Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
EC50: 23 nM (CFTR)[1]
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ln Vitro |
With an EC50 of 342 nM in the presence of 50 nM Forskolin, CFTR activator 1 (compound 16d) (30 nM-10 μM) potently activates the CFTR chloride channel in FRT cells expressing human CFTR[1]. The channel activities of ANO1 and VRAC in FRT cells expressing human ANO1 and in LN215 cells expressing a halide sensor YFP-F46L/H148Q/I152L are not affected by CFTR activator 1 (30 μM; pretreatment for 10 min or 5 min)[1]. In CHO-K1 cells, CFTR activator 1 (30 μM; 10 min) marginally raises the cAMP level in comparison to the control[1]. CorE and ConjE cell viability is unaffected by CFTR activator 1 (30 μM; 48 h)[1].
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ln Vivo |
In a mouse model of dry eye disease (DED), CFTR activator 1 (compound 16d) (2060 μM; 5 μL of eye drops; three times a day for 10 d) reduces corneal erosion and increases tear secretion. In the cornea and conjunctiva of DED animals, CFTR activator 1 decreases the mRNA expression of pro-inflammatory cytokines such as IL-1β, IL-17, TNF-α, and MMP2[1]. The male New Zealand White Rabbit's CFTR-expressing target tissues, the cornea and conjunctiva, are well dispersed in CFTR activator 1 (0.1 mg/eye; single topical instillation of eye drops), which is sustained for an extended length of time with minimal systemic exposure[1].
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Animal Protocol |
Animal/Disease Models: Eight weeks old female C57BL/6J mice were injected Scopolamine hydrobromide[1]
Doses: 2060 μM, 5 μL, and maintained for 30 s Route of Administration: Eye drop application was done in both eyes, three times a day (11:00 am, 2:00 pm, 5:00 pm) for 10 days Experimental Results: Enhanced tear secretion and improved corneal erosion. decreased mRNA expression of pro-inflammatory cytokines including IL-1β, IL-17, and TNF-α and MMP2 in cornea and conjunctiva. |
References |
[1]. Kim BY, et, al. Synthetic Strategies for Improving Solubility: Optimization of Novel Pyrazolo[1,5- a]pyrimidine CFTR Activator That Ameliorates Dry Eye Disease. J Med Chem. 2023 Jan 12;66(1):413-434.
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Molecular Formula |
C27H27N5O4
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Molecular Weight |
485.53
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CAS # |
2768261-09-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
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
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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 | 2.0596 mL | 10.2980 mL | 20.5960 mL | |
5 mM | 0.4119 mL | 2.0596 mL | 4.1192 mL | |
10 mM | 0.2060 mL | 1.0298 mL | 2.0596 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.