| Size | Price | Stock | Qty |
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LP-935509 (LP935509) is a novel and potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1) with the potential to Treat Neuropathic Pain. It inhibits AAK1 with IC50 of 3.3 nM.
| ln Vitro |
LP-935509 has an IC50 value of 2.8 ± 0.4 nM for μ2 phosphorylation inhibition and an IC50 value of 3.3 ± 0.7 nM for phosphorylation of peptides generated from μ2 protein[1]. The reduction of SARS-CoV-2 S-RBD internalization into host cells is demonstrated by LP-935509 in a dose-dependent manner [2].
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| ln Vivo |
The oral single-dose medication LP-935509 (0–60 mg/kg) dramatically lowers pain behaviors [1]. ?In a CCI model, oral LP-935509 (0.1–30 mg/kg; single dosage) reverses thermal hyperalgesia in a dose-dependent manner [1]. ?LP-935509 (intravenous 1 mg/kg or oral 10 mg/kg once) has a 3.6-hour plasma half-life and 100% oral bioavailability [1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice (with SNL (spinal nerve ligation) injury, n=8-10 male mice per group) [1]
Doses: 0, 10, 30 and 60mg/kg (10ml/kg) Route of Administration: PO, Single Outcome: Produced a dose-dependent reduction in stage II paw withdrawal that was Dramatically lower than in vehicle-treated animals; demonstrated a dose-dependent reversal of mechanical allodynia; resulted in a substantial reduction in pain behaviors. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (CCI (chronic constriction injury) operated rat) [1] Doses: 0, 0.1, 0.3, 1, 3, 10 or 30 mg/kg Route of Administration: po (po (oral gavage)) daily Two, 5 consecutive day Experimental Results: Produced dose-dependent reversal of thermal hyperalgesia, cold hyperalgesia, mechanical hyperalgesia, and mechanical hyperalgesia in CCI animals. Reversal of behavioral deficits, ED50 values range from 2 mg/kg to 10 mg/kg. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat[1] Doses: 1 mg/kg (IV), 10 mg/kg (PO) Route of Administration: IV, PO; once (pharmacokinetic/PK/PK analysis) Experimental Results: Oral bioavailability The conc |
| References |
| Molecular Formula |
C20H24N6O3
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|---|---|
| Molecular Weight |
396.442963600159
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| Exact Mass |
396.191
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| Elemental Analysis |
C, 60.59; H, 6.10; N, 21.20; O, 12.11
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| CAS # |
1454555-29-3
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| Related CAS # |
1454555-29-3;
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| PubChem CID |
86697436
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
556
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GOOYSJIWTIHOGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24N6O3/c1-14(2)29-20(27)25-11-9-24(10-12-25)17-6-8-26-18(23-17)16(13-22-26)15-5-4-7-21-19(15)28-3/h4-8,13-14H,9-12H2,1-3H3
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| Chemical Name |
propan-2-yl 4-[3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl]piperazine-1-carboxylate
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| Synonyms |
LP-935509 LP 935509 LP935509
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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) |
DMSO : ~50 mg/mL (~126.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.25 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 (5.25 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 (5.25 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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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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