| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
STAT3
|
|---|---|
| ln Vivo |
Golotimod (SCV-07) TFA, 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) TFA (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 |
|
| Molecular Formula |
C18H20F3N3O7
|
|---|---|
| Molecular Weight |
447.362515449524
|
| Exact Mass |
447.125
|
| CAS # |
2828433-07-2
|
| Related CAS # |
Golotimod;229305-39-9;Golotimod hydrochloride;1029401-59-9
|
| PubChem CID |
138911395
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
31
|
| Complexity |
568
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C1=CC=C2C(=C1)C(=CN2)C[C@@H](C(=O)O)NC(=O)CC[C@H](C(=O)O)N.C(=O)(C(F)(F)F)O
|
| InChi Key |
ZPZLJEOSWDKEOP-YLAFAASESA-N
|
| InChi Code |
InChI=1S/C16H19N3O5.C2HF3O2/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;3-2(4,5)1(6)7/h1-4,8,11,13,18H,5-7,17H2,(H,19,20)(H,21,22)(H,23,24);(H,6,7)/t11-,13+;/m1./s1
|
| Chemical Name |
(2R)-2-amino-5-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoic acid;2,2,2-trifluoroacetic acid
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2353 mL | 11.1767 mL | 22.3534 mL | |
| 5 mM | 0.4471 mL | 2.2353 mL | 4.4707 mL | |
| 10 mM | 0.2235 mL | 1.1177 mL | 2.2353 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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