ChemicalBook > CAS DataBase List > 2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-

2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-

Product Name
2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-
CAS No.
1931994-81-8
Chemical Name
2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-
Synonyms
BAY-845;BAY-1834845;Zabedosertib;Zabedosertib, 10 mM in DMSO;N-(6-(2-Hydroxypropan-2-yl)-2-(2-(methylsulfonyl)ethyl)-2H-indazol-5-yl)-6-(trifluoromethyl)picolinamide;N-[6-(2-Hydroxy-2-propyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide;N-[6-(1-hydroxy-1-methyl-ethyl)-2-(2-methylsulfonylethyl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide;2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-
CBNumber
CB38237502
Molecular Formula
C20H21F3N4O4S
Formula Weight
470.47
MOL File
1931994-81-8.mol
More
Less

2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)- Property

Boiling point:
620.7±55.0 °C(Predicted)
Density 
1.44±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 125 mg/mL (265.69 mM; ultrasonic and warming and heat to 60°C)
pka
11.53±0.43(Predicted)
form 
Solid
color 
White to off-white
More
Less

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..…

More
Less

2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)- Chemical Properties,Usage,Production

Uses

Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors[1]. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation[2].

in vivo

Zabedosertib (150 mg/kg, p.o., twice) prevents lung injury and reduces inflammation in LPS induced ARDS in BALB/c mice[2].
Zabedosertib inhibits IL-β(p.o., 40-80 mg/kg, once), LPS (p.o., 10-40 mg/kg, once) and Imiquimod (p.o., 15-150 mg/kg, twice daily for 7 days) induced inflammation[3].
Zabedosertib has a Pharmacokinetic profile in rats[3]:
Pharmacokinetic Analysis of Zabedosertib in rats[1]

speciesDoseiv (mg/kg)AUCnorm,iv (kg·h/L)CLblood (L/h/kg)Vss (L/kg)T1/2,iv (h)Dosepo(mg/kg)AUCnorm,po (kg·h/L))Cmax,norm (kg/L)Tmax (h)F (%)
rat0.55.60.240.924.22.05.30.554.094
dog0.5150.0881.6171.0150.572.0104
Animal Model:LPS induced ARDS in BLAB/c mice[2]
Dosage:150 mg/kg
Administration:p.o., twice (30 min before and 6 h after LPS-injection or 4 h and 12 h after LPS-injection)
Result:Decreased inflammatory cells infiltration.
Combination of Zabedosertib and DEX ( HY-14648) decreased T-cells, monocytes and macrophages.
Animal Model:BALB/c mice[3]
Dosage:IL-β:40-80 mg/kg, LPS: 10-40 mg/kg, Imiquimod: 15-150 mg/kg
Administration:oral gavage, IL-β: once, LPS: once, Imiquimod: twice daily for 7 days
Result:Inhibited IL-β, LPS induced inflammation in a dose-dependent manner. Inhibited Imiquimod induced inflammation.

IC 50

IRAK4: 3.55 nM (IC50)

References

[1] Bothe, Ulrich; Siebenreicher, Holger; Schmidt, Nicole; Nubbemeyer, Reinhard; Boemer, Ulf; Guenther, Judith; Steuber, Holger; Lange, Martin; Stegmann, Christian; Sutter, Andreas; et al.New substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs.WO2016083433A1
[2] Li Q, et al., Oral IRAK4 inhibitor BAY-1834845 prevents acute respiratory distress syndrome. Biomed Pharmacother. 2022 Sep;153:113459. DOI:10.1016/j.biopha.2022.113459
[3] Bothe U, et al., Discovery of IRAK4 Inhibitors BAY1834845 (Zabedosertib) and BAY1830839. J Med Chem. 2024 Jan 25;67(2):1225-1242. DOI:10.1021/acs.jmedchem.3c01714

2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)- Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)- Suppliers

China 29 United States 1 Global 30
Shanghai XingMo Biotechnology Co., Ltd.
Tel
+86 13524779951; 13524779951
Fax
QQ: 2075692521
Email
2075692521@qq.com
Country
China
ProdList
294
Advantage
55
Shanghai Haozhixiang Biotechnology Co., Ltd
Tel
526763801 13301653310
Fax
+86-21-51619052
Email
526763801@qq.com
Country
China
ProdList
9433
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
7999
Advantage
62
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9505
Advantage
58
Suzhou Rovathin Foreign Trade Co.,Ltd
Tel
0512-65816829 18662214788
Fax
0512-65816829
Email
info@rovathin.com.cn
Country
China
ProdList
9976
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32467
Advantage
58
Shanghai Dongyang Biotechnology Co., Ltd.
Tel
0512-0512-13601744364 13601744364
Email
chemsharker@126.com
Country
China
ProdList
1139
Advantage
58
Hebei Weite Medical Technology Co., Ltd
Tel
13180081292 13180081292
Email
contact@wetogethermed.com
Country
China
ProdList
7825
Advantage
58
Hubei Kele Fine Chemical Co., Ltd
Tel
027-59101668 19945030958
Fax
027-59101668
Email
2223443625@qq.com
Country
China
ProdList
7999
Advantage
58

1931994-81-8, 2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-Related Search:


  • 2-Pyridinecarboxamide, N-[6-(1-hydroxy-1-methylethyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)-
  • BAY-1834845
  • Zabedosertib
  • N-[6-(1-hydroxy-1-methyl-ethyl)-2-(2-methylsulfonylethyl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide
  • N-(6-(2-Hydroxypropan-2-yl)-2-(2-(methylsulfonyl)ethyl)-2H-indazol-5-yl)-6-(trifluoromethyl)picolinamide
  • N-[6-(2-Hydroxy-2-propyl)-2-[2-(methylsulfonyl)ethyl]-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide
  • Zabedosertib, 10 mM in DMSO
  • BAY-845
  • 1931994-81-8