M-5011

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MedKoo CAT#: 526877

CAS#: 76604-64-3

Description: M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg/kg, being more potent than zaltoprofen (16.80 mg/kg) and tiaprofenic acid (4.78 mg/kg), equipotent to diclofenac sodium (0.68 mg/kg), and less potent than indomethacin (0.21 mg/kg) and ketoprofen (0.28 mg/kg). M-5011 partially inhibits the generalized bone loss accompanying the development of collagen-induced arthritis in rats. M-5011 is a useful NSAID that shows potent antinociceptive effects with low ulcerogenic activities.

Chemical Structure

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M-5011
CAS# 76604-64-3
Instruction

Theoretical Analysis

MedKoo Cat#: 526877
Name: M-5011
CAS#: 76604-64-3
Chemical Formula: C14H14O2S
Exact Mass: 246.07
Molecular Weight: 246.324
Elemental Analysis: C, 68.27; H, 5.73; O, 12.99; S, 13.02

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: M-5011; M 5011; M5011; T-3788; M-5011C; S-MTPPA.

IUPAC/Chemical Name: (R)-2-(4-(3-methylthiophen-2-yl)phenyl)propanoic acid

InChi Key: DTOPKPBTCXKNFF-SNVBAGLBSA-N

InChi Code: InChI=1S/C14H14O2S/c1-9-7-8-17-13(9)12-5-3-11(4-6-12)10(2)14(15)16/h3-8,10H,1-2H3,(H,15,16)/t10-/m1/s1

SMILES Code: O=C(O)[C@H](C)C1=CC=C(C2=C(C)C=CS2)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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 246.32 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Horisawa E, Danjo K, Haruna M. Physical properties of solid dispersion of a nonsteroidal anti-inflammatory drug (M-5011) with Eudragit E. Drug Dev Ind Pharm. 2000 Dec;26(12):1271-8. PubMed PMID: 11147127.

2: Taguchi K, Konishi T, Nishikawa H, Kitamura S. Identification of human cytochrome P450 isoforms involved in the metabolism of S-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid. Xenobiotica. 1999 Sep;29(9):899-907. PubMed PMID: 10548450.

3: Murakami N, Aihara S, Iwata K, Saito T, Naruse T. Effect of a novel non-steroidal anti-inflammatory drug (M-5011) on cytokine levels in rats with monosodium urate crystal- induced pleurisy. Jpn J Pharmacol. 1999 Apr;79(4):439-46. PubMed PMID: 10361883.

4: Konishi T, Nishikawa H, Kitamura S, Tatsumi K. In vivo studies on chiral inversion and amino acid conjugation of 2-[4-(3-methyl-2-thienyl)phenyl]propionic acid in rats and dogs. Drug Metab Dispos. 1999 Jan;27(1):158-60. PubMed PMID: 9884325.

5: Tanaka K, Tanaka H, Kanemoto Y, Tsuboi I. The effects of nonsteroidal anti-inflammatory drugs on immune functions of human peripheral blood mononuclear cells. Immunopharmacology. 1998 Nov;40(3):209-17. PubMed PMID: 9858064.

6: Murakami N, Takase H, Saito T, Iwata K, Miura H, Naruse T. Effects of a novel non-steroidal anti-inflammatory drug (M-5011) on bone metabolism in rats with collagen-induced arthritis. Eur J Pharmacol. 1998 Jul 3;352(1):81-90. PubMed PMID: 9718271.

7: Konishi T, Nishikawa H, Kitamura S, Tatsumi K. Stereoselective determination of R,S-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid and its taurine conjugates in dog urine by high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl. 1998 May 8;709(1):105-11. PubMed PMID: 9653931.

8: Konishi T, Okada S, Nishikawa H, Esumi Y, Kitamura S, Tatsumi K. Disposition of a new nonsteroidal anti-inflammatory agent, S-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid, in rats, dogs and monkeys. Arzneimittelforschung. 1998 Mar;48(3):266-74. PubMed PMID: 9553685.

9: Kido H, Murakami N, Ito A, Kimura K, Kodera N, Doi T, Naruse T. Anti-inflammatory, analgesic and anti-pyretic effects of d-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid (M-5011), a new non-steroidal anti-inflammatory drug, in rats and guinea pigs. Jpn J Pharmacol. 1998 Jan;76(1):75-86. PubMed PMID: 9517407.

10: Ichikawa Y, Nakajima M, Azuma T. [Late phase II clinical study of M-5011C on rheumatoid arthritis--a multi-institutional double-blind, three group comparative, dose finding study]. Ryumachi. 1997 Dec;37(6):851-66. Japanese. PubMed PMID: 9492574.

11: Kondo S, Nakajima M, Azuma T. [Late phase II clinical study of M-5011C on osteoarthritis--a multi-institutional double-blind, three group comparative, dose finding study]. Ryumachi. 1997 Dec;37(6):835-50. Japanese. PubMed PMID: 9492573.

12: Tobetto K, Yamamoto Y, Kataoka M, Ando T, Sugimoto K, Himeno M. The effects of a newly developed nonsteroidal anti-inflammatory drug (M-5011) on arachidonic acid metabolism in rheumatoid synovial fibroblasts. Jpn J Pharmacol. 1997 Dec;75(4):371-9. PubMed PMID: 9469643.

13: Kataoka M, Tonooka K, Ando T, Imai K, Aimoto T. Hydroxyl radical scavenging activity of nonsteroidal anti-inflammatory drugs. Free Radic Res. 1997 Oct;27(4):419-27. Erratum in: Free Radic Res 1998 Jan;28(1):108. PubMed PMID: 9416470.

14: Murakami N, Takase H, Tomita T, Iwata K, Naruse T. Antinociceptive activity of a novel non-steroidal anti-inflammatory drug (M-5011) with low ulcerogenic effects in mice. Jpn J Pharmacol. 1996 Sep;72(1):29-37. PubMed PMID: 8902597.