| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
EC50: 450 nM (FXR)[1] IC50: 160 nM (human DHODH)[3]
|
|---|---|
| ln Vitro |
Vidofludimus hemicalcium (0-1 µM) causes the recruitment of several coactivators with LXXLL motifs and selectively activates FXR in a concentration-dependent manner with an EC50 value of roughly 450 nM [1]. The nuclear translocation of p65 is blocked by inhibiting the IKK-IκB-NF-κB pathway with Vidofludimus hemicalcium (0-8 µM) [1]. With an IC50 value of 160 nM, visdofludimus hemicalcium exhibits inhibitory action against human DHODH[2]. In vitro, dihydroorotate dehydrogenase and lymphocyte proliferation are inhibited by visdofludimus hemicalcium [3]. Vidofludimus hemicalcium, regardless of its impact on lymphocyte proliferation, suppresses the release of interleukin (IL)-17 in vitro [3]. In vitro, IL-23 + IL-1β-stimulated colon strips do not produce any IL-17 secretion when vidofludimus hemicalcium is present [3].
|
| ln Vivo |
In vivo colitis produced by dextran sulfate sodium (DSS) is impacted by vidofludimus hemicalcium (ip; once daily; for 14 days) in a way that is dependent on FXR [1]. Oral Vidofludimus hemicalcium (60 mg/kg) for 6 days significantly improves several TNBS-induced colitis parameters in rats and inhibits colonic STAT3 and IL-17 [3].
|
| References |
|
| Additional Infomation |
Vidofludimus Calcium Anhydrous is the calcium salt form of vidofludimus, an orally bioavailable inhibitor of dihydroorotate dehydrogenase (DHODH), with potential anti-inflammatory, immunomodulating and anti-viral activities. Upon administration, vidofludimus specifically targets, binds to and prevents the activation of DHODH. This prevents the fourth enzymatic step in de novo pyrimidine synthesis, leading to inhibition of transcriptional elongation, cell cycle arrest, and apoptosis in activated lymphocytes. DHODH inhibition also leads to metabolic stress in activated lymphocytes and inhibition of the release of proinflammatory cytokines including interleukin (IL)-17 (IL-17A and IL-17F) and interferon-gamma (IFNg), thereby reducing inflammation. In addition, DHODH inhibition may lead to host-based anti-viral activity against many viruses. DHODH, a mitochondrial enzyme that catalyzes the conversion of dihydroorotate (DHO) to orotate, is a key enzyme in pyrimidine de novo biosynthesis. Metabolically highly activated and rapidly proliferating lymphocytes and various virus infected cells require de novo synthesis to meet their needs for pyrimidines.
|
| Molecular Formula |
C20H18CAFNO4
|
|---|---|
| Molecular Weight |
395.437628269196
|
| Exact Mass |
748.19
|
| CAS # |
1354012-90-0
|
| Related CAS # |
Vidofludimus;717824-30-1
|
| PubChem CID |
56944639
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
53
|
| Complexity |
571
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KWSJBFAXOPFZSO-UHFFFAOYSA-L
|
| InChi Code |
InChI=1S/2C20H18FNO4.Ca/c2*1-26-14-5-2-4-12(10-14)13-8-9-18(17(21)11-13)22-19(23)15-6-3-7-16(15)20(24)25;/h2*2,4-5,8-11H,3,6-7H2,1H3,(H,22,23)(H,24,25);/q;;+2/p-2
|
| Chemical Name |
calcium;2-[[2-fluoro-4-(3-methoxyphenyl)phenyl]carbamoyl]cyclopentene-1-carboxylate
|
| 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 | 2.5288 mL | 12.6441 mL | 25.2883 mL | |
| 5 mM | 0.5058 mL | 2.5288 mL | 5.0577 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5288 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
