Golotimod (SCV 07) HCl An immunomodulatory peptide with antimicrobial activity that significantly increases efficacy in anti-tuberculosis studies, stimulates thymic and splenocyte proliferation, and improves macrophage function. Golotimod HCl inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models receiving radiotherapy or radiotherapy in combination with cisplatin. Golotimod HCl may be used to be utilized in the research of recurrent genital herpes simplex virus type 2 (HSV-2).

Physicochemical Properties

Molecular Formula	C16H20CLN3O5
Molecular Weight	369.800103187561
Exact Mass	369.109
CAS #	1029401-59-9
Related CAS #	Golotimod;229305-39-9;Golotimod TFA;2828433-07-2
PubChem CID	154805962
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	6
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	8
Heavy Atom Count	25
Complexity	484
Defined Atom Stereocenter Count	1
SMILES	C1=CC=C2C(=C1)C(=CN2)CC(C(=O)O)NC(=O)CC[C@H](C(=O)O)N.Cl
InChi Key	YYTBHYZPAMPQGT-ZRMPQGGQSA-N
InChi Code	InChI=1S/C16H19N3O5.ClH/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);1H/t11-,13?;/m1./s1
Chemical Name	(2R)-2-amino-5-[[1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoic acid;hydrochloride
HS Tariff Code	2934.99.9001
Storage	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, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	STAT3
ln Vivo	Golotimod (SCV-07) hydrochloride, administered orally (oral gavage or subcutaneous injection, 100 μg/kg, 5 days), decreases experimental recurrent genital HSV-2 disease. Moreover, oral SCV-07 administered after fasting significantly lowers incidence and severity in female Hartley guinea pigs compared to SCV-07 administered without fasting[1]. In male LVG golden Syrian Hamsters, golotimod (SCV-07) hydrochloride (subcutaneous injection, once or twice a day, 100 μg/kg) can shorten the length of ulcerative OM and lessen the intensity and duration of acute and split radiation-induced oral mucositis (OM)[3].
Animal Protocol	Animal/Disease Models: Female Hartley guinea pigs (250-300 g) infected HSV-2[1] Doses: 100 μg/kg Route of Administration: po (oral gavage) or subcutaneous (sc)injection; 5 days Experimental Results: diminished incidence of lesions from 55% (one week before treatment) to only 18% by oral administration, and demonstrated no significant reduction in disease by subcutaneous (sc)injection of SCV-07. Animal/Disease Models: Male LVG golden Syrian Hamsters weighing approximately 80 g with radiation-induced mucositis[3] Doses: 10, 100 μg/kg or 1 mg/kg Route of Administration: subcutaneous (sc)injection; once or twice a day from days 1 to 20 Experimental Results: demonstrated 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. Dramatically diminished the severity and duration of oral mucositis (OM) at dose of 10 μg/kg, 100 μg/kg or 1 mg/kg.
References	[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.

Solubility Data

Solubility (In Vitro)	H2O : 150 mg/mL (405.62 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 20 mg/mL (54.08 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7042 mL	13.5208 mL	27.0416 mL
	5 mM	0.5408 mL	2.7042 mL	5.4083 mL
	10 mM	0.2704 mL	1.3521 mL	2.7042 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.