| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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CP-100356 HCl (CP100356), the hydrochloride salt of CP-100356, is a novel and potent affinity P-glycoprotein (P-gp) inhibitor, inhibiting protypical ABC transporter.
| ln Vitro |
In human MDR1-transfected MDCKII cells, CP-100356 hydrochloride (0.1-15 μM; only 30 minutes) inhibits the transport of digoxin and calcein-AM solution, with an IC50 of 0.50 μM and digoxin, respectively. CP-100356 hydrochloride (0.064–200 μM; 5 min) suppresses the toxin estrogen 17β 1.2 μM that is mediated by OATP1B1. In investigations of equilibrium inhibition using CP-100356 Hydrochloride (0-50 μM; 10-30 minutes) -D-aldehyde acid solution, the enzymatic activity of monomeric P450 inside P4503A4 is inhibited (IC50 = approximately 66 μM). No inhibition (IC50>50 μM) is observed[1].
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| ln Vivo |
CP-100356 Systemic exposure to fexofenadine at higher dosages (increases in Cmax and AUC at 24 mg/kg of 36 and 80 times, respectively) [1].
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| References |
| Molecular Formula |
C31H37CLN4O6
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|---|---|
| Molecular Weight |
597.109
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| Exact Mass |
596.24
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| CAS # |
142715-48-8
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| Related CAS # |
142716-85-6;142715-48-8(HCl);
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| PubChem CID |
71312025
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| Appearance |
White to off-white solid powder
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| LogP |
5.187
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
42
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| Complexity |
796
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WWCHXVYTCMPAMV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H36N4O6.ClH/c1-36-24-8-7-19(13-25(24)37-2)9-11-32-31-33-23-17-29(41-6)28(40-5)16-22(23)30(34-31)35-12-10-20-14-26(38-3)27(39-4)15-21(20)18-35;/h7-8,13-17H,9-12,18H2,1-6H3,(H,32,33,34);1H
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| Chemical Name |
4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-(3,4-dimethoxyphenethyl)-6,7-dimethoxyquinazolin-2-amine hydrochloride
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| Synonyms |
CP-100356 HClCP 100356 CP-100356CP100356 CP-100356 hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~11.36 mg/mL (~19.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.14 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.4 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.14 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.4 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.14 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6747 mL | 8.3737 mL | 16.7473 mL | |
| 5 mM | 0.3349 mL | 1.6747 mL | 3.3495 mL | |
| 10 mM | 0.1675 mL | 0.8374 mL | 1.6747 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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