ChemicalBook > CAS DataBase List > LP-935509

LP-935509

Product Name
LP-935509
CAS No.
1454555-29-3
Chemical Name
LP-935509
Synonyms
LP-935509;LP-935509 (LP935509;LP-935509, 10 mM in DMSO;Isopropyl 4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate;4-[3-(2-methoxy-pyridin-3-yl)-pyrazolo[1,5-a]pyrimidin-5-yl]-piperazine-1-carboxylicacid isopropyl ester;1-Piperazinecarboxylic acid, 4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-, 1-methylethyl ester;orally active,AP2-associated kinase 1,LP 935509,Inhibitor,brain-penetrant,SARS coronavirus,LP-935509,pain,spinal nerve ligation,SARS-CoV,Cyclin G-associated Kinase (GAK),Antinociceptive,AAK1,infection,LP935509,chronic constriction injury,inhibit,streptozotocin,formalin,Auxilin 2,ATP-competitive,SNL,Adaptor-associated Kinase 1
CBNumber
CB73159379
Molecular Formula
C20H24N6O3
Formula Weight
396.44
MOL File
1454555-29-3.mol
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LP-935509 Property

Density 
1.34±0.1 g/cm3(Predicted)
solubility 
DMSO: Soluble
pka
1.73±0.12(Predicted)
form 
Solid
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Axon Medchem
Product number
Axon2638
Product name
LP-935509
Purity
99%
Packaging
50mg
Price
$495
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
KIN0002499
Product name
LP-935509
Purity
95.00%
Packaging
5MG
Price
$503.18
Updated
2021/12/16
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LP-935509 Chemical Properties,Usage,Production

Description

LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).

Uses

LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research[1].

in vivo

LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior[1].
LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model[1].
LP-935509 (IV (1 mg/kg) or orally (10 mg/kg); once) has 100% oral bioavailability and a plasma half life of 3.6 hours[1].

Animal Model:Male C57BL/6J mice (with SNL(spinal nerve ligation) injury, n=8-10 male mice per group)[1]
Dosage:0, 10, 30 and 60 mg/kg (10 ml/kg)
Administration:PO, single
Result:Caused a dose-dependent reduction in phase II paw flinches that was significantly lower than the vehicle-treated animals; exhibited a dose-dependent reversal of the mechanical allodynia; Caused a robust reduction in pain behavior.
Animal Model:Male Sprague-Dawley rats (CCI (chronic constriction injury)-operated rats)[1]
Dosage:0, 0.1, 0.3, 1, 3, 10, or 30 mg/kg
Administration:PO, two daily, for 5 days
Result:Caused a dose-dependent reversal of thermal hyperalgesia, cold allodynia, mechanical allodynia, and mechanical hyperalgesia in CCI animals. Reversed the behavioral deficits, with ED50 values ranging from 2 mg/kg to 10 mg/kg.
Animal Model:Male Sprague-Dawley rats[1]
Dosage:1 mg/kg (IV), 10 mg/kg (PO)
Administration:IV, PO; once (Pharmacokinetic Analysis)
Result:Had 100% oral bioavailability and a plasma half life of 3.6 hours; The Cmax for the 10 mg/kg oral dose was 5.2 μM at 0.5-hour postdose; had a plasma-free fraction of 2.6% in mice. Brain drug levels exceeded plasma drug levels with a brain/plasma drug ratio typically between 3 and 4, showing that LP-935509 was highly brain-penetrant.

References

[1] Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. DOI:10.1124/jpet.116.235333

[2] Mushtaq, et al. Role Of Endocytic Machinery Regulators in EGFR Traffic and Viral Entry (2021). Theses & Dissertations. 532.
[3] QINFANG LIU. Dysregulation of the AP2M1 phosphorylation cycle by LRRK2 impairs endocytosis and leads to dopaminergic neurodegeneration[J]. Science Signaling, 2021, 14 693. DOI: 10.1126/scisignal.abg3555

LP-935509 Preparation Products And Raw materials

Raw materials

Preparation Products

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LP-935509 Suppliers

China 28 United States 3 Global 31
Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Fax
QQ: 12922499
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huahero21@sina.com
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China
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Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71615
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Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
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9572
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Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
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9025
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TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
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32469
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Fax
86-571-88216895
Email
sales@hzclap.com
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CHINA
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Shanghai Dongyang Biotechnology Co., Ltd.
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0512-0512-13601744364 13601744364
Email
chemsharker@126.com
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China
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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QQ 3610331285
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sales@chemegen.com
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China
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Jinan Jiuli Biotechnology Co. , Ltd.
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15865264761
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486064515@qq.com
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China
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4894
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1454555-29-3, LP-935509Related Search:


  • LP-935509
  • 4-[3-(2-methoxy-pyridin-3-yl)-pyrazolo[1,5-a]pyrimidin-5-yl]-piperazine-1-carboxylicacid isopropyl ester
  • orally active,AP2-associated kinase 1,LP 935509,Inhibitor,brain-penetrant,SARS coronavirus,LP-935509,pain,spinal nerve ligation,SARS-CoV,Cyclin G-associated Kinase (GAK),Antinociceptive,AAK1,infection,LP935509,chronic constriction injury,inhibit,streptozotocin,formalin,Auxilin 2,ATP-competitive,SNL,Adaptor-associated Kinase 1
  • 1-Piperazinecarboxylic acid, 4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-, 1-methylethyl ester
  • Isopropyl 4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate
  • LP-935509, 10 mM in DMSO
  • LP-935509 (LP935509
  • 1454555-29-3