| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
For PK 11195, the median IC50 values were 14.2 μM for L. amazonensis, L at 8.2 μM. major, and L at 3.5 μM. braziliensis. The value of L's selectivity index. amazonensis was 13.7, suggesting that PK 11195 is safe for use in upcoming tests on mammals. There were observed time- and dose-dependent decreases in the number of live intracellular parasites, the number of parasites per infected macrophage, and the proportion of infected macrophages. Several morphological alterations suggestive of autophagy were detected by electron microscopy. It's interesting to note that L had lower MCP-1 and superoxide levels. macrophages infected with Amazonensis and treated with PK 11195 [1].
|
|---|---|
| References |
[1]. Guedes CES, et al. In vitro evaluation of the anti-leishmanial activity and toxicity of PK-11195. Mem Inst Oswaldo Cruz. 2018 Feb 5;113(4):e170345.
|
| Additional Infomation |
PK-11195 is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine It has a role as an antineoplastic agent. It is a member of isoquinolines, a monocarboxylic acid amide, an aromatic amide and a member of monochlorobenzenes.
|
| Molecular Formula |
C21H21CLN2O
|
|---|---|
| Molecular Weight |
352.862
|
| Exact Mass |
352.134
|
| CAS # |
85532-75-8
|
| PubChem CID |
1345
|
| Appearance |
Off-white to light brown solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
511.7±45.0 °C at 760 mmHg
|
| Melting Point |
74-75
|
| Flash Point |
263.3±28.7 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.611
|
| LogP |
4.58
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
457
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N(C(CC)C)C)C1C=C2C(C=CC=C2)=C(C2C(Cl)=CC=CC=2)N=1
|
| InChi Key |
RAVIZVQZGXBOQO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
|
| Chemical Name |
N-(sec-butyl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide
|
| Synonyms |
PK-11195 PK 11195PK11195
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~70.85 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.89 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 (5.89 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8340 mL | 14.1699 mL | 28.3399 mL | |
| 5 mM | 0.5668 mL | 2.8340 mL | 5.6680 mL | |
| 10 mM | 0.2834 mL | 1.4170 mL | 2.8340 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00205595 | UNKNOWN STATUS | Device: Positron Emission Tomography | Normal Aging | Amsterdam UMC, location VUmc | 2001-02 | Phase 1 |
| NCT02092883 | COMPLETED | Drug: ACTH | Infantile Spasms | Wayne State University | 2013-03 | Phase 4 |
| NCT02207075 | COMPLETED | Drug: [C11]PK-1195 PET scan | Secondary Progressive Multiple Sclerosis | Weill Medical College of Cornell University | 2014-07 | |
| NCT04239820 | ACTIVE, NOT RECRUITING | Radiation: Imaging | Multiple Sclerosis | Turku University Hospital | 2020-01-10 | |
| NCT00205582 | UNKNOWN STATUS | Device: Positron Emission Tomography | Traumatic Brain Injury | Amsterdam UMC, location VUmc | 2001-05 | Phase 1 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
