| Identification | Back Directory | [Name]
(R)-2-Amino-5-(((S)-1-carboxy-2-(1H-indol-3-yl)ethyl)amino)-5-oxopentanoic acid trifluoroacetate | [CAS]
2828433-07-2 | [Synonyms]
(R)-2-Amino-5-(((S)-1-carboxy-2-(1H-indol-3-yl)ethyl)amino)-5-oxopentanoic acid trifluoroacetate | [Molecular Formula]
C18H20F3N3O7 | [MOL File]
2828433-07-2.mol | [Molecular Weight]
447.37 |
| Hazard Information | Back Directory | [Uses]
Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3]. | [in vivo]
Golotimod (SCV-07) TFA (oral gavage or subcutaneous injection, 100 μg/kg, 5 days) reduces experimental recurrent genital HSV-2 disease by oral administration, more importantly, oral SCV07 after fasting shows a greater reduction in incidence and severity than SCV-07 without fasting in female hartley guinea pigs[1].
Golotimod (SCV-07) TFA (subcutaneous injection, once or twice a day from days 1 to 20, 100 μg/kg) can reduce the severity and duration of acute and split radiation-induced oral mucositis (OM) and short the duration of ulcerative OM in male LVG golden Syrian Hamsters[3].
| Animal Model: | Female Hartley guinea pigs (250-300 g) infected HSV-2[1] | | Dosage: | 100 μg/kg | | Administration: | Oral gavage or subcutaneous injection; 5 days | | Result: | Reduced incidence of lesions from 55% (one week before treatment) to only 18% by oral administration, and showed no significant reduction in disease by subcutaneous injection of SCV-07. |
| Animal Model: | Male LVG golden Syrian Hamsters weighing approximately 80 g with radiation-induced mucositis[3] | | Dosage: | 10, 100 μg/kg or 1 mg/kg | | Administration: | Subcutaneous injection; once or twice a day from days 1 to 20 | | Result: | Showed a peak mucositis of 3.0 on day 18 in the control group compared to only 2.2 in the test group, and the mucositis score in the SCV-07 treated hamsters was only 6.3% compared to 28.1% in the control group at dose of 100 μg/kg.
Significantly decreased the severity and duration of oral mucositis (OM) at dose of 10 μg/kg, 100 μg/kg or 1 mg/kg.
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| [IC 50]
STAT3 | [References]
[1] Rose WA 2nd, et al. An immunomodulating dipeptide, SCV-07, is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2). Int J Antimicrob Agents. 2008 Sep;32(3):262-6. DOI:10.1016/j.ijantimicag.2008.04.010
[2] Geiger JL, et al. The STAT3 pathway as a therapeutic target in head and neck cancer: Barriers and innovations. Oral Oncol. 2016 May;56:84-92. DOI:10.1016/j.oraloncology.2015.11.022
[3] Watkins B, et al. Attenuation of radiation- and chemoradiation-induced mucositis using gamma-D-glutamyl-L-tryptophan (SCV-07). Oral Dis. 2010 Oct;16(7):655-60. DOI:10.1111/j.1601-0825.2010.01671.x |
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