| Size | Price | Stock | Qty |
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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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| ln Vitro |
Linopirdine (DuP 996) suppresses IC with an IC50 of 16.3 μM, as assessed by moderate ultra-instantaneous tail current, or ImAHP. At 100 μM, linapirdine barely suppresses the slow levels of K+ leakage current (IL), transient outward current (IA), delay regulator (IK), and IAHP by 28, 37, 36, and 52%, in that order. Linopirdine (IC50>300 μM) essentially has no effect on the Na+/K+ mixed inward corrective current IQ[1]. An agonist of TRPV1 (transient transient potential vanilloid type 1) is linopirdine [3].
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|---|---|
| ln Vivo |
Up to 15% of MAP is temporarily increased (10–15 minutes) by linopridine (DuP 996; IV; 0.1-6 mg/kg; escalating dose) and dose stress [2].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (300-350) g)[2]
Doses: 0.1, 0.5, 1, 3, 6 mg/kg Route of Administration: 5 intravenous (iv) (iv)bolus injections, dose escalation Experimental Results: Transient and dose Dependently increases MAP by up to 15%. |
| References |
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| Additional Infomation |
Linopirdine is a member of indoles.
|
| Molecular Formula |
C26H21N3O
|
|---|---|
| Molecular Weight |
391.47
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| Exact Mass |
391.168
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| CAS # |
105431-72-9
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| Related CAS # |
Linopirdine dihydrochloride;113168-57-3
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| PubChem CID |
3932
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.255 g/cm3
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| Boiling Point |
655.9ºC at 760 mmHg
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| Flash Point |
350.5ºC
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| Vapour Pressure |
4.45E-17mmHg at 25°C
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| Index of Refraction |
1.669
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| LogP |
4.943
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
555
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YEJCDKJIEMIWRQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H21N3O/c30-25-26(18-20-10-14-27-15-11-20,19-21-12-16-28-17-13-21)23-8-4-5-9-24(23)29(25)22-6-2-1-3-7-22/h1-17H,18-19H2
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| Chemical Name |
1-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one
|
| Synonyms |
DuP-996; DuP 996; Linopirdine
|
| HS Tariff Code |
2934.99.9001
|
| 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 : ~125 mg/mL (~319.32 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.31 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (5.31 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 20.8 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: ≥ 2.08 mg/mL (5.31 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 | 2.5545 mL | 12.7724 mL | 25.5447 mL | |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1089 mL | |
| 10 mM | 0.2554 mL | 1.2772 mL | 2.5545 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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