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| Targets |
Soluble Guanylate Cyclase[1]
Soluble guanylate cyclase (sGC). Zagociguat is a stimulator of sGC. By activating this enzyme, it increases the production of cGMP, a key second messenger in the NO signaling pathway. This pathway is involved in various physiological processes, including vasodilation, neurotransmission, and neuroprotection. Its ability to penetrate the CNS makes it relevant for neurological applications. |
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| ln Vitro |
Zagociguat is a stimulator of soluble guanylate cyclase (sGC), enhancing NO signaling and increasing cGMP production. By activating this enzyme, it potentiates the effects of NO, which can lead to vasodilation and other downstream effects. Its activity is being explored for its potential to treat neurodegenerative diseases by improving neuronal function and survival.
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| ln Vivo |
In vivo, Zagociguat is being investigated for its potential to treat serious neurodegenerative disorders. By stimulating sGC and increasing cGMP production in the brain, it may improve cognitive function and slow disease progression. Its central nervous system penetrance is a key feature that enables it to exert its effects on the brain.
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| Enzyme Assay |
The activity of Zagociguat is typically assessed using enzyme activity assays with purified sGC. The enzyme is incubated with its substrate, GTP, in the presence of the compound, and the production of cGMP is measured. This allows for the determination of the compound's potency as an sGC stimulator. Binding assays can also be used to study its interaction with the enzyme.
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| Cell Assay |
Cellular assays for sGC stimulators involve treating cells that express sGC, such as neuronal or vascular cells, with the compound. The increase in intracellular cGMP levels is then measured as a readout of sGC activation. This confirms that the compound can effectively penetrate cells and stimulate sGC activity in a relevant biological context.
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| Animal Protocol |
In vivo efficacy of Zagociguat is being evaluated in preclinical and clinical studies for neurodegenerative diseases. Animal models of Alzheimer's disease or other cognitive disorders are used to assess the compound's effects on cognitive function, neuroinflammation, and neuronal survival. Its ability to penetrate the CNS is a critical factor for its efficacy in these models.
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| ADME/Pharmacokinetics |
Zagociguat is a small molecule with the molecular formula C16H10F4N6 and a molecular weight of 362.28. It is soluble in DMSO. As a CNS-penetrant compound, its pharmacokinetic properties, such as oral bioavailability and brain penetration, are key features. It is being developed for the treatment of neurological disorders.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for Zagociguat. As a therapeutic candidate for neurodegenerative diseases, its safety profile is a critical area of investigation. Potential toxicities could be related to its mechanism of action, such as excessive vasodilation or effects on cGMP signaling in peripheral tissues. Standard preclinical toxicology studies would be required to assess its safety.
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| References | |
| Additional Infomation |
Zagociguat (CAS#: 2201048-82-8) is a stimulator of soluble guanylate cyclase (sGC) with central nervous system penetrance. It is being investigated for the treatment of serious neurodegenerative disorders, including Alzheimer's disease. By enhancing NO signaling and increasing cGMP production, it may offer neuroprotective benefits. It is an investigational agent and is not yet approved for clinical use.
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| Molecular Formula |
C16H10F4N6
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| Molecular Weight |
362.284415721893
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| Exact Mass |
362.09
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| CAS # |
2201048-82-8
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| PubChem CID |
134304734
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
492
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC=CC=1CC1C2=NC=CN2C=C(C2=NNC(C(F)(F)F)=N2)N=1
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| InChi Key |
GTKNNCQKFKGSHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10F4N6/c17-10-4-2-1-3-9(10)7-11-14-21-5-6-26(14)8-12(22-11)13-23-15(25-24-13)16(18,19)20/h1-6,8H,7H2,(H,23,24,25)
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| Chemical Name |
8-[(2-fluorophenyl)methyl]-6-[5-(trifluoromethyl)-1H-1,2,4-triazol-3-yl]imidazo[1,2-a]pyrazine
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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: 250 mg/mL (690.07 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 | 2.7603 mL | 13.8015 mL | 27.6030 mL | |
| 5 mM | 0.5521 mL | 2.7603 mL | 5.5206 mL | |
| 10 mM | 0.2760 mL | 1.3801 mL | 2.7603 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06961344
Conditions:Mitochondrial Encephalopathy, Lactic Acidosis and Stroke-Like Episodes (MELAS Syndrome)Link: https://clinicaltrials.gov/ct2/show/NCT06402123
Conditions:Mitochondrial Encephalopathy, Lactic Acidosis and Stroke-Like Episodes (MELAS Syndrome)Link: https://clinicaltrials.gov/ct2/show/NCT04798989
Conditions:Alzheimer's Disease With Vascular Pathology
Title:Phase 2a Study of IW-6463 in Adults Diagnosed With Mitochondrial Encephalomyopathy, Lactic Acidosis, and Stroke-like Episodes (MELAS)
Status:Terminated
updateDate:2024-08-29
Ctid:NCT04475549
Link: https://clinicaltrials.gov/ct2/show/NCT04475549
Conditions:MELASLink: https://clinicaltrials.gov/ct2/show/NCT03856827
Conditions:OtherLink: https://clinicaltrials.gov/ct2/show/NCT04240158
Conditions:OtherLink: https://clinicaltrials.gov/ct2/show/NCT04972227
Conditions:SchizophreniaProducts are for research use only; We do not sell to patients
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