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| Targets |
Parimifasor targets ATPases. The compound is an orally bioavailable intestinal ATPase modulator that is being developed as an intestinal-directed therapy for the treatment of inflammatory bowel disease (IBD). ATPases are enzymes that hydrolyze ATP to ADP and inorganic phosphate, providing energy for various cellular processes. By modulating ATPase activity, Parimifasor may influence cellular energy metabolism, ion transport, and signaling pathways involved in inflammation. The compound exhibits anti-inflammatory activity, making it a potential therapy for IBD. Parimifasor also has antioxidant and anticancer properties. The compound's complex structure, containing chlorophenone, fluorophenone, trifluoromethylpyrazole, and amide functional groups, contributes to its biological activity.
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| ln Vitro |
Parimifasor is an immunomodulator that exhibits anti-inflammatory activity in vitro. The compound modulates ATPase activity, which may influence cellular energy metabolism and inflammatory signaling pathways. Parimifasor has been shown to possess antioxidant and anticancer properties. The compound's anti-inflammatory effects have been characterized in cell-based assays measuring cytokine production and inflammatory markers. Parimifasor is being developed as an intestinal-directed therapy for IBD, indicating that its activity is targeted to the gastrointestinal tract. The compound's mechanism of action involves modulation of ATPase activity, but the specific ATPase targets and downstream pathways are not fully characterized.
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| ln Vivo |
Parimifasor is an orally bioavailable immunomodulator that has been studied in vivo for its anti-inflammatory effects. The compound is being developed as an intestinal-directed therapy for the treatment of inflammatory bowel disease (IBD). By modulating ATPase activity in the intestine, Parimifasor may reduce intestinal inflammation and improve symptoms of IBD. The compound's anti-inflammatory, antioxidant, and anticancer properties have been evaluated in preclinical models. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical studies. Parimifasor is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
ATPase activity assays are performed using purified ATPase enzymes or membrane preparations. The enzyme is incubated with ATP in assay buffer (e.g., 50 mM Tris-HCl pH 7.5, 100 mM NaCl, 5 mM MgCl₂) at 37°C for 30-60 minutes. The inorganic phosphate released is quantified using a colorimetric assay (e.g., malachite green or molybdate assay). Parimifasor is serially diluted in DMSO and added to the reaction mixture to determine IC50 values. Each concentration is tested in duplicate, and IC50 values are calculated by non-linear regression analysis. Appropriate positive controls (e.g., known ATPase inhibitors) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cellular ATPase modulation is evaluated in intestinal epithelial cells and immune cells. Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Parimifasor at concentrations ranging from 0.1 to 10 μM for 24-72 hours. ATPase activity in cell lysates is assessed using ATPase activity assays. Cellular ATP levels are measured using luciferase-based assays. Inflammatory markers (e.g., cytokine production, NF-κB activation) are assessed by ELISA or Western blotting. Cell viability is assessed using MTT or LDH assays. Each experiment includes vehicle controls (DMSO) and appropriate positive controls to validate the assay systems.
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| Animal Protocol |
In vivo efficacy of Parimifasor is evaluated in animal models of inflammatory bowel disease, such as dextran sulfate sodium (DSS)-induced colitis or trinitrobenzene sulfonic acid (TNBS)-induced colitis. The compound is administered orally at doses determined by preclinical studies. Disease activity is assessed by measuring body weight, stool consistency, and bleeding. Colon length and histopathological analysis are performed to assess inflammation. Inflammatory markers (e.g., cytokine levels, myeloperoxidase activity) are measured in colon tissue. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 460.21. Formula: C18H11Cl2F4N5O. CAS No.: 1796641-10-5. Synonyms: Parimifasor; LYC30937; LYC-30937; LYC-30937-EC. Appearance: Solid. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Typically at -20°C. Parimifasor is a first-in-class, orally bioavailable immunomodulator with anti-inflammatory activity targeting ATPases.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Parimifasor. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As an immunomodulator and ATPase modulator, potential toxicities may include effects on cellular energy metabolism and immune function. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| Additional Infomation |
Parimifasor is also known as LYC30937, LYC-30937, and LYC-30937-EC. Its IUPAC name is not fully resolved in publicly available sources. Parimifasor is a first-in-class, orally bioavailable immunomodulator with anti-inflammatory activity. The compound is an orally bioavailable intestinal ATPase modulator being developed as an intestinal-directed therapy for the treatment of inflammatory bowel disease (IBD). Parimifasor exhibits anti-inflammatory, antioxidant, and anticancer properties. No clinical trials have been reported for this compound. Parimifasor is for research use only.
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| Molecular Formula |
C18H11CL2F4N5O
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| Molecular Weight |
460.212455034256
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| Exact Mass |
459.027
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| CAS # |
1796641-10-5
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| PubChem CID |
135565102
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| Appearance |
White to off-white solid powder
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
638
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GPLAWHGEODGIAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H11Cl2F4N5O/c19-10-3-1-2-9(4-10)16(30)27-17(25-13-6-11(20)5-12(21)7-13)26-15-8-14(28-29-15)18(22,23)24/h1-8H,(H3,25,26,27,28,29,30)
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| Chemical Name |
3-chloro-N-[N-(3-chloro-5-fluorophenyl)-N'-[5-(trifluoromethyl)-1H-pyrazol-3-yl]carbamimidoyl]benzamide
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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 |
| 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) |
DMSO : ~66.67 mg/mL (~144.87 mM)
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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 | 2.1729 mL | 10.8646 mL | 21.7292 mL | |
| 5 mM | 0.4346 mL | 2.1729 mL | 4.3458 mL | |
| 10 mM | 0.2173 mL | 1.0865 mL | 2.1729 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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