| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
DP
Pizuglanstat targets hematopoietic prostaglandin D synthase (H-PGDS). H-PGDS is an enzyme that catalyzes the conversion of prostaglandin H2 (PGH2) to prostaglandin D2 (PGD2). PGD2 is involved in various physiological and pathological processes, including inflammation, allergy, and muscle degeneration. Inhibition of H-PGDS reduces PGD2 production, which may have therapeutic benefits in Duchenne muscular dystrophy and other myodegenerative diseases. |
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| ln Vitro |
Pizuglanstat demonstrates potent inhibition of human hematopoietic prostaglandin D synthase (H-PGDS) with an IC50 of 76 nM. This enzymatic inhibition is highly selective for H-PGDS. The compound's potency is characterized in enzyme inhibition assays using recombinant H-PGDS. Its ability to block PGD2 production in vitro has been confirmed. The compound is a potent, selective prostaglandin D synthase inhibitor.
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| ln Vivo |
Pizuglanstat has been investigated for its therapeutic potential in Duchenne muscular dystrophy (DMD) and other myodegenerative diseases. In vivo studies have demonstrated its ability to inhibit H-PGDS and reduce PGD2 levels in animal models. The compound's efficacy in improving muscle function and reducing muscle degeneration has been evaluated in preclinical studies. It is a promising candidate for DMD research. Detailed efficacy data are limited in publicly available sources.
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| Enzyme Assay |
H-PGDS enzyme inhibition assays are performed using recombinant human H-PGDS enzyme. The enzyme is incubated with the substrate prostaglandin H2 (PGH2) in assay buffer. The reaction product prostaglandin D2 (PGD2) is quantified by ELISA or LC-MS/MS. Test compounds are serially diluted and added to the reaction mixture. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate. Appropriate positive controls (known H-PGDS inhibitors) and vehicle controls are included.
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| Cell Assay |
Cellular H-PGDS inhibition is evaluated in cell lines expressing H-PGDS, such as mast cells, macrophages, or transfected cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and stimulated to produce PGD2 (e.g., by calcium ionophore or IgE cross-linking). Cells are treated with Pizuglanstat at various concentrations (0.01-100 μM) for 1-24 hours. PGD2 levels in the culture supernatant are measured by ELISA. Cell viability is assessed using MTT or LDH assays. Each experiment includes positive controls (known H-PGDS inhibitors) and vehicle controls.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of Duchenne muscular dystrophy, such as the mdx mouse model. Pizuglanstat is administered orally at doses typically ranging from 1-30 mg/kg/day. Muscle function is assessed by grip strength, treadmill running, and other functional tests. Muscle tissue is collected for histopathological analysis (H&E staining, fibrosis assessment) and biochemical assays (PGD2 levels, inflammatory markers). Body weight and clinical signs are monitored throughout the study. Sample sizes typically range from 8-12 animals per group.
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| ADME/Pharmacokinetics |
Pizuglanstat has a molecular weight of 508.61 g/mol and a molecular formula of C27H36N6O4. Solubility: DMSO. Storage: typically at -20°C. Bioavailability, half-life, and tissue distribution data are not publicly available. The compound is a research tool for studying H-PGDS inhibition and its therapeutic potential in myodegenerative diseases.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for Pizuglanstat. As an H-PGDS inhibitor, potential toxicities would need to be characterized. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on muscle function and inflammation. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Pizuglanstat is also known as TAS-205. Its chemical name is 4-(1-Methyl-1H-pyrrole-2-carbonyl)-N-(4-(4-(morpholine-4-carbonyl)piperidin-1-yl)phenyl)piperazine-1-carboxamide. It is a potent and selective H-PGDS inhibitor with an IC50 of 76 nM. It has been investigated for Duchenne muscular dystrophy and other myodegenerative diseases. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C27H36N6O4
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|---|---|
| Molecular Weight |
508.612545967102
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| Exact Mass |
508.28
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| Elemental Analysis |
C, 63.76; H, 7.13; N, 16.52; O, 12.58
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| CAS # |
1244967-98-3
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| PubChem CID |
46911296
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| Appearance |
White to light yellow solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
797
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZNFJGCDCPYTEKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H36N6O4/c1-29-10-2-3-24(29)26(35)31-13-15-33(16-14-31)27(36)28-22-4-6-23(7-5-22)30-11-8-21(9-12-30)25(34)32-17-19-37-20-18-32/h2-7,10,21H,8-9,11-20H2,1H3,(H,28,36)
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| Chemical Name |
4-(1-methylpyrrole-2-carbonyl)-N-[4-[4-(morpholine-4-carbonyl)piperidin-1-yl]phenyl]piperazine-1-carboxamide
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| Synonyms |
Pizuglanstat
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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: ~12.5 mg/mL (~24.6 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 | 1.9661 mL | 9.8307 mL | 19.6614 mL | |
| 5 mM | 0.3932 mL | 1.9661 mL | 3.9323 mL | |
| 10 mM | 0.1966 mL | 0.9831 mL | 1.9661 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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