| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| ln Vitro |
With an IC50 of 70 nM, monomethyl fumarate totally prevents the synthesis of cAMP produced by forskolin. With an EC50 of 9.4 μM, monomethyl fumarate causes a dose-dependent Ca2+ signal in GPR109A transfected cells [1]. The cytotoxicity caused by 7β-OHC, which includes inducing cell death, decreasing cell viability, inhibiting cell growth, and disrupting mitochondria, is lessened by monomethyl fumarate (25 μM; 24 hours) [3].
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|---|---|
| ln Vivo |
In a dose-dependent way, these morphological alterations (photoreceptor loss caused by bright light exposure) are prevented by a single dose of monomethyl fumarate (50–100 mg/kg; i.p.) prior to light exposure [2]. Both oxidative stress and retinal inflammation are decreased by monomethyl fumarate (100 mg/kg). Monomethyl fumarate has the ability to strongly suppress genes that are elevated in light-induced retinopathy (LIR) through the NFkB pathway, including as Tnf-α, Nlrp3, Casp1, and Il-1β[2].
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| Animal Protocol |
Animal/Disease Models: Albino balb/c (Bagg ALBino) mouse (male, 6 weeks old) [2] Doses: 50, 65, 75, 100 mg/kg
Route of Administration: intraperitoneal (ip) injection Experimental Results: These morphological changes were prevented in one dose ( Photoreceptor death induced by bright light exposure)-dependent manner. |
| References |
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| Additional Infomation |
Monomethyl fumarate is a dicarboxylic acid monoester resulting from the formal condensation of one of the carboxy groups of fumaric acid with methanol. Is is a metabolite of dimethyl fumarate and used for the the treatment of patients with relapsing multiple sclerosis (MS). It also induces the NFE2L2 (Nrf2) transcription factor by binding to KEAP1. It has a role as an immunomodulator, an antioxidant and a drug metabolite. It is an enoate ester, a methyl ester and a dicarboxylic acid monoester. It is functionally related to a fumaric acid.
Monomethyl fumarate has been reported in Amesia nigricolor, Rothmannia longiflora, and other organisms with data available. See also: Fumaric Acid (has active moiety); Dimethyl Fumarate (active moiety of); Diroximel Fumarate (active moiety of). |
| Molecular Formula |
C5H6O4
|
|---|---|
| Molecular Weight |
130.0987
|
| Exact Mass |
130.026
|
| CAS # |
2756-87-8
|
| Related CAS # |
Monomethyl fumarate-d3;1616345-41-5;Monomethyl fumarate-d5;1616345-45-9
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| PubChem CID |
5369209
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
250.0±23.0 °C at 760 mmHg
|
| Melting Point |
144-145ºC
|
| Flash Point |
108.9±16.1 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.469
|
| LogP |
-0.24
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
9
|
| Complexity |
147
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC(=O)/C=C/C(=O)O
|
| InChi Key |
NKHAVTQWNUWKEO-NSCUHMNNSA-N
|
| InChi Code |
InChI=1S/C5H6O4/c1-9-5(8)3-2-4(6)7/h2-3H,1H3,(H,6,7)/b3-2+
|
| Chemical Name |
(E)-4-methoxy-4-oxobut-2-enoic 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) |
DMSO : ~50 mg/mL (~384.32 mM)
H2O : ~10 mg/mL (~76.86 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (19.22 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (19.22 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: 2.5 mg/mL (19.22 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 8.33 mg/mL (64.03 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.6864 mL | 38.4320 mL | 76.8640 mL | |
| 5 mM | 1.5373 mL | 7.6864 mL | 15.3728 mL | |
| 10 mM | 0.7686 mL | 3.8432 mL | 7.6864 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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