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| ln Vitro |
BDNF levels are raised by glutaramer acetate (25–100 mg/kg; Sc; 5 days)[3]. The N171-82Q transgenic mouse line, used in the huntington's disease (HD) animal model, shows a faster-moving illness course. Beginning at 8 weeks of age and continuing until 20 weeks of age, which is close to the age at which the disease would cause death, mice were given 1 mg/mouse; sc; 5×week. Several motor function assessments show improved performance when administered with glutaraldehyde acetate. The rotarod test, which is administered to 15-week-old N171-82Q transgenic mice over a 4-day period, shows a considerable improvement in performance when administered with glutaramer acetate[3].
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| References |
[1]. McKeage K. Glatiramer Acetate 40 mg/mL in Relapsing-Remitting Multiple Sclerosis: A Review. CNS Drugs. 2015;29(5):425-432.
[2]. Arnon R, et al. Mechanism of action of glatiramer acetate in multiple sclerosis and its potential for the development of new applications. Proc Natl Acad Sci U S A. 2004;101 Suppl 2(Suppl 2):14593-14598. [3]. Corey-Bloom J, et al. Beneficial effects of glatiramer acetate in Huntington's disease mouse models: Evidence for BDNF-elevating and immunomodulatory mechanisms. Brain Res. 2017;1673:102-110. [4]. Aharoni R, et al. Glatiramer acetate-specific T cells in the brain express T helper 2/3 cytokines and brain-derived neurotrophic factor in situ [published correction appears in Proc Natl Acad Sci U S A. 2005 Aug 23;102(34):12288]. Proc Natl Acad Sci U S A |
| Additional Infomation |
A random polymer of L-ALANINE, L-GLUTAMIC ACID, L-LYSINE, and L-TYROSINE that structurally resembles MYELIN BASIC PROTEIN. It is used in the treatment of RELAPSING-REMITTING MULTIPLE SCLEROSIS.
See also: Glatiramer Acetate (annotation moved to). |
| Molecular Formula |
(C9H11NO3.C6H14N2O2.C5H9NO4.C3H7NO2)X.XC2H4O2
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|---|---|
| Molecular Weight |
623.65
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| Exact Mass |
623.301
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| CAS # |
147245-92-9
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| PubChem CID |
3081884
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
385.2ºC at 760mmHg
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| Melting Point |
>239°C (dec.) (lit.)
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| Flash Point |
186.7ºC
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| Vapour Pressure |
1.27E-06mmHg at 25°C
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| LogP |
2.147
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
43
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| Complexity |
519
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(=O)O.NCCCCC(C(=O)O)N.OC(CCC(C(=O)O)N)=O.CC(C(=O)O)N.OC(C(CC1=CC=C(O)C=C1)N)=O
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| InChi Key |
FHEAIOHRHQGZPC-KIWGSFCNSA-N
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| InChi Code |
InChI=1S/C9H11NO3.C6H14N2O2.C5H9NO4.C3H7NO2.C2H4O2/c10-8(9(12)13)5-6-1-3-7(11)4-2-6;7-4-2-1-3-5(8)6(9)10;6-3(5(9)10)1-2-4(7)8;1-2(4)3(5)6;1-2(3)4/h1-4,8,11H,5,10H2,(H,12,13);5H,1-4,7-8H2,(H,9,10);3H,1-2,6H2,(H,7,8)(H,9,10);2H,4H2,1H3,(H,5,6);1H3,(H,3,4)/t8-;5-;3-;2-;/m0000./s1
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| Chemical Name |
acetic acid;(2S)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2S)-2-aminopentanedioic acid;(2S)-2-aminopropanoic acid;(2S)-2,6-diaminohexanoic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O: 50 mg/mL
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| 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 | 1.6035 mL | 8.0173 mL | 16.0346 mL | |
| 5 mM | 0.3207 mL | 1.6035 mL | 3.2069 mL | |
| 10 mM | 0.1603 mL | 0.8017 mL | 1.6035 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.
A Study in Subjects With Relapsing-Remitting Multiple Sclerosis (RRMS) to Assess the Efficacy, Safety and Tolerability of Glatiramer Acetate (GA) Injection 40 mg Administered Three Times a Week Compared to Placebo
CTID: NCT01067521
Phase: Phase 3 Status: Completed
Date: 2021-12-09
Products are for research use only; We do not sell to patients
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