| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CPL500036 (0.1–10 μM; 5 min) inhibited hERG tail currents in hERG-HEK-293 transfected cells with an IC25 value of 3.2 μM[1]. CPL500036 (0.0457–100 μM; 14 days) did not affect key cardiac spheroid health parameters at concentrations up to 100 μM, but it did impair DNA structure in 3D cardiac spheroids derived from human pluripotent stem cells with an IC50 value of 37.4 μM[1]. CPL500036 (8 nM–60 μM; 72 h) was non-cytotoxic to NCI-H1299, HepG2, and SH-SY5Y cell lines at concentrations up to 60 μM[1].
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| ln Vivo |
CPL500036 (0.15–2 mg/kg; orally; single dose) induces dose-dependent rigidity in male Sprague-Dawley rats[1]. CPL500036 (0.1–0.3 mg/kg; orally; single acute dose, in combination with levodopa/benserazide for 16 consecutive days) dose-dependently improves sensorimotor deficits in 6-hydroxydopamine-induced rats[2].
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| Animal Protocol |
Animal/Disease Models:Sprague-Dawley mice (male, approximately 300 g) [1]
Doses: 0.15 mg/kg; 0.3 mg/kg; 0.6 mg/kg; 2 mg/kg Route of Administration: Oral; Single dose Experimental Results: The 0.15 mg/kg dose did not induce rigidity. The 0.3 mg/kg dose induced mild rigidity only at 210 and 240 minutes after administration. The 0.6 mg/kg dose induced rigidity from 120 to 240 minutes after administration, but its effect was weaker than that of the positive control drug haloperidol. The 2 mg/kg dose produced a potent rigidity effect comparable to that of haloperidol. The minimum effective dose (MED) for treating rigidity was confirmed by AUC data to be 0.6 mg/kg. Animal/Disease Models:Wistar Han (male, initial weight 270-300 g, unilateral medial forebrain tract injury, 6-hydroxydopamine) [2] Doses: 0.1 mg/kg (acute single dose; chronic daily in combination with levodopa/benserazide); 0.3 mg/kg (acute single dose; chronic daily in combination with levodopa/benserazide) Route of Administration: Oral; acute single dose; once daily for 16 days (in combination with levodopa/benserazide) Experimental Results: After acute administration, forelimb use impairment in gait tests was dose-dependently reversed. In the second dose test, the 0.3 mg/kg acute dose group showed complete recovery of forelimb use symmetry in cylinder tests. Neither acute dose affected whisker test defects or injury-induced rigidity. Acute combination therapy with 0.1 mg/kg levodopa significantly improved impaired forelimb function in the whisker test. Acute combination therapy with 0.3 mg/kg levodopa reduced levodopa-induced contralateral rotation. Chronic combination therapy with 0.3 mg/kg completely reversed forelimb asymmetry in the whisker test. Neither chronic dose altered the anti-Parkinson's disease effect of levodopa in gait, rigidity, or rotation tests. Compared with injured rats, chronic combination therapy with 0.3 mg/kg significantly improved impaired forelimb function in the gait test during the withdrawal period. |
| References |
|
| Molecular Formula |
C19H15N7
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|---|---|
| Molecular Weight |
341.37
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| CAS # |
1829530-11-1
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC1=NC=C(C)N2N=C(C3=NC4=NC(C5=CC=CC=C5)=CN4C=C3)N=C21
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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 | 2.9294 mL | 14.6469 mL | 29.2937 mL | |
| 5 mM | 0.5859 mL | 2.9294 mL | 5.8587 mL | |
| 10 mM | 0.2929 mL | 1.4647 mL | 2.9294 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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