubMed PMID: 29403903; PubMed Central PMCID: PMC5761480. 11: Nakamura H, Ueki Y, Sakito S, Matsumoto K, Yano M, Miyake S, Tominaga Y, Eguchi K. Clinical effects of actarit in rheumatoid arthritis: improvement of early disease activity mediated by reduction of serum concentrations of nitric oxide. Clin Exp Rheumatol. 2000 Jul-Aug;18(4):445-50. PubMed PMID: 10949718. 12: Aso M, Tanaka Y, Saito K, Fujii K, Takazawa A, Ota T, Eto S. Additive combination of actarit and methotrexate in the treatment of refractory rheumatoid arthritis. Mod Rheumatol. 2000 Jun;10(2):103-9. doi: 10.3109/s101650050007. PubMed PMID: 24383564. 13: Fujisawa H, Nishimura T, Inaba M, Ikehara S. Suppressive effect of actarit on IgA production in mice: activation of CD4+ suppressor T-cells in Peyer's patches. Int J Immunopharmacol. 1995 Jul;17(7):611-7. PubMed PMID: 8586490. 14: Nagaoka S, Ohno M, Ishigatsubo Y. Usefulness of actarit in elderly rheumatoid arthritis. Mod Rheumatol. 2002 Jun;12(2):118-27. doi: 10.3109/s101650200021. PubMed PMID: 24383899. 15: Tanaka H, Abe T, Nishimura S, Sakai H, Kimura H, Oki M, Nojima M, Taga M, Matsumoto S, Takahashi H, Imai K. [A case of rheumatoid arthritis/Sjogren's syndrome with acute renal failure due to hyperuricemia associated with mizoribine therapy]. Nihon Rinsho Meneki Gakkai Kaishi. 2004 Jun;27(3):171-6. Review. Japanese. PubMed PMID: 15291254. 16: Kawasaki Y, Moriyama M, Shibata K, Gomita Y. [Examination of the escape phenomenon in disease modifying antirheumatic drugs]. Yakugaku Zasshi. 2005 Mar;125(3):293-7. Japanese. PubMed PMID: 15738628. 17: Minami M, Kato S, Hirachi K, Nagai M. A total wrist arthroplasty in rheumatoid arthritis: a case followed for 24 years. Mod Rheumatol. 2004 Dec;14(6):488-93. doi: 10.3109/s10165-004-0345-y. PubMed PMID: 24387729. 18: Ruether F, Sadowski G. Modeling the solubility of pharmaceuticals in pure solvents and solvent mixtures for drug process design. J Pharm Sci. 2009 Nov;98(11):4205-15. doi: 10.1002/jps.21725. PubMed PMID: 19283772. 19: Higuchi M, Sakai Y, Koyanagi M, Tsuda Y, Motomura S. [Eosinophilic meningoencephalitis in a case of rheumatoid arthritis]. Nihon Rinsho Meneki Gakkai Kaishi. 1998 Dec;21(5):198-205. Japanese. PubMed PMID: 11155592. 20: Yoshida K, Kurosaka D, Ozawa Y, Yokoyama T, Tajima N. [A case of rheumatoid arthritis associated with autoimmune hemolytic anemia due to weekly low-dose methotrexate therapy]. Ryumachi. 2000 Aug;40(4):693-8. Japanese. PubMed PMID: 11021173.

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ACT-660602