ChemicalBook > CAS DataBase List > N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)

N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)

Product Name
N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)
CAS No.
1079400-07-9
Chemical Name
N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)
Synonyms
PF 04531083;PF-04531083 >=98% (HPLC);PF 04531083, 10 mM in DMSO;N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide;1H-Pyrazole-5-carboxamide, N-[6-amino-5-(2-chloro-5-methoxyphenyl)-2-pyridinyl]-1-methyl-;PF04531083,inhibit,Inhibitor,Na+ channels,PF 04531083,PF-04531083,Sodium Channel,Na channels;N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)
CBNumber
CB63509146
Molecular Formula
C17H16ClN5O2
Formula Weight
357.79
MOL File
1079400-07-9.mol
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N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095) Property

Boiling point:
471.0±45.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 125 mg/mL (349.37 mM)
form 
Solid
pka
11.32±0.70(Predicted)
color 
Light yellow to yellow
InChI
1S/C17H16ClN5O2/c1-23-14(7-8-20-23)17(24)22-15-6-4-11(16(19)21-15)12-9-10(25-2)3-5-13(12)18/h3-9H,1-2H3,(H3,19,21,22,24)
InChIKey
ZRJGMDIPCQOGNI-UHFFFAOYSA-N
SMILES
Clc1c(cc(cc1)OC)c2c(nc(cc2)NC(=O)c3[n](ncc3)C)N
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
Hazard Classifications
Acute Tox. 4 Oral
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0025617
Product name
PF04531083
Purity
98.24%
Packaging
5mg
Price
$100
Updated
2021/12/16
ChemScene
Product number
CS-0025617
Product name
PF04531083
Purity
98.24%
Packaging
10mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-0025617
Product name
PF04531083
Purity
98.24%
Packaging
25mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0025617
Product name
PF04531083
Purity
98.24%
Packaging
50mg
Price
$580
Updated
2021/12/16
ChemScene
Product number
CS-0025617
Product name
PF04531083
Purity
98.24%
Packaging
100mg
Price
$900
Updated
2021/12/16
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N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095) Chemical Properties,Usage,Production

Uses

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain[1][2][3].

Biological Activity

PF-04531083 is an orally available, potent and selective sodium channel Nav1.8 blocker. PF-04531083 was designated as a potential treatment of pain.

in vivo

PF 04531083 (1 mg/kg, i.v.; or 2 mg/kg, p.o.) is a low clearance compound with good bioavailability ～60% in rats[2].
PF 04531083 (40 mg/kg; 1.5 h) is efficacious in the tibial nerve transection (TNT) induced mechanical allodynia model in rat[2].
PF 04531083 inhibits native tetrodotoxin-resistant (TTX-R) currents in rodent dorsal root ganglion (DRG) neurons with an IC50 of 0.54 μM[2].
PF 04531083 (40 mg/kg; 1.5 h) improves baseline breathing in Tcf4tr/+ mice[3].
PF 04531083 (30 min before test) improves behavioral abnormalities associated with Pitt-Hopkins syndrome (PTHS) in Tcf4tr/+ mice[3].

Animal Model:Tcf4+/+ and Tcf4tr/+ mice [3]
Dosage:40 mg/kg
Administration:Intraperitoneal injection (i.p.), 1.5 h before test
Result:Decreased episodes of hyperventilation, increased the occurrence of spontaneous sighs, diminished duration of post-sigh apnea and improved the CO2 minute ventilatory response in Tcf4tr/+ mice.
Showed stable respiratory activity in Tcf4+/+ mice.
Showed a robust increase in respiratory activity (62.5% increase in minute ventilation from 3 to 7% CO2) in Tcf4tr/+ pups.

IC 50

Nav1.8

References

[1] Yekkirala AS, et al. Breaking barriers to novel analgesic drug development. Nat Rev Drug Discov. 2017 Aug;16(8):545-564. DOI:10.1038/nrd.2017.87
[2] Bagal SK, et al. Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain. ACS Med Chem Lett. 2015 Apr 29;6(6):650-4. DOI:10.1021/acsmedchemlett.5b00059
[3] Cleary CM, et al. Disordered breathing in a Pitt-Hopkins syndrome model involves Phox2b-expressing parafacial neurons and aberrant Nav1.8 expression. Nat Commun. 2021 Oct 13;12(1):5962. DOI:10.1038/s41467-021-26263-2

N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095) Preparation Products And Raw materials

Raw materials

Preparation Products

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N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095) Suppliers

CHINA 28 United States 2 Global 30
Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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info@efebio.com
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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Beijing Solarbio Science & Tecnology Co., Ltd.
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010-50973130 18101056239
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3193328036@qq.com
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Wuxi AppTec
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022-59987777 13552403979
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jia_guoqiang@wuxiapptec.com
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China
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Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
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liming@bio-fount.com
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China
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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InvivoChem
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+1-708-310-1919 +1-13798911105
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708-557-7486
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sales@invivochem.cn
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
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86-571-88216897,88216896 13588875226
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86-571-88216895
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sales@hzclap.com
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Shanghai hongqu biomedical technology co. LTD
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88888888888
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hongquchem@qq.com
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ShangHai ChuanQian Chemcial Technique Centre
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1079400-07-9, N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)Related Search:


  • N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide(WX150095)
  • N-(6-amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide
  • PF 04531083
  • 1H-Pyrazole-5-carboxamide, N-[6-amino-5-(2-chloro-5-methoxyphenyl)-2-pyridinyl]-1-methyl-
  • PF-04531083 >=98% (HPLC)
  • PF04531083,inhibit,Inhibitor,Na+ channels,PF 04531083,PF-04531083,Sodium Channel,Na channels
  • PF 04531083, 10 mM in DMSO
  • 1079400-07-9