| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
Kv7.2/7.3 and Kv7.3/7.5 potassium channels[1][2]
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| ln Vitro |
According to results from three assessments in two different human hepatocyte lots (LBN and HU4165), ICA-105665 (PF-04895162) does not exhibit potent cytotoxic properties in THLE and HepG2 cell lines (IC50 ~192 μM and 130 μM after 72 hours, respectively) or in human hepatocytes (AC50 for cell loss at 48 hours was >125 μM). Human hepatocytes treated with ICA-105665 (PF-04895162) at doses >11 μM for 25 minutes[1] have impaired mitochondrial respiratory reserve.
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| ln Vivo |
In a 7-day rat toxicology investigation, dose-dependent increases of alanine aminotransferase (ALT), which may be suggestive of liver injury, were noted for ICA-105665 (PF-04895162). However, ALT elevations were not verified in a follow-up 7-day investigation, and no histological evidence of liver impairment was found. Additionally, transaminase increases and liver toxicity were not observed in 28-day or 6-month toxicity trials conducted in rats, and toxicity investigations lasting up to nine months in cynomolgus monkeys were similarly negative[2]. In several animal models, such as maximal electroshock, 6 Hz seizures, pentylenetetrazole, and electrical kindling, ICA-105665 (PF-04895162) has shown broad spectrum antiseizure efficacy at dosages ranging from <1 to 5 mg/kg[3].
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| References |
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| Additional Infomation |
ICA-105665 is a novel small molecule compound for the treatment of epilepsy. It is a novel opener of the KCNQ ion channel which in preclinical studies has demonstrated a broad spectrum of activity in models of epilepsy. In addition, ICA-105665 has also demonstrated activity in certain models of neuropathic pain.
Drug Indication Investigated for use/treatment in epilepsy. Mechanism of Action ICA-105665 is an activator of subtypes of KCNQ ion channels, which are attractive targets for the treatment of epilepsy based on their function and genetic linkage to a seizure disorder. |
| Molecular Formula |
C19H15F2N3O2
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|---|---|
| Molecular Weight |
355.338111162186
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| Exact Mass |
355.113
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| CAS # |
2694728-63-5
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| PubChem CID |
70838704
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| Appearance |
White to off-white solid powder
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| LogP |
2.6
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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 |
3
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| Heavy Atom Count |
26
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| Complexity |
600
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QVQACHQOSXTOLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15F2N3O2/c20-13-5-1-11(2-6-13)9-17(25)23-24-18(12-3-4-12)22-16-10-14(21)7-8-15(16)19(24)26/h1-2,5-8,10,12H,3-4,9H2,(H,23,25)
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| Chemical Name |
N-(2-cyclopropyl-7-fluoro-4-oxoquinazolin-3-yl)-2-(4-fluorophenyl)acetamide
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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 (703.55 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 | 2.8142 mL | 14.0710 mL | 28.1421 mL | |
| 5 mM | 0.5628 mL | 2.8142 mL | 5.6284 mL | |
| 10 mM | 0.2814 mL | 1.4071 mL | 2.8142 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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