Golotimod targets the immune system, specifically activating macrophages and enhancing their antimicrobial activity. It stimulates the production of pro-inflammatory cytokines including TNF-α, IL-1β, and IL-6. The compound also enhances the activity of natural killer (NK) cells and promotes the differentiation of T cells. Its immunomodulatory effects are mediated through interaction with Toll-like receptors and activation of NF-κB signaling pathways.

In vitro, golotimod demonstrates immunomodulatory activity by activating macrophages and stimulating cytokine production. It enhances the phagocytic activity of macrophages and increases their ability to kill intracellular pathogens. The compound shows activity against Mycobacterium tuberculosis in infected macrophage cultures. Specific EC₅₀ values for immune activation are documented in the literature. It also shows antiviral activity against various viruses in cell-based assays.

Significantly, oral SCV-07 (oral gavage or subcutaneous injection, 100 μg/kg, 5 days) was found to be more effective than SCV Greater incidence and reduced severity -07 when administered after fasting in female Hartley guinea pigs [1]. Golotimod (SCV-07) is a medication used to treat experimental recurrent genital HSV-2 disease. In male LVG golden Syrian hamsters, golotimod (SCV-07) (subcutaneous injection, 100 μg/kg once or twice daily on days 1 to 20) shortens the length of ulcers and lessens the severity and severity of acute and chronic oral radiation mucositis (OM)[3].
In vivo, golotimod has been studied in animal models of infectious diseases, including tuberculosis and viral infections. It enhances immune function and reduces bacterial or viral load in infected animals. The compound has been evaluated in clinical trials for the treatment of tuberculosis and other infectious diseases. It shows potential as an adjunctive therapy to enhance the efficacy of standard antimicrobial treatments.

In vitro immune cell activation assays are performed using primary macrophages, dendritic cells, or peripheral blood mononuclear cells (PBMCs). Cells are treated with golotimod at various concentrations. Cytokine production is measured by ELISA. Phagocytic activity is assessed using fluorescently labeled bacteria or beads. Cell surface marker expression is analyzed by flow cytometry. The compound is dissolved in appropriate aqueous buffers for cellular experiments.

In vitro cellular assays use immune cell lines such as THP-1 macrophages or primary human PBMCs. Cells are cultured in appropriate media with supplements at 37°C in 5% CO₂. Golotimod is tested at various concentrations. Endpoints include cytokine production (TNF-α, IL-1β, IL-6), phagocytic activity, and cell viability. Antimicrobial activity is assessed in infected macrophage cultures using colony counting or fluorescence-based detection.

Animal/Disease Models: Female Hartley guinea pig (250-300 g) infected with HSV-2[1]
Doses: 100 μg/kg
Route of Administration: po (oral gavage) or subcutaneous injection; 5-day
Experimental Results: Oral administration diminished the incidence of lesions from 55 % (1 week before treatment) was diminished to only 18%, whereas subcutaneous injection of SCV-07 did not Dramatically reduce the incidence of lesions.

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Animal/Disease Models: Male LVG golden Syrian hamster, weighing about 80 grams, suffering from radiation mucositis [3]
Doses: 10, 100μg/kg or 1mg/kg
Route of Administration: subcutaneous injection; 200mg/kg. Once or twice (two times) daily from day 1 to day 20
Experimental Results: On day 18, the control group had a peak mucositis score of 3.0, while the test group had only 2.2, and the SCV-07-treated hamsters had a mucositis score of only 6.3%. At a dose of 100 μg/kg, the mortality rate in the control group was diminished to 28.1%. Doses of 10 μg/kg, 100 μg/kg or 1 mg/kg Dramatically diminished the severity and duration of oral mucositis (OM).
In vivo efficacy is evaluated in animal models of infectious diseases, including murine models of tuberculosis, bacterial infections, and viral infections. Golotimod is administered orally, intraperitoneally, or subcutaneously. Endpoints include survival rates, bacterial or viral load in tissues, immune cell activation, and histopathological assessment. Clinical studies have been conducted to evaluate safety and efficacy in humans.

Golotimod (SCV07) has a dipeptide structure. It is soluble in aqueous buffers and is stable under physiological conditions. The compound is orally bioavailable and has been studied in clinical trials as an oral formulation. Specific pharmacokinetic parameters (half-life, Cmax, bioavailability) are documented in the literature from clinical studies. It is metabolized through normal peptide degradation pathways and excreted primarily in urine.

Specific toxicity data for golotimod are documented in preclinical and clinical studies. The compound is generally well-tolerated with a favorable safety profile. Common adverse effects are mild and may include gastrointestinal disturbances. No significant organ toxicity has been reported at therapeutic doses. The compound has been studied in clinical trials for the treatment of tuberculosis and other infectious diseases, demonstrating acceptable safety and tolerability.

[1]. 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.

[2]. The STAT3 pathway as a therapeutic target in head and neck cancer: Barriers and innovations. Oral Oncol. 2016 May;56:84-92.

[3]. Attenuation of radiation- and chemoradiation-induced mucositis using gamma-D-glutamyl-L-tryptophan (SCV-07). Oral Dis. 2010 Oct;16(7):655-60.

Golotimod is a dipeptide. SCV-07 (γ-D-glutamyl-L-tryptophan) is a novel synthetic dipeptide that acts broadly on the Toll-like receptor pathway. Studies have shown that it stimulates T lymphocyte differentiation, macrophage phagocytosis, and specific immune responses, and enhances the production of IL-2 and INF-γ. Due to its preferential activation of Th1 cytokine production, SCV-07 may have potential applications in the treatment of tuberculosis. It can be administered orally or subcutaneously. In independent studies, treatment of tuberculosis with SCV-07 improved mycobacterial clearance, promoted cavity healing, improved immune markers, and alleviated symptoms (fever, fatigue, sweating, dry cough, sputum production, dyspnea, chest pain, tachycardia) without any observed local or systemic adverse reactions. SCV-07 has shown efficacy in treating various viral and bacterial infections. Glottimod is a highly bioavailable synthetic peptide composed of D-glutamine and L-tryptophan linked by γ-glutamyl, possessing potential immunostimulatory, antibacterial, and antitumor activities. Although its exact mechanism of action is unclear, glottimod appears to inhibit STAT-3 expression, thereby reversing immunosuppression and stimulating antitumor immune responses. The drug may stimulate the production of T lymphocytes (especially helper T cells (Th1 cells)), activate macrophages, and increase the levels of interleukin-2 and interferon-γ. STAT-3 is a transcription factor upregulated in various cancer cell types, involved in tumor cell growth, survival, and immunosuppression.

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Drug Indications
It has been investigated for the treatment of hepatitis (viral, hepatitis C), infectious and parasitic diseases (not specified), and tuberculosis.

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Mechanism of Action
SCV-07 (γ-D-glutamyl-L-tryptophan) has broad effects on the Toll-like receptor (TLR) pathway.

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Pharmacodynamics
SCV-07 (γ-D-glutamyl-L-tryptophan) is a novel synthetic dipeptide that acts extensively on the Toll-like receptor pathway. Studies have shown that it can stimulate T lymphocyte differentiation, macrophage phagocytosis, and specific immune responses, and enhance the production of IL-2 and IFN-γ.

Golotimod (SCV07) is an immunomodulatory dipeptide studied for the treatment of infectious diseases including tuberculosis and viral infections. It activates macrophages and enhances antimicrobial activity through stimulation of cytokine production and immune cell activation. The compound has been evaluated in clinical trials as an adjunctive therapy to enhance the efficacy of standard antimicrobial treatments. It represents a novel approach to immunotherapy for infectious diseases by harnessing the body's own immune system to fight infections.

C16H19N3O5

333.33916

333.132

229305-39-9

Golotimod hydrochloride;1029401-59-9;Golotimod TFA;2828433-07-2

6992140

White to off-white solid powder

1.428g/cm3

737.3ºC at 760 mmHg

399.7ºC

7.99E-23mmHg at 25°C

1.659

1.563

5

6

8

24

484

2

C1=CC=C2C(=C1)C(=CN2)C[C@@H](C(=O)O)NC(=O)CC[C@H](C(=O)O)N

CATMPQFFVNKDEY-YPMHNXCESA-N

InChI=1S/C16H19N3O5/c17-11(15(21)22)5-6-14(20)19-13(16(23)24)7-9-8-18-12-4-2-1-3-10(9)12/h1-4,8,11,13,18H,5-7,17H2,(H,19,20)(H,21,22)(H,23,24)/t11-,13+/m1/s1

(R)-2-amino-5-(((S)-1-carboxy-2-(1H-indol-3-yl)ethyl)amino)-5-oxopentanoic acid

SCV 07 SCV-07 SCV07 gammaDglutamylLtryptophan.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~125 mg/mL (~374.99 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)